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Prezista darunavir 150 mg Tablet, Film Coated, 240-count — NDC 59676-0564-01 package photo
Label image from the product's FDA listing (DailyMed) — may show a different pack size or an older label revision.

Prezista darunavir 150 mg Tablet, Film Coated, 240-count — NDC 59676-564-01 (Billing 59676-0564-01)

by Janssen Products LP · 240 TABLET, FILM COATED in 1 BOTTLE, PLASTIC

This is a package of 240 tablets of Prezista darunavir 150 mg Tablet, Film Coated from Janssen Products LP, marketed since Apr 2009 and currently FDA-listed. It is this product's only package size.

NDC 59676-0564-01
🏷️ FDA NDC (as labeled) 59676-564-01 billing pads the product segment with a zero
Rx only Brand On market Non-controlled ⇄ Compare with another NDC
🗂️ FDA directory synced Oct 1, 2026 · this listing last changed Jul 24, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →

This page is curated, coded, and maintained by

Compiled from public FDA, CMS, DailyMed, NADAC, and related drug data sources. Editorial policy

NDC database record

One package, one record: these facts belong to NDC 59676-564-01 alone.

Record
FDA NDC Directory package listing · Human prescription drug
Code segments
59676 labeler · 564 product · 01 package
Package marketed since
Apr 27, 2009
Sample package
No — commercial package
Listing certified through
Dec 31, 2026
Billing quantity
240 EA per package
Barcode (UPC)
0359676563013, 0359676562016, 0359676564010, 0359676566304
FDA record last changed
Jul 24, 2026

Identity & classification

Regulatory identifiers FDA, NLM and CMS codes for this package

FDA NDC (as labeled) 59676-564-01
Product NDC 59676-564
11-digit billing NDC 59676056401
NCPDP billing unit EA — each (per item)
RxCUI 670026, 794610, 831868, 831870, 850455, 850457, 1236628, 1236632,
UNII 33O78XF0BW
UPC 0359676563013, 0359676562016, 0359676564010, 0359676566304
Application # NDA021976
SPL Set ID 814301f9-c990-46a5-b481-2879a521a16f
Established class (EPC) Protease Inhibitor
Mechanism of action Cytochrome P450 2D6 Inhibitors; Cytochrome P450 3A Inhibitors; HIV Protease Inhibitors
DEA schedule Non-controlled
Marketing category NDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2009-04-27
Route ORAL
Dosage form TABLET, FILM COATED
Substance DARUNAVIR ETHANOLATE
TE code (Orange Book) AB · RLD · RS

Drug-database identifiers Medi-Span GPI and First Databank GCN / HICL / AHFS classification

GPI-14 12104520000310
GPI class Prezista
GCN Seq No 065191
GCN 23489
HICL code 033842
Ingredient (HICL) Darunavir
HIC1 code W
Therapeutic class — broad (HIC1) Anti-Infecting Agents
HIC2 code W5
Therapeutic class — intermediate (HIC2) Antiviral Agents
HIC3 code W5P
Therapeutic class — specific (HIC3) Antivirals, Hiv-Spec, Non-Peptidic Protease Inhib
AHFS code 08:18.08.08
AHFS class Hiv Protease Inhibitor Antiretrovirals
FDB label name PREZISTA 150 MG TABLET
FDB brand name Prezista
Legend status F — Federal legend — prescription drug or device
Quick answers
  • GSN (GCN sequence number): 065191
  • GCN: 23489
  • GPI-14 (Medi-Span): 12104520000310
  • HICL (First Databank): 033842
  • AHFS class code: 08:18.08.08
  • RxCUI (RxNorm): 670026
Why two NDCs? The FDA registers this code as 59676-564-01 — a 5-3-2 layout, and that's what's printed on the package and shown on DailyMed. For insurance claims, every NDC is standardized to a uniform 11-digit 5-4-2 format by adding a zero to the product segment → 59676-0564-01. Same drug, same package — only the format differs.
Where does this data come from?
Identifiers from the FDA openFDA NDC Directory and Structured Product Labeling; RxCUI from RxNorm (NLM); GPI from Medi-Span; GCN / HIC / AHFS / legend from First Databank.

RxNorm drug class

This medicine belongs to the Protease Inhibitor class.

Pharmacologic class Protease Inhibitor
Drug family (ATC) Protease inhibitors
How it works HIV Protease Inhibitors, Cytochrome P450 2D6 Inhibitors, Cytochrome P450 3A Inhibitors
Where does this data come from?
Therapeutic classes from RxNorm RxClass (U.S. National Library of Medicine) — Established Pharmacologic Class (FDA), ATC drug family (WHO) and mechanism of action, matched by this product’s RxCUI.

Clinical

Label name PREZISTA 150 MG TABLET Ingredient Darunavir
📖 What it is MedlinePlus · NLM

Darunavir is used to treat human immunodeficiency virus (HIV) infection. Darunavir is in a class of medications called protease inhibitors. It works by decreasing the amount of HIV in the blood. Although darunavir does not cure HIV, it may decrease your chance of developing acquired immunodeficiency syndrome (AIDS) and HIV-related illnesses. Taking these medications and making other lifestyle changes may decrease the risk of giving the HIV virus to other people.

Read the full MedlinePlus article ↗
📗 Our plain-language guide HelloPharmacist
  • It treats HIV-1 infection in adults and children 3 years and older. You take it with ritonavir and other HIV medicines. It works by blocking an enzyme the virus needs to mature.
  • Ritonavir boosts darunavir to levels high enough to work, and food helps your body absorb it. Without them, the medicine may not control the virus well. Please don't skip either on...
  • Why do I have to take it with ritonavir and food?
  • The most common are diarrhea, nausea, rash, headache, belly pain, and vomiting. Rash is often mild and may go away as you keep taking it. Call your doctor if the rash is severe or...
📖 Read our full Darunavir guide →
Where does this data come from?
Plain-language summary from MedlinePlus (U.S. National Library of Medicine); supplement & herbal interactions and nutrient depletion data from the Natural Medicines database; our full guide is HelloPharmacist editorial content.

Pricing

A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.

Price systemPer eachPer package
Retail pharmacies payNADAC · weekly Not in the retail survey — common for institutional, discontinued, or low-volume packs.
Medicaid paysCMS SDUD · 12 mo No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data.
Medicare drug plans payPart D · Q2 2026 $9.01 $2,161.92 / 240 tablets
Where does this data come from?
NADAC (National Average Drug Acquisition Cost) is the CMS weekly pharmacy-acquisition-cost survey — what pharmacies pay. ASP (Average Sales Price) is the CMS Medicare Part B drug-payment file, published quarterly. Medicaid pays is computed by us from CMS State Drug Utilization Data (total reimbursed ÷ units, trailing 12 months) — gross of rebates and inclusive of dispensing fees, so it reflects what Medicaid paid, not an acquisition cost. Medicare drug plans pay is the median negotiated point-of-sale unit cost across plans listing this NDC in the CMS quarterly Prescription Drug Plan pricing files, before rebates. The VA pays is the federal contract price (FSS, and the statutory Big 4 ceiling where listed) from the VA National Acquisition Center pharmaceutical price file. All are free public government data; each measures a different payer, so the figures are not directly comparable.

Packaging — all sizes for this product

Package NDCDescription Marketing startMarketing endStatus
59676-0564-01 You're viewing this Main listing 240 TABLET, FILM COATED in 1 BOTTLE, PLASTIC 2009-04-27 — Active

Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Prezista 150 mgthis 59676-0564-01 Janssen 240 tablets — AB FDA listed —
About this product: this is the brand-name version. FDA-approved generic versions are listed, and recent pricing/market data suggests they may be available.
Where does this data come from?
Equivalents are other NDCs of the same ingredient, form and route from the openFDA NDC Directory, ranked least-expensive-first by NADAC. Therapeutic-equivalence (AB) ratings come from the FDA Orange Book; biologics use the FDA Purple Book for biosimilar & interchangeable status.

Availability & generic status

🏛️
2012
First FDA approval
Nov 2012
📍
2026
Currently FDA-listed
14 years listed
🛡️
2027
Latest patent/protection listed
not a guaranteed launch date
✅Generic appears available

FDA-approved generic versions are listed, and recent pricing/market data suggests they may be available — see Therapeutic equivalents.

🛡️ Latest patent/protection date listed: FDA patent/protection data lists protections through Jun 2027. This may affect when a full generic version becomes widely available, but it is not a guaranteed launch date.
📅 FDA approved Nov 9, 2012 AB TE-rated RLD RS ⏳ ~0.7 yr to latest listed protection

Why the date isn’t exact: Generic timing can change because patents may be challenged, settled, licensed, added, removed, or worked around with a narrower label — and FDA approval does not always mean a pharmacy can get the generic today.

Patents & exclusivity — FDA Orange Book
US 7700645 — drug substance
US 7700645 — drug substance
US 7700645 — drug substance
US 7700645 — drug substance
US 7700645 — drug substance
US 7700645 — drug substance
US 7700645*PED — drug product
US 7700645*PED — drug product
US 7700645*PED — drug product
US 7700645*PED — drug product
US 7700645*PED — drug product
US 7700645*PED — drug product
2012 2014 2016 2018 2020 2022 2024 2026
Today
LOE
Substance patent Formulation patent Method-of-use patent Exclusivity Pediatric +6mo
🏛️FDA exclusivity
FDA-granted marketing protection. It’s separate from patents and may be shorter than patent protection.
🧪Product / substance patents
Patents covering the active ingredient, product, formulation, or related drug features.
🎯Method-of-use patents
Patents covering specific approved uses. These can sometimes be carved out with a “skinny label,” but not always.
🛈 What do these terms mean?
Patent
Legal protection listed in the Orange Book that may delay generic approval or launch. Issued by the U.S. Patent & Trademark Office.
Substance patent
Covers the active drug molecule itself — the hardest to design around. A generic generally can’t launch until it expires.
Formulation (product) patent
Covers a specific formulation or dosage form. A generic can sometimes work around it with a different formulation.
Method-of-use patent
A patent covering one specific approved use of the drug — not necessarily the whole molecule. A generic can sometimes launch with a “skinny label” that carves out the protected use and keeps the others.
Skinny label
A generic label that omits a still-patented use when the FDA allows it — letting a generic reach the market for the unprotected uses.
Exclusivity
FDA-granted marketing protection, separate from patents — e.g. 5-yr new chemical entity, 7-yr orphan drug, or a +6-month pediatric extension.
Paragraph IV
A generic applicant’s formal challenge to a listed patent. It can potentially lead to earlier generic entry, but often involves litigation or a settlement.
RLD / RS
Reference Listed Drug — the brand product the FDA uses as the reference for generic applications. Reference Standard — the product the FDA expects generics to compare against in bioequivalence testing.
TE / AB rating
FDA therapeutic-equivalence rating. An AB rating generally means the FDA considers a generic therapeutically equivalent to — and substitutable for — the brand.
LOE (loss of exclusivity)
The latest patent or exclusivity currently listed — the loss-of-exclusivity / latest-listed-protection date shown on this page. Paragraph-IV challenges and settlements can move the real date earlier; FDA approval and a manufacturer’s decision to market can move it later.

Built from the FDA Orange Book. The bars above are scaled to each protection’s expiry; the red LOE marker is the last one to lapse.

Listed patents (12)
PatentTypeUse codeExpires
US 7700645 ↗ Drug substance — Dec 26, 2026
US 7700645 ↗ Drug substance — Dec 26, 2026
US 7700645 ↗ Drug substance — Dec 26, 2026
US 7700645 ↗ Drug substance — Dec 26, 2026
US 7700645 ↗ Drug substance — Dec 26, 2026
US 7700645 ↗ Drug substance — Dec 26, 2026
US 7700645*PED ↗ Drug product — Jun 26, 2027
US 7700645*PED ↗ Drug product — Jun 26, 2027
US 7700645*PED ↗ Drug product — Jun 26, 2027
US 7700645*PED ↗ Drug product — Jun 26, 2027
US 7700645*PED ↗ Drug product — Jun 26, 2027
US 7700645*PED ↗ Drug product — Jun 26, 2027
Common questions
Is there a generic version of PREZISTA 150 MG TABLET?
Yes — an FDA-approved generic equivalent is listed in the FDA Orange Book for PREZISTA 150 MG TABLET. See the alternatives section for substitutable, lower-cost products.
The FDA approved a generic — why can’t I get it at my pharmacy yet?
FDA approval and pharmacy availability are two different things. The FDA can approve a generic years before it actually reaches pharmacies, because the brand company may still hold patents or have a settlement that delays the launch. A manufacturer also has to choose to make and sell it, and have supply ready. So a drug can be “FDA-approved generic exists” and still be brand-only at the counter today.
Why do different websites show different generic release dates?
Generic availability is not based on one single date. Some sources use the first exclusivity expiration, some use the last product patent, and others use the latest method-of-use patent. Patent challenges, settlements, licenses, and label carve-outs can also change the real-world launch date. This page shows the underlying Orange Book dates so you can see why estimates may differ.
What does “FDA listed” mean?
It means the product appears in the FDA’s official NDC directory. That’s a good sign a product exists and is intended for the U.S. market, but on its own it does not confirm a pharmacy can fill it today. Where we have recent retail pricing data (NADAC) for a product, we label it “Availability likely” instead.
What does a patent or protection date mean here?
It’s the latest date currently listed in the FDA Orange Book for a patent or exclusivity on the brand product. It can affect when a full generic version becomes widely available — but it is not a guaranteed generic launch date. Generics sometimes arrive earlier (through a settlement or patent challenge) or later (a manufacturer still has to make and sell one).
What does “current Orange Book estimate” mean?
It means we are using the latest patent and exclusivity dates currently listed in the FDA Orange Book. It is not a guaranteed launch date.
Can a generic come out before the last patent expires?
Sometimes. A generic company may challenge a patent, settle with the brand manufacturer, receive a license, or obtain approval with a narrower label that avoids a patented use. In other cases, the last listed protection may delay full-label generic competition.
Can a generic come out after the listed dates?
Yes. Even after patents or exclusivity expire, a generic still needs FDA approval and a manufacturer must choose to market it. Supply, litigation, business decisions, or regulatory issues can delay actual availability.
What is the difference between patents and exclusivity?
Patents are legal protections usually issued by the U.S. Patent and Trademark Office. FDA exclusivity is marketing protection granted by the FDA. They are separate, and either one can affect generic timing.
Why are there multiple patent dates?
One drug can have several patents covering different things: the active ingredient, a formulation, a manufacturing process, or a specific approved use. That is why a page may show several expiration dates instead of one simple generic date.
Built from FDA Orange Book patent and exclusivity data. Dates are refreshed from public FDA data when available; the marker is max(latest patent expiry, latest exclusivity expiry). Paragraph-IV settlements and first-filer 180-day exclusivity can shift the real date; a method-of-use patent may allow an earlier skinny-label generic for non-protected indications. Generic launch timing is an estimate, not a guarantee.
Where does this data come from?
Patents and exclusivity from the FDA Orange Book (small-molecule drugs), refreshed from public FDA data. Generic launch timing is an estimate, not a guarantee.

What it looks like

Color white / orange / red
ShapeOval
Imprint800;T
Size2 mm
ScoringNot scored
FlavorStrawberry
One label can cover several strengths, so colors may be combined — always confirm a loose pill against the dispensed prescription label or a pharmacist.
Where does this data come from?
Physical description (imprint, shape, color, scoring, coating) from this product’s FDA Structured Product Labeling (SPL), mirrored from DailyMed / openFDA.

Inactive Ingredients / Excipients

Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.

💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.

  • UNII 68401960MK
    Crospovidone is a synthetic polymer made from polyvinylpyrrolidone. It acts as a disintegrant, helping tablets break apart quickly in the stomach so the medicine dissolves and absorbs into the body.
  • UNII 70097M6I30
    Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
  • UNII OP1R32D61U
    Microcrystalline cellulose is a purified form of cellulose, a natural fiber from plant sources. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and give the medicine its shape and size.
  • UNII G2M7P15E5P
    Polyethylene glycol 3350 is a synthetic polymer used as a solvent, humectant, and thickening agent in medicines. It helps dissolve other ingredients, retain moisture in the product, and achieve the desired consistency.
  • UNII 532B59J990
    Polyvinyl alcohol is a synthetic polymer made from plant-derived materials. It's used as a binder to hold ingredients together, a film-former in coatings, and a thickener in liquid formulations.
  • UNII ETJ7Z6XBU4
    Silicon dioxide is a naturally occurring mineral used as a glidant and anti-caking agent. It helps powder ingredients flow smoothly and prevents clumping during manufacturing and storage.
  • UNII 7SEV7J4R1U
    A powder made from a naturally occurring mineral. In medicines, talc works as a glidant and anti-caking agent, helping tablets and capsules flow smoothly during manufacturing and preventing clumping.
  • UNII 15FIX9V2JP
    Titanium dioxide is a bright white mineral powder commonly used as a colorant and opacifying agent. It makes pills and tablets white or lighter in color and helps make coatings non-transparent.

8 inactive ingredients listed in the exact product block matched to this NDC.

Where does this data come from?
Data sourced from official FDA Structured Product Labeling (SPL) via DailyMed — ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.

Inactive ingredient FAQ

Are inactive ingredients the same for every manufacturer?
No. Inactive ingredients can differ by manufacturer, dosage form, strength, and package / product version.
Why might an inactive ingredient be missing?
Some SPLs do not provide a complete structured inactive-ingredient list, and older or unusual labels may only include the information in narrative text.
Can inactive ingredients matter?
Yes. They can matter for allergies, intolerances, dyes, gluten / lactose concerns, preservatives, and formulation differences — but confirm with a pharmacist or the manufacturer when it’s clinically important.

Manufacturer & labeler

LabelerJanssen Products LP
Application holderJANSSEN PRODUCTS LP
FDA applicationNDA021976 (NDA)
Labeler code59676
First marketedApr 2009
Product typeHuman Prescription Drug
Portfolio12 products on file

More NDCs from Janssen Products LP labeler code 59676

The labeler markets the product; the application holder owns the FDA approval. They’re often the same company but can differ (e.g. a repackager or an authorized generic). A mailing address / phone appears here when the manufacturer includes it in the product’s FDA label (not all do).
Where does this data come from?
Labeler, application holder and registered establishment from the FDA openFDA NDC Directory and Drugs@FDA; address/contact from the product’s FDA label.

Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. Very long sections are excerpted here and marked; the full text is on DailyMed (linked in the sources below). Jump with a chip, search within the label, or expand everything.
🎯 Indications and Usage ⏱️ Dosage and Administration 💊 Dosage Forms and Strengths ⛔ Contraindications ⚠️ Warnings and Cautions 🤒 Adverse Reactions 🔄 Drug Interactions 👥 Use in Specific Populations 🤰 Pregnancy 🧒 Pediatric Use 🧓 Geriatric Use 🆘 Overdosage 🧬 Clinical Pharmacology 🧬 Mechanism of Action 📦 How Supplied / Storage and Handling 📦 Storage and Handling 📋 Description 💬 Information for Patients 🧬 Pharmacokinetics 🧬 Pharmacodynamics 🔬 Clinical Studies 🧪 Nonclinical Toxicology 📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 📄 Patient Package Insert 📖 Instructions for Use 📄 Recent Major Changes 📄 Package Label / Principal Display Panel
🎯 Indications and Usage 91 words ▾

1 INDICATIONS AND USAGE PREZISTA, co-administered with ritonavir (PREZISTA/ritonavir), in combination with other antiretroviral agents, is indicated for the treatment of human immunodeficiency virus (HIV-1) infection in adult and pediatric patients 3 years of age and older [see Use in Specific Populations (8.4) and Clinical Studies (14) ] . PREZISTA is a human immunodeficiency virus (HIV-1) protease inhibitor indicated for the treatment of HIV-1 infection in adult and pediatric patients 3 years of age and older. PREZISTA must be co-administered with ritonavir (PREZISTA/ritonavir) and with other antiretroviral agents.

( 1 )

⏱️ Dosage and Administration ~3 min read ▾

2 DOSAGE AND ADMINISTRATION Testing: In treatment-experienced patients, treatment history genotypic and/or phenotypic testing is recommended prior to initiation of therapy with PREZISTA/ritonavir to assess drug susceptibility of the HIV-1 virus ( 2.1 , 12.4 ) Monitor serum liver chemistry tests before and during therapy with PREZISTA/ritonavir. ( 2.1 , 2.2 , 5.2 ) Treatment-naïve adult patients and treatment-experienced adult patients with no darunavir resistance associated substitutions: 800 mg (one 800 mg tablet) taken with ritonavir 100 mg once daily and with food.

( 2.3 ) Treatment-experienced adult patients with at least one darunavir resistance associated substitution: 600 mg (one 600 mg tablet) taken with ritonavir 100 mg twice daily and with food. ( 2.3 ) Pregnant patients: 600 mg (one 600 mg tablet) taken with ritonavir 100 mg twice daily and with food. ( 2.4 ) Pediatric patients (3 to less than 18 years of age and weighing at least 10 kg): dosage of PREZISTA and ritonavir is based on body weight and should not exceed the adult dose.

PREZISTA should be taken with ritonavir and with food. ( 2.5 ) PREZISTA/ritonavir is not recommended for use in patients with severe hepatic impairment. ( 2.6 )

2.1Testing Prior to Initiation of PREZISTA/ritonavir In treatment-experienced patients, treatment history, genotypic and/or phenotypic testing is recommended to assess drug susceptibility of the HIV-1 virus [see Microbiology (12.4) ]. Refer to Dosage and Administration (2.3) , (2.4) and (2.5) for dosing recommendations. Appropriate laboratory testing such as serum liver biochemistries should be conducted prior to initiating therapy with PREZISTA/ritonavir [see Warnings and Precautions (5.2) ] .

2.2Monitoring During Treatment with PREZISTA/ritonavir Patients with underlying chronic hepatitis, cirrhosis, or in patients who have pre-treatment elevations of transaminases should be monitored for elevation in serum liver biochemistries, especially during the first several months of PREZISTA/ritonavir treatment [see Warnings and Precautions (5.2) ] .

2.3Recommended Dosage in Adult Patients PREZISTA must be co-administered with ritonavir to exert its therapeutic effect. Failure to correctly co-administer PREZISTA with ritonavir will result in plasma levels of darunavir that will be insufficient to achieve the desired antiviral effect and will alter some drug interactions. Patients who have difficulty swallowing PREZISTA tablets can use the 100 mg per mL PREZISTA oral suspension.

Treatment-Naïve Adult Patients The recommended oral dose of PREZISTA is 800 mg (one 800 mg tablet or 8 mL of the oral suspension) taken with ritonavir 100 mg (one 100 mg tablet or capsule or 1.25 mL of a 80 mg per mL ritonavir oral solution) once daily and with food. An 8 mL PREZISTA dose should be taken as two 4 mL administrations with the included oral dosing syringe. Treatment-Experienced Adult Patients The recommended oral dosage for treatment-experienced adult patients is summarized in Table 1.

Baseline genotypic testing is recommended for dose selection. However, when genotypic testing is not feasible, PREZISTA 600 mg taken with ritonavir 100 mg twice daily is recommended. Table 1: Recommended PREZISTA/ritonavir Dosage in Treatment-Experienced Adult Patients Formulation and Recommended Dosing Baseline Resistance PREZISTA tablets with ritonavir tablets or capsule PREZISTA oral suspension (100 mg/mL) with ritonavir oral solution (80 mg/mL) With no darunavir resistance associated substitutions V11I, V32I, L33F, I47V, I50V, I54L, I54M, T74P, L76V, I84V and L89V One 800 mg PREZISTA tablet with one 100 mg ritonavir tablet/capsule, taken once daily with food 8 mL An 8 mL darunavir dose should be taken as two 4 mL administrations with the included oral dosing syringe.

PREZISTA oral suspension with 1.25 mL ritonavir oral solution, taken once daily with food With at least one darunavir resistance associated substitutions , or with no baseline resistance information… [Excerpted — this section continues on DailyMed.]

💊 Dosage Forms and Strengths 131 words ▾

3 DOSAGE FORMS AND STRENGTHS Oral suspension: 100 mg per mL ( 3 ) Tablets: 75 mg, 150 mg, 600 mg, and 800 mg ( 3 ) PREZISTA Oral Suspension PREZISTA 100 mg per mL is supplied as a white to off-white opaque suspension for oral use, containing 100 mg of darunavir per mL of suspension. PREZISTA Tablets 75 mg: white, caplet-shaped, film-coated tablets debossed with "75" on one side and "TMC" on the other side. 150 mg: white, oval-shaped, film-coated tablets debossed with "150" on one side and "TMC" on the other side.

600 mg: orange, oval-shaped, film-coated tablets debossed with "600MG" on one side and "TMC" on the other side. 800 mg: dark red, oval-shaped, film-coated tablets debossed with "800" on one side and "T" on the other side.

⛔ Contraindications 183 words ▾

4 CONTRAINDICATIONS Co-administration of PREZISTA/ritonavir is contraindicated with drugs that are highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events (narrow therapeutic index). Examples of these drugs and other contraindicated drugs (which may lead to reduced efficacy of darunavir) are listed below [see Drug Interactions (7.3) ] . Due to the need for co-administration of PREZISTA with ritonavir, please refer to ritonavir prescribing information for a description of ritonavir contraindications.

Alpha 1-adrenoreceptor antagonist: alfuzosin Anti-gout: colchicine, in patients with renal and/or hepatic impairment Antimycobacterial: rifampin Antipsychotics: lurasidone, pimozide Cardiac Disorders: dronedarone, ivabradine, ranolazine Ergot derivatives, e.g. dihydroergotamine, ergotamine, methylergonovine Herbal product: St. John's wort ( Hypericum perforatum ) Hepatitis C direct acting antiviral: elbasvir/grazoprevir Lipid modifying agents: lomitapide, lovastatin, simvastatin Opioid Antagonist: naloxegol PDE-5 inhibitor: sildenafil when used for treatment of pulmonary arterial hypertension Sedatives/hypnotics: orally administered midazolam, triazolam Co-administration of PREZISTA/ritonavir is contraindicated with drugs that are highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events (narrow therapeutic index).

( 4 )

⚠️ Warnings and Cautions ~2 min read ▾

5 WARNINGS AND PRECAUTIONS Drug-induced hepatitis (e.g., acute hepatitis, cytolytic hepatitis) has been reported with PREZISTA/ritonavir. Monitor liver function before and during therapy, especially in patients with underlying chronic hepatitis, cirrhosis, or in patients who have pre-treatment elevations of transaminases. Post-marketing cases of liver injury, including some fatalities, have been reported.

( 5.2 ) Skin reactions ranging from mild to severe, including Stevens-Johnson Syndrome, toxic epidermal necrolysis, drug rash with eosinophilia and systemic symptoms and acute generalized exanthematous pustulosis, have been reported. Discontinue treatment if severe reaction develops. ( 5.3 ) Use with caution in patients with a known sulfonamide allergy.

( 5.4 ) Patients may develop new onset diabetes mellitus or hyperglycemia. Initiation or dose adjustments of insulin or oral hypoglycemic agents may be required. ( 5.6 ) Patients may develop redistribution/accumulation of body fat or immune reconstitution syndrome.

( 5.7 , 5.8 ) Patients with hemophilia may develop increased bleeding events. ( 5.9 ) PREZISTA/ritonavir is not recommended in pediatric patients below 3 years of age in view of toxicity and mortality observed in juvenile rats dosed with darunavir up to days 23 to 26 of age. ( 5.10 )

5.1Importance of Co-administration with Ritonavir PREZISTA must be co-administered with ritonavir and food to achieve the desired antiviral effect. Failure to administer PREZISTA with ritonavir and food may result in a loss of efficacy of darunavir. Please refer to ritonavir prescribing information for additional information on precautionary measures.

5.2Hepatotoxicity Drug-induced hepatitis (e.g., acute hepatitis, cytolytic hepatitis) has been reported with PREZISTA/ritonavir. During the clinical development program (N=3063), hepatitis was reported in 0.5% of patients receiving combination therapy with PREZISTA/ritonavir. Patients with pre-existing liver dysfunction, including chronic active hepatitis B or C, have an increased risk for liver function abnormalities including severe hepatic adverse events.

Post-marketing cases of liver injury, including some fatalities, have been reported. These have generally occurred in patients with advanced HIV-1 disease taking multiple concomitant medications, having co-morbidities including hepatitis B or C co-infection, and/or developing immune reconstitution syndrome. A causal relationship with PREZISTA/ritonavir therapy has not been established.

Appropriate laboratory testing should be conducted prior to initiating therapy with PREZISTA/ritonavir and patients should be monitored during treatment. Increased AST/ALT monitoring should be considered in patients with underlying chronic hepatitis, cirrhosis, or in patients who have pre-treatment elevations of transaminases, especially during the first several months of PREZISTA/ritonavir treatment. Evidence of new or worsening liver dysfunction (including clinically significant elevation of liver enzymes and/or symptoms such as fatigue, anorexia, nausea, jaundice, dark urine, liver tenderness, hepatomegaly) in patients on PREZISTA/ritonavir should prompt consideration of interruption or discontinuation of treatment.

5.3Severe Skin Reactions During the clinical development program (n=3063), severe skin reactions, accompanied by fever and/or elevations of transaminases in some cases, have been reported in 0.4% of subjects. Stevens-Johnson Syndrome was rarely (less than 0.1%) reported during the clinical development program. During post-marketing experience toxic epidermal necrolysis, drug rash with eosinophilia and systemic symptoms, and acute generalized exanthematous pustulosis have been reported.

Discontinue PREZISTA/ritonavir immediately if signs or symptoms of severe skin reactions develop. These can include but are not limited to severe rash or rash accompanied with fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions,… [Excerpted — this section continues on DailyMed.]

🤒 Adverse Reactions ~3 min read ▾

6 ADVERSE REACTIONS The following adverse reactions are discussed in other sections of labeling: Hepatotoxicity [see Warnings and Precautions (5.2) ] Severe Skin Reactions [see Warnings and Precautions (5.3) ] Diabetes Mellitus/Hyperglycemia [see Warnings and Precautions (5.6) ] Fat Redistribution [see Warnings and Precautions (5.7) ] Immune Reconstitution Syndrome [see Warnings and Precautions (5.8) ] Hemophilia [see Warnings and Precautions (5.9) ] Due to the need for co-administration of PREZISTA with ritonavir, please refer to ritonavir prescribing information for ritonavir-associated adverse reactions.

The most common clinical adverse drug reactions to PREZISTA/ritonavir (incidence greater than or equal to 5%) of at least moderate intensity (greater than or equal to Grade 2) were diarrhea, nausea, rash, headache, abdominal pain and vomiting. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Janssen Products, LP at 1-800-JANSSEN (1-800-526-7736) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. Treatment Naïve-Adults: TMC114-C211 The safety assessment is based on all safety data from the Phase 3 trial TMC114-C211 comparing PREZISTA/ritonavir 800/100 mg once daily versus lopinavir/ritonavir 800/200 mg per day in 689 antiretroviral treatment-naïve HIV-1-infected adult subjects.

The total mean exposure for subjects in the PREZISTA/ritonavir 800/100 mg once daily arm and in the lopinavir/ritonavir 800/200 mg per day arm was 162.5 and 153.5 weeks, respectively. The majority of the adverse drug reactions (ADRs) reported during treatment with PREZISTA/ritonavir 800/100 mg once daily were mild in severity. The most common clinical ADRs to PREZISTA/ritonavir 800/100 mg once daily (greater than or equal to 5%) of at least moderate intensity (greater than or equal to Grade 2) were diarrhea, headache, abdominal pain and rash.

2.3% of subjects in the PREZISTA/ritonavir arm discontinued treatment due to ADRs. ADRs to PREZISTA/ritonavir 800/100 mg once daily of at least moderate intensity (greater than or equal to Grade 2) in antiretroviral treatment-naïve HIV-1-infected adult subjects are presented in Table 6 and subsequent text below the table. Table 6: Selected Clinical Adverse Drug Reactions to PREZISTA/ritonavir 800/100 mg Once Daily Excluding laboratory abnormalities reported as ADRs. of at Least Moderate Intensity (≥Grade 2) Occurring in ≥2% of Antiretroviral Treatment-Naïve HIV-1-Infected Adult Subjects (Trial TMC114-C211) System organ class, preferred term, % PREZISTA/ritonavir 800/100 mg once daily + TDF/FTC N=343 lopinavir/ritonavir 800/200 mg per day + TDF/FTC N=346 N=total number of subjects per treatment group; FTC=emtricitabine; TDF=tenofovir disoproxil fumarate Gastrointestinal Disorders Abdominal pain 6% 6% Diarrhea 9% 16% Nausea 4% 4% Vomiting 2% 4% General Disorders and Administration Site Conditions Fatigue <1% 3% Metabolism and Nutrition Disorders Anorexia 2% <1% Nervous System Disorders Headache 7% 6% Skin and Subcutaneous Tissue Disorders Rash 6% 7% Less Common Adverse Reactions Treatment-emergent ADRs of at least moderate intensity (greater than or equal to Grade 2) occurring in less than 2% of antiretroviral treatment-naïve subjects receiving PREZISTA/ritonavir 800/100 mg once daily are listed below by body system: Gastrointestinal Disorders : acute pancreatitis, dyspepsia, flatulence General Disorders and Administration Site Conditions : asthenia Hepatobiliary Disorders : acute hepatitis (e.g., acute hepatitis, cytolytic hepatitis, hepatotoxicity) Immune System Disorders : (drug) hypersensitivity, immune reconstitution syndrome Metabolism and Nutrition Disorders : diabetes mellitus Musculoskeletal and Connectiv… [Excerpted — this section continues on DailyMed.]

🔄 Drug Interactions ~3 min read ▾

7 DRUG INTERACTIONS Co-administration of PREZISTA/ritonavir with other drugs can alter the concentrations of other drugs and other drugs may alter the concentrations of darunavir. The potential drug-drug interactions must be considered prior to and during therapy. ( 4 , 5.5 , 7 , 12.3 )

7.1Potential for PREZISTA/ritonavir to Affect Other Drugs PREZISTA co-administered with ritonavir is an inhibitor of CYP3A, CYP2D6, and P-gp. Co-administration of PREZISTA and ritonavir with drugs that are primarily metabolized by CYP3A and CYP2D6 or are transported by P-gp may result in increased plasma concentrations of such drugs, which could increase or prolong their therapeutic effect and adverse events. PREZISTA co-administered with ritonavir with drugs that have active metabolite(s) formed by CYP3A may result in reduced plasma concentrations of these active metabolite(s), potentially leading to loss of their therapeutic effect (see Table 10 ).

7.2Potential for Other Drugs to Affect Darunavir Darunavir and ritonavir are metabolized by CYP3A. In vitro data indicate that darunavir may be a P-gp substrate. Drugs that induce CYP3A activity would be expected to increase the clearance of darunavir and ritonavir, resulting in lowered plasma concentrations of darunavir and ritonavir.

Co-administration of darunavir and ritonavir and other drugs that inhibit CYP3A, or P-gp may decrease the clearance of darunavir and ritonavir and may result in increased plasma concentrations of darunavir and ritonavir (see Table 10 ).

7.3Established and Other Potentially Significant Drug Interactions Table 10 provides dosing recommendations as a result of drug interactions with PREZISTA/ritonavir. These recommendations are based on either drug interaction studies or predicted interactions due to the expected magnitude of interaction and potential for serious adverse events or loss of efficacy. The table includes examples of potentially significant interactions but is not all inclusive [see Contraindications (4) and Clinical Pharmacology (12.3) ] , and therefore the label of each drug that is co-administered with PREZISTA/ritonavir should be consulted for information related to the route of metabolism, interaction pathways, potential risks, and specific actions to be taken with regard to co-administration.

Table 10: Established and Other Potentially Significant Drug Interactions: Alterations in Dose or Regimen May be Recommended Based on Drug Interaction Studies or Predicted Interaction (see Contraindications (4) for a list of examples of contraindicated drugs) [see Clinical Pharmacology (12.3) for Magnitude of Interaction, Tables 15 and 16 ] Concomitant Drug Class Drug Name Examples Effect on Concentration of Darunavir Or Concomitant Drug Clinical Comment HIV-1-Antiviral Agents: Nucleoside Reverse Transcriptase Inhibitors (NRTIs) didanosine ↔ darunavir ↔ didanosine Didanosine should be administered one hour before or two hours after PREZISTA/ritonavir (which are administered with food).

HIV-1-Antiviral Agents: HIV-Protease Inhibitors (PIs) indinavir ↑ darunavir ↑ indinavir The appropriate dose of indinavir in combination with PREZISTA/ritonavir has not been established. (The reference regimen for indinavir was indinavir/ritonavir 800/100 mg twice daily.) lopinavir/ritonavir ↓ darunavir ↔ lopinavir Appropriate doses of the combination have not been established. Hence, it is not recommended to co-administer lopinavir/ritonavir and PREZISTA, with or without ritonavir. saquinavir ↓ darunavir ↔ saquinavir Appropriate doses of the combination have not been established.

Hence, it is not recommended to co-administer saquinavir and PREZISTA, with or without ritonavir. Other HIV protease inhibitors, except atazanavir [see Drug Interactions (7.4) ] As co-administration with PREZISTA/ritonavir has not been studied, co-administration is not recommended. HIV-1-Antiviral Agents: CCR5 co-receptor antagonists maraviroc ↑ maraviroc When used in combination with PREZISTA/ritonavir… [Excerpted — this section continues on DailyMed.]

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS Pregnancy: Total darunavir exposures were generally lower during pregnancy compared to postpartum period. The reduction in darunavir exposures during pregnancy were greater for once daily dosing compared to the twice daily dosing regimen. ( 8.1 , 12.3 ) Lactation: Women infected with HIV should be instructed not to breastfeed due to the potential for HIV transmission.

( 8.2 ) Pediatrics: Not recommended for patients less than 3 years of age. ( 8.4 )

8.1Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to PREZISTA during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) 1-800-258-4263. Risk Summary Prospective pregnancy data from the APR are not sufficient to adequately assess the risk of birth defects or miscarriage.

Available limited data from the APR show no statistically significant difference in the overall risk of major birth defects for darunavir compared with the background rate for major birth defects of 2.7% in a U.S. reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP ) [see Data ] . The rate of miscarriage is not reported in the APR. The estimated background rate of miscarriage in clinically recognized pregnancies in the U.S. general population is 15-20%.

The background risk of major birth defects and miscarriage for the indicated population is unknown. Studies in animals did not show evidence of developmental toxicity. Exposures (based on AUC) in rats were 3-fold higher, whereas in mice and rabbits, exposures were lower (less than 1-fold) than human exposures at the recommended daily dose [see Data ] .

Clinical Considerations The recommended dosage in pregnant patients is PREZISTA 600 mg taken with ritonavir 100 mg twice daily with food. PREZISTA 800 mg taken with ritonavir 100 mg once daily should only be considered in certain pregnant patients who are already on a stable PREZISTA 800 mg with ritonavir 100 mg once daily regimen prior to pregnancy, are virologically suppressed (HIV-1 RNA less than 50 copies per mL), and in whom a change to twice daily PREZISTA 600 mg with ritonavir 100 mg may compromise tolerability or compliance [see Dosage and Administration (2.4) and Clinical Pharmacology (12.3) ] .

Data Human Data PREZISTA/ritonavir (600/100 mg twice daily or 800/100 mg once daily) in combination with a background regimen was evaluated in a clinical trial of 36 pregnant women during the second and third trimesters, and postpartum. Eighteen subjects were enrolled in each BID and QD treatment arms. Twenty-nine subjects completed the trial through the postpartum period (6–12 weeks after delivery) and 7 subjects discontinued before trial completion, 5 subjects in the BID arm and 2 subjects in the QD arm.

The pharmacokinetic data demonstrate that exposure to darunavir and ritonavir as part of an antiretroviral regimen was lower during pregnancy compared with postpartum (6–12 weeks). Exposure reductions during pregnancy were greater for the once daily regimen as compared to the twice daily regimen [see Clinical Pharmacology (12.3) ]. Virologic response was preserved.

In the BID arm, the proportion of subjects with HIV-1 RNA <50 copies/mL were 39% (7/18) at baseline, 61% (11/18) through the third trimester visit, and 61% (11/18) through the 6–12 week postpartum visit. Virologic outcomes during the third trimester visit showed HIV-1 RNA ≥50 copies/mL for 11% (2/18) of subjects and were missing for 5 subjects (1 subject discontinued prematurely due to virologic failure). In the QD arm, the proportion of subjects with HIV-1 RNA <50 copies/mL were 61% (11/18) at baseline, 83% (15/18) through the third trimester visit, and 78% (14/18) through the 6–12 week postpartum visit.

Virologic outcomes during the third trimester visit showed HIV-1 RNA ≥50 copies/mL for none of the subjects and were missing for 3 subjects (1… [Excerpted — this section continues on DailyMed.]

🤰 Pregnancy ~3 min read ▾

8.1Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to PREZISTA during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) 1-800-258-4263. Risk Summary Prospective pregnancy data from the APR are not sufficient to adequately assess the risk of birth defects or miscarriage.

Available limited data from the APR show no statistically significant difference in the overall risk of major birth defects for darunavir compared with the background rate for major birth defects of 2.7% in a U.S. reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP ) [see Data ] . The rate of miscarriage is not reported in the APR. The estimated background rate of miscarriage in clinically recognized pregnancies in the U.S. general population is 15-20%.

The background risk of major birth defects and miscarriage for the indicated population is unknown. Studies in animals did not show evidence of developmental toxicity. Exposures (based on AUC) in rats were 3-fold higher, whereas in mice and rabbits, exposures were lower (less than 1-fold) than human exposures at the recommended daily dose [see Data ] .

Clinical Considerations The recommended dosage in pregnant patients is PREZISTA 600 mg taken with ritonavir 100 mg twice daily with food. PREZISTA 800 mg taken with ritonavir 100 mg once daily should only be considered in certain pregnant patients who are already on a stable PREZISTA 800 mg with ritonavir 100 mg once daily regimen prior to pregnancy, are virologically suppressed (HIV-1 RNA less than 50 copies per mL), and in whom a change to twice daily PREZISTA 600 mg with ritonavir 100 mg may compromise tolerability or compliance [see Dosage and Administration (2.4) and Clinical Pharmacology (12.3) ] .

Data Human Data PREZISTA/ritonavir (600/100 mg twice daily or 800/100 mg once daily) in combination with a background regimen was evaluated in a clinical trial of 36 pregnant women during the second and third trimesters, and postpartum. Eighteen subjects were enrolled in each BID and QD treatment arms. Twenty-nine subjects completed the trial through the postpartum period (6–12 weeks after delivery) and 7 subjects discontinued before trial completion, 5 subjects in the BID arm and 2 subjects in the QD arm.

The pharmacokinetic data demonstrate that exposure to darunavir and ritonavir as part of an antiretroviral regimen was lower during pregnancy compared with postpartum (6–12 weeks). Exposure reductions during pregnancy were greater for the once daily regimen as compared to the twice daily regimen [see Clinical Pharmacology (12.3) ]. Virologic response was preserved.

In the BID arm, the proportion of subjects with HIV-1 RNA <50 copies/mL were 39% (7/18) at baseline, 61% (11/18) through the third trimester visit, and 61% (11/18) through the 6–12 week postpartum visit. Virologic outcomes during the third trimester visit showed HIV-1 RNA ≥50 copies/mL for 11% (2/18) of subjects and were missing for 5 subjects (1 subject discontinued prematurely due to virologic failure). In the QD arm, the proportion of subjects with HIV-1 RNA <50 copies/mL were 61% (11/18) at baseline, 83% (15/18) through the third trimester visit, and 78% (14/18) through the 6–12 week postpartum visit.

Virologic outcomes during the third trimester visit showed HIV-1 RNA ≥50 copies/mL for none of the subjects and were missing for 3 subjects (1 subject discontinued prematurely due to virologic failure). PREZISTA/ritonavir was well tolerated during pregnancy and postpartum. There were no new clinically relevant safety findings compared with the known safety profile of PREZISTA/ritonavir in HIV-1-infected adults.

Among the 31 infants with HIV test results available data, born to the 31 HIV-infected pregnant women who completed trial through delivery or postpartum period, all 31 infants had test results that were negative… [Excerpted — this section continues on DailyMed.]

🧒 Pediatric Use ~2 min read ▾

8.4Pediatric Use PREZISTA/ritonavir is not recommended in pediatric patients below 3 years of age because of toxicity and mortality observed in juvenile rats dosed with darunavir (from 20 mg/kg to 1000 mg/kg) up to days 23 to 26 of age [see Warnings and Precautions (5.10) , Use in Specific Populations (8.1) and Clinical Pharmacology (12.3) ] . The safety, pharmacokinetic profile, and virologic and immunologic responses of PREZISTA/ritonavir administered twice daily were evaluated in treatment-experienced HIV-1-infected pediatric subjects 3 to less than 18 years of age and weighting at least 10 kg.

These subjects were evaluated in clinical trials TMC114-C212 (80 subjects, 6 to less than 18 years of age) and TMC114-228 (21 subjects, 3 to less than 6 years of age) [see Adverse Reactions (6.1) , Clinical Pharmacology (12.3) and Clinical Studies (14.4) ] . Frequency, type, and severity of adverse drug reactions in pediatric subjects were comparable to those observed in adults [see Adverse Reactions (6.1) ] . Refer to Dosage and Administration (2.5) for twice-daily dosing recommendations for pediatric subjects 3 to less than 18 years of age and weighing at least 10 kg.

In clinical trial TMC114-C230, the safety, pharmacokinetic profile and virologic and immunologic responses of PREZISTA/ritonavir administered once daily were evaluated in treatment-naïve HIV-1 infected pediatric subjects 12 to less than 18 years of age (12 subjects) [see Adverse Reactions (6.1) , Clinical Pharmacology (12.3) and Clinical Studies (14.4) ] . Frequency, type, and severity of adverse drug reactions in pediatric subjects were comparable to those observed in adults [see Adverse Reactions (6.1) ] . Once daily dosing recommendations for pediatric patients 3 to less than 12 years of age were derived using population pharmacokinetic modeling and simulation.

Although a PREZISTA/ritonavir once daily dosing pediatric trial was not conducted in children less than 12 years of age, there is sufficient clinical safety data to support the predicted PREZISTA exposures for the dosing recommendations in this age group [see Clinical Pharmacology (12.3) ] . Please see Dosage and Administration (2.5) for once-daily dosing recommendations for pediatric subjects 3 to less than 18 years of age and weighing at least 10 kg. Juvenile Animal Data In a juvenile toxicity study where rats were directly dosed with darunavir (up to 1000 mg/kg), deaths occurred from post-natal day 5 at plasma exposure levels ranging from 0.1 to 1.0 of the human exposure levels.

In a 4-week rat toxicology study, when dosing was initiated on post-natal day 23 (the human equivalent of 2 to 3 years of age), no deaths were observed with a plasma exposure (in combination with ritonavir) 2 times the human plasma exposure levels.

🧓 Geriatric Use 66 words ▾

8.5Geriatric Use Clinical studies of PREZISTA did not include sufficient numbers of patients aged 65 years and over to determine whether they respond differently from younger patients. In general, caution should be exercised in the administration and monitoring of PREZISTA in elderly patients, reflecting the greater frequency of decreased hepatic function, and of concomitant disease or other drug therapy [see Clinical Pharmacology (12.3) ] .

🆘 Overdosage 63 words ▾

10 OVERDOSAGE Human experience of acute overdose with PREZISTA/ritonavir is limited. No specific antidote is available for overdose with PREZISTA. Treatment of overdose with PREZISTA consists of general supportive measures including monitoring of vital signs and observation of the clinical status of the patient. Since PREZISTA is highly protein bound, dialysis is unlikely to be beneficial in significant removal of the active substance.

🧬 Clinical Pharmacology ~3 min read ▾

12 CLINICAL PHARMACOLOGY

12.1Mechanism of Action Darunavir is an HIV-1 antiviral drug [see Microbiology (12.4) ] .

12.2Pharmacodynamics Cardiac Electrophysiology In a thorough QT/QTc study in 40 healthy subjects, PREZISTA/ritonavir doses of 1.33 times the maximum recommended dose did not affect the QT/QTc interval.

12.3Pharmacokinetics Pharmacokinetics in Adults General Darunavir is primarily metabolized by CYP3A. Ritonavir inhibits CYP3A, thereby increasing the plasma concentrations of darunavir. When a single dose of PREZISTA 600 mg was given orally in combination with 100 mg ritonavir twice daily, there was an approximate 14-fold increase in the systemic exposure of darunavir.

Therefore, PREZISTA should only be used in combination with 100 mg of ritonavir to achieve sufficient exposures of darunavir. The pharmacokinetics of darunavir, co-administered with low dose ritonavir (100 mg), has been evaluated in healthy adult volunteers and in HIV-1-infected subjects. Table 11 displays the population pharmacokinetic estimates of darunavir after oral administration of PREZISTA/ritonavir 600/100 mg twice daily (based on sparse sampling in 285 patients in trial TMC114-C214, 278 patients in trial TMC114-C229 and 119 patients [integrated data] from trials TMC114-C202 and TMC114-C213) and PREZISTA/ritonavir 800/100 mg once daily (based on sparse sampling in 335 patients in trial TMC114-C211 and 280 patients in trial TMC114-C229) to HIV-1-infected patients.

Table 11: Population Pharmacokinetic Estimates of Darunavir at PREZISTA/ritonavir 800/100 mg Once Daily (Trial TMC114-C211, 48-Week Analysis and Trial TMC114-C229, 48-Week Analysis) and PREZISTA/ritonavir 600/100 mg Twice Daily (Trial TMC114-C214, 48-Week Analysis, Trial TMC114-C229, 48-Week Analysis and Integrated Data from Trials TMC114-C213 and TMC114-C202, Primary 24-Week Analysis) PREZISTA/ritonavir 800/100 mg once daily PREZISTA/ritonavir 600/100 mg twice daily Parameter TMC114-C211 N=335 TMC114-C229 N=280 TMC114-C214 N=285 TMC114-C229 N=278 TMC114-C213 + TMC114-C202 (integrated data) N=119 N=number of subjects with data AUC 24h (ng.h/mL) AUC 24h is calculated as AUC 12h*2.

Mean ± Standard Deviation 93026 ± 27050 93334 ± 28626 116796 ± 33594 114302 ± 32681 124698 ± 32286 Median (Range) 87854 (45000–219240) 87788 (45456–236920) 111632 (64874–355360) 109401 (48934–323820) 123336 (67714–212980) C 0h (ng/mL) Mean ± Standard Deviation 2282 ± 1168 2160 ± 1201 3490 ± 1401 3386 ± 1372 3578 ± 1151 Median (Range) 2041 (368–7242) 1896 (184–7881) 3307 (1517–13198) 3197 (250–11865) 3539 (1255–7368) Absorption and Bioavailability Darunavir, co-administered with 100 mg ritonavir twice daily, was absorbed following oral administration with a T max of approximately 2.5–4 hours.

The absolute oral bioavailability of a single 600 mg dose of darunavir alone and after co-administration with 100 mg ritonavir twice daily was 37% and 82%, respectively. In vivo data suggest that PREZISTA/ritonavir is an inhibitor of the P-glycoprotein (P-gp) transporters. Effects of Food on Oral Absorption When PREZISTA tablets were administered with food, the C max and AUC of darunavir, co-administered with ritonavir, is approximately 40% higher relative to the fasting state.

Within the range of meals studied, darunavir exposure is similar. The total caloric content of the various meals evaluated ranged from 240 Kcal (12 gms fat) to 928 Kcal (56 gms fat). Distribution Darunavir is approximately 95% bound to plasma proteins.

Darunavir binds primarily to plasma alpha 1-acid glycoprotein (AAG). Metabolism In vitro experiments with human liver microsomes (HLMs) indicate that darunavir primarily undergoes oxidative metabolism. Darunavir is extensively metabolized by CYP enzymes, primarily by CYP3A.

A mass balance study in healthy volunteers showed that after a single dose administration of 400 mg 14 C-darunavir, co-administered with 100 mg ritonavir, the majority of the radioactivity in the plasma was due to darunavir. At… [Excerpted — this section continues on DailyMed.]

🧬 Mechanism of Action 47 words ▾

12.1Mechanism of Action Darunavir is an HIV-1 antiviral drug [see Microbiology (12.4) ] .

Mechanism of Action Darunavir is an inhibitor of the HIV-1 protease. It selectively inhibits the cleavage of HIV-1 encoded Gag-Pol polyproteins in infected cells, thereby preventing the formation of mature virus particles.

📦 How Supplied / Storage and Handling ~1 min read ▾

16 HOW SUPPLIED/STORAGE AND HANDLING PREZISTA ® (darunavir) 100 mg per mL oral suspension is a white to off-white opaque liquid supplied in amber-colored multiple-dose bottles containing 100 mg of darunavir per mL packaged with a 6 mL oral dosing syringe with 0.2 mL gradations. PREZISTA ® (darunavir) 75 mg tablets are supplied as white, caplet-shaped, film-coated tablets debossed with "75" on one side and "TMC" on the other side. PREZISTA ® (darunavir) 150 mg tablets are supplied as white, oval-shaped, film-coated tablets debossed with "150" on one side and "TMC" on the other side.

PREZISTA ® (darunavir) 600 mg tablets are supplied as orange, oval-shaped, film-coated tablets debossed with "600MG" on one side and "TMC" on the other side. PREZISTA ® (darunavir) 800 mg tablets are supplied as dark red, oval-shaped, film-coated tablets debossed with "800" on one side and "T" on the other side. PREZISTA is packaged in bottles in the following configuration: 100 mg/mL oral suspension – 200 mL bottles (NDC 59676-565-01) 75 mg tablets — bottles of 480 (NDC 59676-563-01) 150 mg tablets — bottles of 240 (NDC 59676-564-01) 600 mg tablets — bottles of 60 (NDC 59676-562-01) 800 mg tablets — bottles of 30 (NDC 59676-566-30) Storage PREZISTA Oral Suspension Store at 25°C (77°F); with excursions permitted to 15°–30°C (59°–86°F).

Do not refrigerate or freeze. Avoid exposure to excessive heat. Store in the original container.

Shake well before each usage. PREZISTA Tablets Store at 25°C (77°F); with excursions permitted to 15°–30°C (59°–86°F). Keep PREZISTA out of reach of children.

📦 Storage and Handling 53 words ▾

Storage PREZISTA Oral Suspension Store at 25°C (77°F); with excursions permitted to 15°–30°C (59°–86°F). Do not refrigerate or freeze. Avoid exposure to excessive heat. Store in the original container. Shake well before each usage. PREZISTA Tablets Store at 25°C (77°F); with excursions permitted to 15°–30°C (59°–86°F). Keep PREZISTA out of reach of children.

📋 Description ~2 min read ▾

11 DESCRIPTION PREZISTA (darunavir) is an inhibitor of the human immunodeficiency virus (HIV-1) protease. PREZISTA tablets and oral suspension contain the active ingredient darunavir, (present as darunavir ethanolate) which has the following chemical name: [(1S,2R)-3-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]-carbamic acid (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester monoethanolate. Its molecular formula is C 27 H 37 N 3 O 7 S ∙ C 2 H 5 OH and its molecular weight is 593.73.

Darunavir ethanolate has the following structural formula: Darunavir ethanolate is a white to off-white powder with a solubility of approximately 0.15 mg per mL in water at 20°C. PREZISTA ® 100 mg per mL oral suspension is available as a white to off-white opaque suspension for oral administration. Each mL of the oral suspension contains darunavir 100 mg (present as darunavir ethanolate).

In addition, each mL contains the inactive ingredients citric acid monohydrate, hydrochloric acid (for pH adjustment), hydroxypropyl cellulose, masking flavor, methylparaben sodium, microcrystalline cellulose, purified water, sodium carboxymethylcellulose, strawberry cream flavor and sucralose. PREZISTA ® 75 mg tablets are available as white, caplet-shaped, film-coated tablets for oral administration. Each 75 mg tablet contains darunavir 75 mg (present as darunavir ethanolate).

PREZISTA ® 150 mg tablets are available as white, oval-shaped, film-coated tablets for oral administration. Each 150 mg tablet contains darunavir 150 mg (present as darunavir ethanolate). PREZISTA ® 600 mg tablets are available as orange, oval-shaped, film-coated tablets for oral administration.

Each 600 mg tablet contains darunavir 600 mg (present as darunavir ethanolate). PREZISTA ® 800 mg tablets are available as dark red, oval-shaped, film-coated tablets for oral administration. Each 800 mg tablet contains darunavir 800 mg (present as darunavir ethanolate).

During storage, partial conversion from ethanolate to hydrate may occur; however, this does not affect product quality or performance. Each tablet also contains the inactive ingredients colloidal silicon dioxide, crospovidone, magnesium stearate, and microcrystalline cellulose. The 800 mg tablet also contains hypromellose.

The 75 and 150 mg tablet film coating, OPADRY ® White, contains polyethylene glycol 3350, polyvinyl alcohol-partially hydrolyzed, talc, and titanium dioxide. The 600 mg tablet film coating, OPADRY ® Orange, contains FD&C Yellow No. 6, polyethylene glycol 3350, polyvinyl alcohol-partially hydrolyzed, talc, and titanium dioxide.

The 800 mg tablet film coating, OPADRY ® Dark Red, contains iron oxide red, polyethylene glycol 3350, polyvinyl alcohol-partially hydrolyzed, talc, and titanium dioxide. All strengths for PREZISTA are expressed in terms of the free form of darunavir. Chemical Structure

💬 Information for Patients ~2 min read ▾

17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information and Instruction for Use). Instructions for Use Advise patients to take PREZISTA and ritonavir with food every day on a regular dosing schedule, as missed doses can result in development of resistance. PREZISTA must always be used with ritonavir in combination with other antiretroviral drugs.

Advise patients not to alter the dose of either PREZISTA or ritonavir, discontinue ritonavir, or discontinue therapy with PREZISTA without consulting their physician [see Dosage and Administration (2) ] . Hepatotoxicity Inform patients that drug-induced hepatitis (e.g., acute hepatitis, cytolytic hepatitis) has been reported with PREZISTA co-administered with 100 mg of ritonavir. Advise patients about the signs and symptoms of liver problems [see Warnings and Precautions (5.2) ] .

Severe Skin Reactions Inform patients that skin reactions ranging from mild to severe, including Stevens-Johnson Syndrome, drug rash with eosinophilia and systemic symptoms, and toxic epidermal necrolysis, have been reported with PREZISTA co-administered with 100 mg of ritonavir. Advise patients to discontinue PREZISTA/ritonavir immediately if signs or symptoms of severe skin reactions develop. These can include but are not limited to severe rash or rash accompanied with fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, hepatitis and/or eosinophilia [see Warnings and Precautions (5.3) ] .

Drug Interactions PREZISTA/ritonavir may interact with many drugs; therefore, advise patients to report to their healthcare provider the use of any other prescription or nonprescription medication or herbal products, including St. John's wort [see Contraindications (4) , Warnings and Precautions (5.4 , 5.5) and Drug Interactions (7) ] . Contraception Instruct patients receiving combined hormonal contraception or the progestin only pill to use an effective alternative (non-hormonal) contraceptive method or add a barrier method during therapy with PREZISTA/ritonavir because hormonal levels may decrease [see Drug Interactions (7.3) and Use in Specific Populations (8.3) ] .

Fat Redistribution Inform patients that redistribution or accumulation of body fat may occur in patients receiving antiretroviral therapy, including PREZISTA/ritonavir, and that the cause and long-term health effects of these conditions are not known at this time [see Warnings and Precautions (5.7) ] . Immune Reconstitution Syndrome Advise patients to inform their healthcare provider immediately of any symptoms of infection, as in some patients with advanced HIV infection (AIDS), signs and symptoms of inflammation from previous infections may occur soon after anti-HIV treatment is started [see Warnings and Precautions (5.8) ].

Pregnancy Registry Inform patients that there is an antiretroviral pregnancy registry to monitor fetal outcomes of pregnant women exposed to PREZISTA [see Use in Specific Populations (8.1) ] . Lactation Instruct women with HIV-1 infection not to breastfeed because HIV-1 can be passed to the baby in breast milk [see Use in Specific Populations (8.2) ] .

🧬 Pharmacokinetics ~3 min read ▾

12.3Pharmacokinetics Pharmacokinetics in Adults General Darunavir is primarily metabolized by CYP3A. Ritonavir inhibits CYP3A, thereby increasing the plasma concentrations of darunavir. When a single dose of PREZISTA 600 mg was given orally in combination with 100 mg ritonavir twice daily, there was an approximate 14-fold increase in the systemic exposure of darunavir.

Therefore, PREZISTA should only be used in combination with 100 mg of ritonavir to achieve sufficient exposures of darunavir. The pharmacokinetics of darunavir, co-administered with low dose ritonavir (100 mg), has been evaluated in healthy adult volunteers and in HIV-1-infected subjects. Table 11 displays the population pharmacokinetic estimates of darunavir after oral administration of PREZISTA/ritonavir 600/100 mg twice daily (based on sparse sampling in 285 patients in trial TMC114-C214, 278 patients in trial TMC114-C229 and 119 patients [integrated data] from trials TMC114-C202 and TMC114-C213) and PREZISTA/ritonavir 800/100 mg once daily (based on sparse sampling in 335 patients in trial TMC114-C211 and 280 patients in trial TMC114-C229) to HIV-1-infected patients.

Table 11: Population Pharmacokinetic Estimates of Darunavir at PREZISTA/ritonavir 800/100 mg Once Daily (Trial TMC114-C211, 48-Week Analysis and Trial TMC114-C229, 48-Week Analysis) and PREZISTA/ritonavir 600/100 mg Twice Daily (Trial TMC114-C214, 48-Week Analysis, Trial TMC114-C229, 48-Week Analysis and Integrated Data from Trials TMC114-C213 and TMC114-C202, Primary 24-Week Analysis) PREZISTA/ritonavir 800/100 mg once daily PREZISTA/ritonavir 600/100 mg twice daily Parameter TMC114-C211 N=335 TMC114-C229 N=280 TMC114-C214 N=285 TMC114-C229 N=278 TMC114-C213 + TMC114-C202 (integrated data) N=119 N=number of subjects with data AUC 24h (ng.h/mL) AUC 24h is calculated as AUC 12h*2.

Mean ± Standard Deviation 93026 ± 27050 93334 ± 28626 116796 ± 33594 114302 ± 32681 124698 ± 32286 Median (Range) 87854 (45000–219240) 87788 (45456–236920) 111632 (64874–355360) 109401 (48934–323820) 123336 (67714–212980) C 0h (ng/mL) Mean ± Standard Deviation 2282 ± 1168 2160 ± 1201 3490 ± 1401 3386 ± 1372 3578 ± 1151 Median (Range) 2041 (368–7242) 1896 (184–7881) 3307 (1517–13198) 3197 (250–11865) 3539 (1255–7368) Absorption and Bioavailability Darunavir, co-administered with 100 mg ritonavir twice daily, was absorbed following oral administration with a T max of approximately 2.5–4 hours.

The absolute oral bioavailability of a single 600 mg dose of darunavir alone and after co-administration with 100 mg ritonavir twice daily was 37% and 82%, respectively. In vivo data suggest that PREZISTA/ritonavir is an inhibitor of the P-glycoprotein (P-gp) transporters. Effects of Food on Oral Absorption When PREZISTA tablets were administered with food, the C max and AUC of darunavir, co-administered with ritonavir, is approximately 40% higher relative to the fasting state.

Within the range of meals studied, darunavir exposure is similar. The total caloric content of the various meals evaluated ranged from 240 Kcal (12 gms fat) to 928 Kcal (56 gms fat). Distribution Darunavir is approximately 95% bound to plasma proteins.

Darunavir binds primarily to plasma alpha 1-acid glycoprotein (AAG). Metabolism In vitro experiments with human liver microsomes (HLMs) indicate that darunavir primarily undergoes oxidative metabolism. Darunavir is extensively metabolized by CYP enzymes, primarily by CYP3A.

A mass balance study in healthy volunteers showed that after a single dose administration of 400 mg 14 C-darunavir, co-administered with 100 mg ritonavir, the majority of the radioactivity in the plasma was due to darunavir. At least 3 oxidative metabolites of darunavir have been identified in humans; all showed activity that was at least 90% less than the activity of darunavir against wild-type HIV-1. Elimination A mass balance study in healthy volunteers showed that after single dose administration of 400 mg 14 C-darunavir, co-administere… [Excerpted — this section continues on DailyMed.]

🧬 Pharmacodynamics 28 words ▾

12.2Pharmacodynamics Cardiac Electrophysiology In a thorough QT/QTc study in 40 healthy subjects, PREZISTA/ritonavir doses of 1.33 times the maximum recommended dose did not affect the QT/QTc interval.

🔬 Clinical Studies ~3 min read ▾

14 CLINICAL STUDIES

14.1Description of Adult Clinical Trials The evidence of efficacy of PREZISTA/ritonavir is based on the analyses of 192-week data from a randomized, controlled open-label Phase 3 trial in treatment-naïve (TMC114-C211) HIV-1-infected adult subjects and 96-week data from a randomized, controlled, open-label Phase 3 trial in antiretroviral treatment-experienced (TMC114-C214) HIV-1-infected adult subjects. In addition, 96-week data are included from 2 randomized, controlled Phase 2b trials, TMC114-C213 and TMC114-C202, in antiretroviral treatment-experienced HIV-1-infected adult subjects.

14.2Treatment-Naïve Adult Subjects TMC114-C211 TMC114-C211 is a randomized, controlled, open-label Phase 3 trial comparing PREZISTA/ritonavir 800/100 mg once daily versus lopinavir/ritonavir 800/200 mg per day (given as a twice daily or as a once daily regimen) in antiretroviral treatment-naïve HIV-1-infected adult subjects. Both arms used a fixed background regimen consisting of tenofovir disoproxil fumarate 300 mg once daily (TDF) and emtricitabine 200 mg once daily (FTC). HIV-1-infected subjects who were eligible for this trial had plasma HIV-1 RNA greater than or equal to 5000 copies/mL.

Randomization was stratified by screening plasma viral load (HIV-1 RNA less than 100,000 copies/mL or greater than or equal to 100,000 copies/mL) and screening CD4+ cell count (less than 200 cells/mm 3 or greater than or equal to 200 cells/mm 3 ). Virologic response was defined as a confirmed plasma HIV-1 RNA viral load less than 50 copies/mL. Analyses included 689 subjects in trial TMC114-C211 who had completed 192 weeks of treatment or discontinued earlier.

Demographics and baseline characteristics were balanced between the PREZISTA/ritonavir arm and the lopinavir/ritonavir arm (see Table 19 ). Table 19 compares the demographic and baseline characteristics between subjects in the PREZISTA/ritonavir 800/100 mg once daily arm and subjects in the lopinavir/ritonavir 800/200 mg per day arm in trial TMC114-C211. Table 19: Demographic and Baseline Characteristics of Subjects in Trial TMC114-C211 PREZISTA/ritonavir 800/100 mg once daily + TDF/FTC N=343 lopinavir/ritonavir 800/200 mg per day + TDF/FTC N=346 FTC=emtricitabine; TDF=tenofovir disoproxil fumarate Demographic characteristics Median age (years) (range, years) 34 (18–70) 33 (19–68) Sex Male 70% 70% Female 30% 30% Race White 40% 45% Black 23% 21% Hispanic 23% 22% Asian 13% 11% Baseline characteristics Mean baseline plasma HIV-1 RNA (log 10 copies/mL) 4.86

4.84Median baseline CD4+ cell count (cells/mm 3 ) (range, cells/mm 3 ) 228 (4–750) 218 (2–714) Percentage of patients with baseline viral load ≥100,000 copies/mL 34% 35% Percentage of patients with baseline CD4+ cell count <200 cells/mm 3 41% 43% Week 192 outcomes for subjects on PREZISTA/ritonavir 800/100 mg once daily from trial TMC114-C211 are shown in Table 20. Table 20: Virologic Outcome of Randomized Treatment of Trial TMC114-C211 at 192 Weeks PREZISTA/ritonavir 800/100 mg once daily + TDF/FTC N=343 lopinavir/ritonavir 800/200 mg per day + TDF/FTC N=346 N = total number of subjects with data; FTC=emtricitabine; TDF=tenofovir disoproxil fumarate Virologic success HIV-1 RNA <50 copies/mL 70% 95% CI: 1.9; 16.1 61% Virologic failure Includes patients who discontinued prior to Week 192 for lack or loss of efficacy and patients who are ≥50 copies in the 192-week window and patients who had a change in their background regimen that was not permitted by the protocol.

12% 15% No virologic data at Week 192 window Window 186–198 Weeks. Reasons Discontinued trial due to adverse event or death Includes patients who discontinued due to adverse event or death at any time point from Day 1 through the time window if this resulted in no virologic data on treatment during the specified window. 5% 13% Discontinued trial for other reasons Other includes: withdrew consent, loss to follow-up, etc., if the viral load at the time of discontinuation wa… [Excerpted — this section continues on DailyMed.]

🧪 Nonclinical Toxicology ~1 min read ▾

13 NONCLINICAL TOXICOLOGY

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis and Mutagenesis Darunavir was evaluated for carcinogenic potential by oral gavage administration to mice and rats up to 104 weeks. Daily doses of 150, 450 and 1000 mg/kg were administered to mice and doses of 50, 150 and 500 mg/kg was administered to rats. A dose-related increase in the incidence of hepatocellular adenomas and carcinomas were observed in males and females of both species as well as an increase in thyroid follicular cell adenomas in male rats.

The observed hepatocellular findings in rodents are considered to be of limited relevance to humans. Repeated administration of darunavir to rats caused hepatic microsomal enzyme induction and increased thyroid hormone elimination, which predispose rats, but not humans, to thyroid neoplasms. At the highest tested doses, the systemic exposures to darunavir (based on AUC) were between 0.4- and 0.7-fold (mice) and 0.7- and 1-fold (rats), relative to those observed in humans at the recommended therapeutic doses (600/100 mg twice daily or 800/100 mg once daily).

Darunavir was not mutagenic or genotoxic in a battery of in vitro and in vivo assays including bacterial reserve mutation (Ames), chromosomal aberration in human lymphocytes and in vivo micronucleus test in mice. Impairment of Fertility No effects on fertility or early embryonic development were observed with darunavir in rats.

📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 218 words ▾

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis and Mutagenesis Darunavir was evaluated for carcinogenic potential by oral gavage administration to mice and rats up to 104 weeks. Daily doses of 150, 450 and 1000 mg/kg were administered to mice and doses of 50, 150 and 500 mg/kg was administered to rats. A dose-related increase in the incidence of hepatocellular adenomas and carcinomas were observed in males and females of both species as well as an increase in thyroid follicular cell adenomas in male rats.

The observed hepatocellular findings in rodents are considered to be of limited relevance to humans. Repeated administration of darunavir to rats caused hepatic microsomal enzyme induction and increased thyroid hormone elimination, which predispose rats, but not humans, to thyroid neoplasms. At the highest tested doses, the systemic exposures to darunavir (based on AUC) were between 0.4- and 0.7-fold (mice) and 0.7- and 1-fold (rats), relative to those observed in humans at the recommended therapeutic doses (600/100 mg twice daily or 800/100 mg once daily).

Darunavir was not mutagenic or genotoxic in a battery of in vitro and in vivo assays including bacterial reserve mutation (Ames), chromosomal aberration in human lymphocytes and in vivo micronucleus test in mice. Impairment of Fertility No effects on fertility or early embryonic development were observed with darunavir in rats.

📄 Patient Package Insert ~3 min read ▾

This Patient Information has been approved by the U.S. Food and Drug Administration. Revised: 03/2023 PATIENT INFORMATION PREZISTA ® (pre-ZIS-ta) (darunavir) oral suspension PREZISTA ® (pre-ZIS-ta) (darunavir) tablet Read this Patient Information before you start taking PREZISTA and each time you get a refill.

There may be new information. This information does not take the place of talking to your healthcare provider about your medical condition or your treatment. Also read the Patient Information leaflet for ritonavir.

What is the most important information I should know about PREZISTA? Ask your healthcare provider or pharmacist about medicines that should not be taken with PREZISTA. For more information, see " Who should not take PREZISTA? " and " What should I tell my healthcare provider before taking PREZISTA? " PREZISTA may cause liver problems.

Some people taking PREZISTA in combination with ritonavir have developed liver problems, which may be life-threatening. Your healthcare provider should do blood tests before and during your PREZISTA and ritonavir combination treatment. If you have chronic hepatitis B or C infection, your healthcare provider should check your blood tests more often because you have an increased chance of developing liver problems.

Tell your healthcare provider if you have any of the below signs and symptoms of liver problems. dark (tea colored) urine yellowing of your skin or whites of your eyes pale colored stools (bowel movements) nausea vomiting pain or tenderness on your right side below your ribs loss of appetite tiredness PREZISTA may cause severe or life-threatening skin reactions or rash. Sometimes these skin reactions and skin rashes can become severe and require treatment in a hospital. Tell your healthcare provider right away if you develop a rash.

Stop taking PREZISTA and ritonavir combination treatment and tell your healthcare provider right away if you have any skin changes with symptoms below: fever tiredness muscle or joint pain blisters or skin lesions mouth sores or ulcers red or inflamed eyes, like "pink eye" (conjunctivitis) Rash occurred more often in people taking PREZISTA and raltegravir together than with either drug separately, but was generally mild. See " What are the possible side effects of PREZISTA? " for more information about side effects.

What is PREZISTA? PREZISTA is a prescription HIV-1 (Human Immunodeficiency Virus-type 1) medicine used with ritonavir and other antiretroviral medicines to treat HIV-1 infection in adults and children 3 years of age and older. HIV is the virus that causes AIDS (Acquired Immune Deficiency Syndrome).

PREZISTA should not be used in children under 3 years of age. When used with other antiretroviral medicines to treat HIV-1 infection, PREZISTA may help: reduce the amount of HIV-1 in your blood. This is called "viral load". increase the number of CD4+ (T) cells in your blood that help fight off other infections.

Reducing the amount of HIV-1 and increasing the CD4+ (T) cells in your blood may improve your immune system. This may reduce your risk of death or getting infections that can happen when your immune system is weak (opportunistic infections). PREZISTA does not cure HIV-1 infection or AIDS.

You must keep taking HIV-1 medicines to control HIV-1 infection and decrease HIV-related illnesses. Avoid doing things that can spread HIV-1 infection to others: Do not share or re-use needles or other injection equipment. Do not share personal items that can have blood or body fluids on them, like toothbrushes and razor blades.

Do not have any kind of sex without protection. Always practice safe sex by using a latex or polyurethane condom to lower the chance of sexual contact with semen, vaginal secretions, or blood. Ask your healthcare provider if you have any questions on how to prevent passing HIV to other people.

Who should not take PREZISTA? Do not take PREZISTA with any medicine that contains: alfuzosin colchicine, if you have liver or k… [Excerpted — this section continues on DailyMed.]

📖 Instructions for Use ~3 min read ▾

Instructions for Use Advise patients to take PREZISTA and ritonavir with food every day on a regular dosing schedule, as missed doses can result in development of resistance. PREZISTA must always be used with ritonavir in combination with other antiretroviral drugs. Advise patients not to alter the dose of either PREZISTA or ritonavir, discontinue ritonavir, or discontinue therapy with PREZISTA without consulting their physician [see Dosage and Administration (2) ] .

INSTRUCTIONS FOR USE PREZISTA (pre-ZIS-ta) (darunavir) oral suspension Be sure that you read, understand, and follow these Instructions for Use so that you measure and take PREZISTA oral suspension correctly. Ask your healthcare provider if you are not sure. Each PREZISTA oral suspension carton contains: 1 bottle of PREZISTA oral suspension Oral dosing syringe 1 oral syringe adapter Important information for use: Shake PREZISTA oral suspension well before each use.

PREZISTA oral suspension should be given with the oral dosing syringe provided to make sure you measure the right amount. The oral dosing syringe provided with your PREZISTA oral suspension should not be used for any other medicines. Shake the bottle.

Shake the bottle well before each use (See Figure A ). Figure A: Shake the bottle Open the bottle of PREZISTA oral suspension. Open the bottle by pushing downward on the cap and twisting it in the direction of the arrow (counter-clockwise) (See Figure B ).

Figure B: Opening the bottle The first time a bottle of PREZISTA oral suspension is used: Insert the oral syringe adapter into the bottle. Press on the adapter until it is even with the top of the bottle (See Figure C ). Do not remove the oral syringe adapter from the bottle once inserted.

Figure C: Inserting the adapter Insert the oral dosing syringe. Fully push down (depress) the plunger of the syringe. Insert the syringe into the opening of the oral syringe adapter until it is firmly in place (See Figure D ).

Figure D: Inserting the syringe Withdraw the prescribed amount of PREZISTA oral suspension. Turn the bottle upside down. Gently pull back the plunger of the syringe until the bottom of the plunger is even with the markings on the syringe for the prescribed dose (See Figure E ).

If you see air bubbles in the syringe, push the plunger in to empty the oral suspension back into the bottle. Then repeat steps 4 and 5. If you or your child's dose of PREZISTA oral suspension is more than 6 mL, you will need to divide the dose.

Follow the instructions given to you by your healthcare provider or pharmacist about how to divide the dose. Figure E: Withdrawing the Oral Suspension Turn the bottle upright and remove the syringe from the bottle by pulling straight up on the oral dosing syringe (See Figure F ). Figure F: Removing the syringe Take the dose of PREZISTA.

Place the tip of the oral dosing syringe in the mouth. Press on the plunger of the syringe towards the mouth (See Figure G ). If you or your child's dose is more than 6 mL you will need to divide the dose.

Follow the instructions given to you by your healthcare provider or pharmacist about how to divide the dose, and repeat steps 4 through 7. Figure G: Taking the dose of PREZISTA Close the bottle with the cap after use. Close the bottle by twisting the cap in the direction of the arrow (clockwise) (See Figure H ).

Figure H: Closing the bottle Remove the plunger from the barrel by pulling the plunger and barrel away from each other (See Figure I ). Rinse both parts of the syringe with water and allow to air dry after each use. Figure I: Removing the plunger from the barrel After air drying, put the oral dosing syringe back together by inserting the plunger into the barrel (See Figure J ).

Store the oral dosing syringe with PREZISTA oral suspension. Figure J: Putting the syringe back together How should I store PREZISTA? Store PREZISTA oral suspension and the oral dosing syringe at room temperature 77°F (25°C).

Do not refrigerate or freeze PREZISTA o… [Excerpted — this section continues on DailyMed.]

📄 Recent Major Changes 5 words ▾

Contraindications ( 4 ) 4/2022

📄 Package Label / Principal Display Panel ~1 min read ▾

PRINCIPAL DISPLAY PANEL - 75 mg Tablet Bottle Label NDC 59676- 563 -01 PREZISTA ® (darunavir) tablets 75 mg ALERT Find out about medicines that should NOT be taken with PREZISTA Rx only 480 Tablets Johnson &Johnson PREZISTA 75 mg PDP

PRINCIPAL DISPLAY PANEL - 150 mg Tablet Bottle Label NDC 59676- 564 -01 PREZISTA ® (darunavir) tablets 150 mg ALERT Find out about medicines that should NOT be taken with PREZISTA. Rx only 240 Tablets Johnson &Johnson PREZISTA 150 mg PDP

PRINCIPAL DISPLAY PANEL - 600 mg Tablet Bottle Label NDC 59676- 562 -01 PREZISTA ® (darunavir) tablets 600 mg ALERT Find out about medicines that should NOT be taken with PREZISTA. Rx only 60 Tablets Johnson &Johnson PREZISTA 600 mg PDP

PRINCIPAL DISPLAY PANEL - 800 mg Tablet Bottle Label NDC 59676- 566 -30 PREZISTA ® (darunavir) tablets 800 mg ALERT Find out about medicines that should NOT be taken with PREZISTA. Rx only 30 Tablets Johnson &Johnson PREZISTA 800 mg PDP

PRINCIPAL DISPLAY PANEL - 200 mL Bottle Carton NDC 59676- 565 -01 PREZISTA ® (darunavir) Oral Suspension 100 mg per mL DISPENSING: For information concerning proper usage of the oral dosing syringe, see accompanying PATIENT INFORMATION and INSTRUCTIONS FOR USE. ALERT Find out about medicines that should NOT be taken with PREZISTA. Rx only 200 mL Johnson &Johnson PREZISTA OS PDP

Source: FDA Structured Product Labeling, mirrored from DailyMed / openFDA. Prefer the government’s original formatting? View this label on DailyMed ↗

Medicare Part D spend CMS · PART D · 2026 (Q1)

Medicare Part D (outpatient prescription) spending for Prezista — the program that covers self-administered drugs. 1 manufacturer.
⚠️ Drug-level data: CMS publishes Part D spending by drug, not by NDC — these figures combine every manufacturer, strength and package size sold under the name Prezista. That’s a different level of aggregation than the Medicaid card above, which is specific to this exact 11-digit NDC (pack size included), so the two aren’t directly comparable.
Period
Total Part D spend
$1.64M
Claims incl. refills
809
Beneficiaries
386
Spend / beneficiary
$4,237.13
Spend / claim
$2,021.67
Trend by period
💵 About the dollar figures: spending is what Part D plans paid before confidential manufacturer rebates, so the program’s real net cost is lower. A blank patient count means fewer than 11 people — CMS hides counts that small to protect privacy. Source: CMS Medicare Quarterly Part D Spending by Drug (data.cms.gov), updated quarterly.

About this NDC listing & data coverage

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Questions about this listing

Why is there no price listed?
The pricing shown on our NDC pages comes from CMS NADAC, a voluntary survey of retail community pharmacy invoices. CMS does not publish a NADAC for every NDC — packages outside the retail survey (institutional and hospital products, bulk packages, discontinued items, and many OTC items) may never receive one. A missing price reflects the survey's scope, not this product's actual cost, and does not mean the product is free or unavailable.
Is the NDC printed on the package the same as the 11-digit billing NDC?
Yes, they identify this exact package in different formats. The form printed on the packaging and shown on DailyMed is the one the FDA registered. Insurance claims use a fixed 11-digit 5-4-2 format, so the short segment is padded with a leading zero and the dashes are dropped. The Identity section at the top of this page lists each form of this code.
Is this package still being marketed?
Yes, per the latest FDA NDC Directory data on this page: this package is listed as actively marketed, with no marketing end date reported by Janssen Products LP. Listing status can change — the directory data on this page refreshes weekly.
Who lists this product with the FDA?
Janssen Products LP is the labeler of record for this NDC — the company under whose FDA-assigned code the package is listed. The labeler may be the manufacturer itself or a distributor marketing the product under its own code.
Do I need a prescription for this product?
This NDC is listed with FDA as a prescription product, so it is dispensed under a prescriber's order. Your pharmacist can tell you whether any over-the-counter forms of the same medication exist.
This page identifies an FDA-listed package (the NDC) and reports public regulatory and pricing data about the listing. It is reference information, not a medical recommendation — talk to your pharmacist or prescriber about your own medication.
Where does this data come from?
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← 59676-0563-01 · Janssen 59676-0565-01 · Janssen →
For educational and professional reference only — not medical advice. Pricing reflects published NADAC and CMS ASP (free public data) and may differ from your acquisition cost; always verify before billing or dispensing.