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Rilpivirine 25 mg Tablet, Film Coated, 30-count — NDC 42385-0999-30 package photo

Rilpivirine 25 mg Tablet, Film Coated, 30-count

by Laurus Labs Limited · 30 TABLET, FILM COATED in 1 BOTTLE (42385-999-30)
NDC 42385-0999-30
🏷️ FDA NDC (as labeled) 42385-999-30 billing pads the product segment with a zero
This package
Contains30-count Pack sizes2 compare ↓
Also comes in: 30 tablets 42385-0999-31
Rx only Generic On market Non-controlled
🗂️ Data synced 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

🆔 Identity & classification

FDA NDC (as labeled) 42385-999-30
Product NDC 42385-999
11-digit billing NDC 42385099930
RxCUI 1102273
UNII 212WAX8KDD
Application # ANDA219788
SPL Set ID dadbf50d-6b7d-4fb5-bd9f-7769b048e764
Established class (EPC) Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor
Mechanism of action Non-Nucleoside Reverse Transcriptase Inhibitors
Chemical class Non-Nucleoside Analog
DEA schedule Non-controlled
Marketing category ANDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2026-07-10
Route ORAL
Dosage form TABLET, FILM COATED
Substance RILPIVIRINE HYDROCHLORIDE
TE code (Orange Book) AB · RLD · RS
Why two NDCs? The FDA registers this code as 42385-999-30 — 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 → 42385-0999-30. 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 Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor class.

Pharmacologic class Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor
Drug family (ATC) Non-nucleoside reverse transcriptase inhibitors
How it works Non-Nucleoside Reverse Transcriptase 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.

🏭 Manufacturer & labeler

LabelerLaurus Labs Limited
Application holderLAURUS LABS LTD
FDA applicationANDA219788 (ANDA)
Labeler code42385
First marketedJul 2026
Product typeHuman Prescription Drug
Portfolio86 products on file
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.

🩺 Clinical

📖 What it is MedlinePlus · NLM

Rilpivirine is used to treat human immunodeficiency virus type 1 (HIV-1). Rilpivirine is in a class of medications called non-nucleoside reverse transcriptase inhibitors (NNRTIs). It works by decreasing the amount of HIV in the blood. Although rilpivirine 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
  • Rilpivirine is one piece of your HIV treatment — it blocks a specific enzyme the virus uses to copy itself. But HIV is smart and can develop resistance if only one medicine is used...
  • What exactly is rilpivirine and why do I have to take it with other HIV medicines?
  • It really does matter. When rilpivirine is taken without food, your body absorbs about 40% less of the medicine — and if levels in your blood fall too low, the virus can start repl...
  • Why is it so important to take this with food? Can't I just take it whenever?
📖 Read our full Rilpivirine 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.

💊 What it looks like

Color White
ShapeRound
Imprint5L
Size12 mm
ScoringNot scored
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 M28OL1HH48
    Croscarmellose sodium is a plant-based substance derived from cellulose. It acts as a disintegrant, helping tablets and capsules break down quickly in the digestive system so the medicine can be absorbed.
  • UNII 0WZ8WG20P6
    Hypromellose 2910 is a plant-based cellulose derivative that acts as a thickener, binder, and film-coating agent. It helps control how quickly the medicine dissolves and protects the tablet or capsule from moisture and light.
  • UNII EWQ57Q8I5X
    Lactose monohydrate is a natural sugar derived from milk. It serves as a filler and binder in tablets and capsules, helping create the proper size, texture, and consistency of the medicine.
  • 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 Q662QK8M3B
    Polyethylene glycol 8000 is a synthetic polymer made from ethylene oxide. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and add bulk to the medicine.
  • UNII 7T1F30V5YH
    A synthetic emulsifier derived from sorbitol and oleic acid. It helps mix oil and water-based ingredients together and keeps them from separating in liquid formulations.
  • UNII U725QWY32X
    Povidone K30 is a synthetic polymer made from petroleum. It acts as a binder to hold tablet ingredients together and as a disintegrant to help the tablet break apart in the stomach so the medicine can be absorbed.
  • UNII GRV5BG8C5N
    A plant-based filler and binder made from cellulose combined with silica. It helps hold tablet ingredients together, improves flowability during manufacturing, and ensures consistent tablet density and shape.
  • 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.

9 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.

💲 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 · quarterly No Part D plan price is available for this NDC in our data.
ℹ️
No price is published for this exact package yet. CMS surveys NADAC per package size, so a different pack of the same drug often has one.
Try another pack size: 30 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.

🔁 Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Rilpivirine 25 mg 70069-0848-30 Somerset 30 tablets — AB FDA listed —
Rilpivirine 25 mgthis 42385-0999-30 Laurus 30 tablets — AB FDA listed —
About this product: this is a generic version of the medicine. FDA equivalence ratings are shown when available, and other versions are listed above, least expensive first.
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

🏛️
2026
On the market since
Jul 2026
📍
2026
Currently FDA-listed
listed with the FDA
🔓
·
Generic on the market
this product is a generic
✅This is a generic drug

This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.

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.

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

Medicare Part D (outpatient prescription) spending for Rilpivirine — 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 Rilpivirine. 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.
Total Part D spend
$347.9K
Claims incl. refills
246
Beneficiaries
226
Spend / beneficiary
$1,539.18
Spend / claim
$1,414.05
💵 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.

🔬 Reported adverse events (FAERS)

Read carefully: FAERS reports are voluntary and unverified. Counts are not incidence, do not establish causation, are subject to reporting bias, and cannot be used to compare one drug to another. Shown for signal context only. Reports for RILPIVIRINE — the ingredient across all brands.

Top reported reactions

Bone Density Decreased4,430
Renal Injury3,215
Skeletal Injury2,981
Chronic Kidney Disease2,716
Pain2,656
Tooth Loss2,413
Renal Failure2,172

Age at onset

Neonate46
Infant23
Child7
Adolescent21
Adult10,162
Elderly733

Reporter sex

24,864 reports
Male · 70%
Female · 29%
Unknown · 0%

Serious outcomes

Hospitalization2,090
Reports over time (by year) — tap or hover for the count & year
2021 2022 2024 2026 3,708 1,129
Most recent year is provisional (FAERS lags ~3 months).
Where does this data come from?
Adverse-event reports from the FDA Adverse Event Reporting System (FAERS) via openFDA. FAERS reports are voluntary and unverified — counts are not incidence and don’t establish causation.

📦 Packaging — all sizes for this product

Package NDCDescription Marketing startStatus
42385-0999-30 You're viewing this 30 TABLET, FILM COATED in 1 BOTTLE (42385-999-30) 2026-07-10 Active
42385-0999-31 30 TABLET, FILM COATED in 1 BOTTLE (42385-999-31) 2026-07-10 Active

Pack size FAQ

What quantity is in NDC 42385-0999-30?
NDC 42385-0999-30 is a 30-count package — 30 tablet, film coated in 1 bottle.
What is the difference between NDC 42385-0999-30 and NDC 42385-0999-31?
Both are Rilpivirine 25 mg Tablet, Film Coated — the drug itself is identical. NDC 42385-0999-30 is the 30-count package, while NDC 42385-0999-31 is the 30 tablets package.
What NDC number is used to bill for this package of Rilpivirine 25 mg Tablet, Film Coated?
Bill NDC 42385-0999-30 — the 11-digit billing format is 42385099930. Pharmacy and medical claims use the 11-digit form; the FDA label may print a shorter form of the same code.

🧭 About this NDC listing & data coverage

Finished prescription product
What data is (and isn’t) available for this NDC — tap to expand
NDC identity (package / product / labeler codes) ✓ Available
Labeler ✓ Available
Product & package description ✓ Available
Marketing category & status ✓ Available
Active ingredient / dosage form / route ✓ Available
FDA label (SPL via DailyMed) ✓ Available
Package photos ✓ Available
Inactive ingredients (structured) ✓ Available
NADAC pharmacy acquisition price (CMS) — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey.
Orange Book / therapeutic-equivalence data ✓ Available
HCPCS J-code billing crosswalk — Not published for this NDC Most self-administered / retail products have no J-code — that is normal.
Medicaid utilization (CMS SDUD) — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold.
“Not published” reflects what the public FDA / CMS / NLM sources provide for this exact package code — it is a property of the data feeds, not a judgment about the product.

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 FDA registers it as 42385-999-30, which is what is printed on the packaging and shown on DailyMed. Insurance claims use a fixed 11-digit 5-4-2 format, so the short segment is padded with a leading zero: 42385-0999-30, written without dashes as 42385099930. The Identity section at the top of this page lists every form of this code.
What do the three segments of this NDC mean?
In 42385-0999-30, the first segment (42385) is the labeler code FDA assigned to Laurus Labs Limited; the middle segment (0999) identifies this specific product — its ingredient, strength, and dosage form; and the last segment (30) identifies this exact package size and type. Together they name one specific package of one specific product.
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 Laurus Labs Limited. Listing status can change — the directory data on this page refreshes weekly.
Does this product come in other package sizes?
Yes — the FDA directory lists 1 other package presentation of this same product, including 30 tablets (42385-0999-31). Each has its own NDC and its own page — see the package list near the top of this page.
Who lists this product with the FDA?
Laurus Labs Limited 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?
Listing facts (marketing category, packager status, marketing dates) from the FDA openFDA NDC Directory; label availability from DailyMed; pricing coverage from CMS NADAC; equivalence scope from the FDA Orange Book.

📄 Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. 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 📋 Description 💬 Information for Patients
🎯 Indications and Usage ~2 min read ▾

1 INDICATIONS AND USAGE Rilpivirine tablets are a human immunodeficiency virus type 1 (HIV-1) specific, non-nucleoside reverse transcriptase inhibitor (NNRTI) indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in treatment-naïve patients 12 years of age and older and weighing at least 35 kg with HIV-1 RNA less than or equal to 100,000 copies/mL. ( 1.1 ). Limitations of Use: • More rilpivirine treated subjects with HIV-1 RNA greater than 100,000 copies/mL at the start of therapy experienced virologic failure (HIV-1 RNA ≥50 copies/mL) compared to rilpivirine treated subjects with HIV-1 RNA less than or equal to 100,000 copies/mL.

( 1.1 , 14 ) Rilpivirine tablets are indicated in combination with VOCABRIA (cabotegravir), for short-term treatment of HIV-1 infection in adults and adolescents 12 years and older and weighing at least 35 kg who are virologically suppressed (HIV-1 RNA less than 50 copies/mL) on a stable regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine. ( 1.2 )

1.1Treatment of HIV-1 in Treatment-Naïve Patients Rilpivirine tablets, in combination with other antiretroviral agents, are indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in antiretroviral treatment-naïve patients 12 years of age and older and weighing at least 35 kg with plasma HIV-1 RNA less than or equal to 100,000 copies/mL at the start of therapy. Limitations of Use • More rilpivirine treated subjects with HIV-1 RNA greater than 100,000 copies/mL at the start of therapy experienced virologic failure (HIV-1 RNA ≥50 copies/mL) compared to rilpivirine treated subjects with HIV-1 RNA less than or equal to 100,000 copies/mL [see Clinical Studies (14.1) ].

Additional pediatric use information is approved for Janssen Products LP's Edurant (Rilpivirine) tablets. However, due to Janssen Products LP's marketing exclusivity rights, this drug product is not labeled with that information.

1.2Treatment of HIV-1 in Combination with Cabotegravir Rilpivirine tablets are indicated in combination with VOCABRIA (cabotegravir) for short-term treatment of HIV-1 infection in adults and adolescents 12 years and older and weighing at least 35 kg who are virologically suppressed (HIV-1 RNA less than 50 copies/mL) on a stable antiretroviral regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine, for use as [see Dosage and Administration (2.6) ] : • oral lead-in to assess the tolerability of rilpivirine prior to administration of rilpivirine extended-release injectable suspension, a component of CABENUVA (cabotegravir extended- release injectable suspension; rilpivirine extended-release injectable suspension). • oral therapy for patients who will miss planned injection dosing with CABENUVA (cabotegravir extended-release injectable suspension; rilpivirine extended-release injectable suspension).

⏱️ Dosage and Administration ~3 min read ▾

2 DOSAGE AND ADMINISTRATION • One 25 mg rilpivirine tablet taken once daily with a meal for patients weighing at least 35 kg. ( 2.2 ) • Do not substitute rilpivirine tablets and EDURANT PED tablets for oral suspension on a milligram-per-milligram basis due to differing pharmacokinetic profiles. ( 2.1 , 5.6 ) • See full prescribing information for dosing information when used in combination with cabotegravir.

( 2.6 ) • For pregnant patients who are already on a stable rilpivirine regimen prior to pregnancy and who are virologically suppressed (HIV-1 RNA less than 50 copies per mL) the recommended dosage in adults and pediatric patients weighing more than 35 kg is one 25 mg tablet once daily taken orally with a meal. ( 2.5 , 12.3 ) • Rifabutin coadministration: Take two 25 mg tablets of rilpivirine once daily with a meal for the duration of the rifabutin coadministration. ( 2.7 )

2.1Overview of Dosage Form Rilpivirine tablets are available in : • Rilpivirine 25 mg film-coated tablets for adults and pediatric patients weighing at least 35 kg. Do not substitute rilpivirine tablets and EDURANT PED tablets for oral suspension on a milligram-per-milligram basis due to differing pharmacokinetic profiles. [see Warnings and Precautions (5.6) ] . Take rilpivirine tablets once daily with a meal in combination with other antiretrovirals [see Clinical Pharmacology (12.3) ] .

Additional pediatric use information is approved for Janssen Products LP's Edurant (Rilpivirine) tablets. However, due to Janssen Products LP's marketing exclusivity rights, this drug product is not labeled with that information.

2.2Recommended Dosage in Treatment-Naïve Adult Patients The recommended dosage of rilpivirine in adult patients is one 25 mg tablet taken orally once daily with a meal [see Use in Specific Populations (8.1) and Clinical Pharmacology (12.3) ] .

2.3Recommended Dosage in Treatment-Naïve Pediatric Patients 12 Years of Age and Older and Weighing at least 35 kg The recommended dosage of rilpivirine tablets in pediatric patients 12 years of age and older and weighing at least 35 kg is based on body weight (see Table 1). Rilpivirine tablets should be taken orally once daily with a meal [see Use in Specific Populations (8.4) and Clinical Pharmacology (12.3) ]. Table 1: Recommended Dosage of Rilpivirine Tablets for Pediatric Patients Body Weight (kg) Rilpivirine 25 mg Tablets Total Daily Dose Greater than or equal to 35 kg 1 tablet once daily 25 mg rilpivirine tablets once daily Additional pediatric use information is approved for Janssen Products LP's Edurant (Rilpivirine) tablets.

However, due to Janssen Products LP's marketing exclusivity rights, this drug product is not labeled with that information.

2.5Recommended Dosage During Pregnancy For pregnant patients who are already on a stable rilpivirine regimen prior to pregnancy and who are virologically suppressed (HIV-1 RNA less than 50 copies per mL) the recommended dosage in adults and pediatric patients weighing at least 35 kg is one 25 mg tablet once daily taken orally with a meal. Refer to Table 1 for dosing recommendations for pediatric patients [see Dosage and Administration (2.2 , 2.3) ] . Lower exposures of rilpivirine were observed during pregnancy, therefore viral load should be monitored closely [see Use in Specific Populations (8.1) and Clinical Pharmacology (12.3) ] .

Additional pediatric use information is approved for Janssen Products LP's Edurant (Rilpivirine) tablets. However, due to Janssen Products LP's marketing exclusivity rights, this drug product is not labeled with that information.

2.6Recommended Dosage in Combination with Cabotegravir in Adults and Adolescents 12 Years of Age and Older and Weighing at least 35 kg Consult the prescribing information for CABENUVA (cabotegravir extended-release injectable suspension; rilpivirine extended-release injectable suspension) before initiating rilpivirine to ensure therapy with CABENUVA is appropriate. Oral Lead-In Dosing to Asses…

💊 Dosage Forms and Strengths 54 words ▾

3 DOSAGE FORMS AND STRENGTHS Rilpivirine 25 mg Film-Coated Tablets 25 mg white to off-white, round, biconvex film coated tablets debossed with ‘5L’ on one side and plain on other side. Each tablet contains 27.5 mg of rilpivirine hydrochloride, which is equivalent to 25 mg of rilpivirine. Rilpivirine: 25 mg tablets ( 3 )

⛔ Contraindications 185 words ▾

4 CONTRAINDICATIONS Rilpivirine is contraindicated for coadministration with the drugs in Table 2 for which significant decreases in rilpivirine plasma concentrations may occur due to CYP3A enzyme induction or gastric pH increase, which may result in loss of virologic response and possible resistance to rilpivirine or to the class of NNRTIs [see Drug Interactions (7) and Clinical Pharmacology (12.3) ]. Table 2: Drugs That are Contraindicated with Rilpivirine Drug Class Contraindicated Drugs in Class Clinical Comment Anticonvulsants Carbamazepine Oxcarbazepine Phenobarbital Phenytoin Potential for significant decreases in rilpivirine plasma concentrations due to CYP3A enzyme induction, which may result in loss of virologic response.

Antimycobacterials Rifampin Rifapentine Glucocorticoid (systemic) Dexamethasone (more than a single- dose treatment) Herbal Products St. John’s wort ( Hypericum perforatum ) Proton Pump Inhibitors e.g., Esomeprazole Lansoprazole Omeprazole Pantoprazole Rabeprazole Potential for significant decreases in rilpivirine plasma concentrations due to gastric pH increase, which may result in loss of virologic response. Coadministration of rilpivirine is contraindicated with drugs where significant decreases in rilpivirine plasma concentrations may occur, which may result in loss of virologic response and possible resistance and cross-resistance.

( 4 )

⚠️ Warnings and Cautions ~2 min read ▾

5 WARNINGS AND PRECAUTIONS • Skin and Hypersensitivity Reactions: Severe skin and hypersensitivity reactions have been reported during postmarketing experience, including cases of Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS), with rilpivirine-containing regimens. Immediately discontinue treatment if hypersensitivity or rash with systemic symptoms or elevations in hepatic serum biochemistries develop and closely monitor clinical status, including hepatic serum biochemistries. ( 5.1 ) • Hepatotoxicity: Hepatic adverse events have been reported in patients with underlying liver disease, including hepatitis B or C virus co-infection, or in patients with elevated baseline transaminases.

A few cases of hepatotoxicity have occurred in patients with no pre-existing hepatic disease. Monitor liver function tests before and during treatment with rilpivirine in patients with underlying hepatic disease, such as hepatitis B or C virus co-infection, or marked elevations in transaminase. Also consider monitoring liver functions tests in patients without pre-existing hepatic dysfunction or other risk factors.

( 5.2 ) • Depressive Disorders: Severe depressive disorders have been reported. Immediate medical evaluation is recommended for severe depressive disorders. ( 5.3 ) • Patients may develop immune reconstitution syndrome.

( 5.5 )

5.1Skin and Hypersensitivity Reactions Severe skin and hypersensitivity reactions have been reported during the postmarketing experience, including cases of Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS), with rilpivirine-containing regimens. While some skin reactions were accompanied by constitutional symptoms such as fever, other skin reactions were associated with organ dysfunctions, including elevations in hepatic serum biochemistries. During the Phase 3 clinical trials, treatment-related rashes with at least Grade 2 severity were reported in 3% of subjects receiving rilpivirine.

No Grade 4 rash was reported. Overall, most rashes were Grade 1 or 2 and occurred in the first four to six weeks of therapy [see Adverse Reactions (6.1 and 6.2) ]. Discontinue rilpivirine immediately if signs or symptoms of severe skin or hypersensitivity reactions develop, including but not limited to, severe rash or rash accompanied by fever, blisters, mucosal involvement, conjunctivitis, facial edema, angioedema, hepatitis or eosinophilia.

Clinical status including laboratory parameters should be monitored and appropriate therapy should be initiated.

5.2Hepatotoxicity Hepatic adverse events have been reported in patients receiving a rilpivirine-containing regimen. Patients with underlying hepatitis B or C virus infection, or marked elevations in transaminases prior to treatment may be at increased risk for worsening or development of transaminase elevations with use of rilpivirine. A few cases of hepatic toxicity have been reported in adult patients receiving a rilpivirine-containing regimen who had no pre-existing hepatic disease or other identifiable risk factors.

Appropriate laboratory testing prior to initiating therapy and monitoring for hepatotoxicity during therapy with rilpivirine is recommended in patients with underlying hepatic disease such as hepatitis B or C virus infection, or in patients with marked elevations in transaminases prior to treatment initiation. Liver enzyme monitoring should also be considered for patients without pre-existing hepatic dysfunction or other risk factors.

5.3Depressive Disorders The adverse reaction depressive disorders (depressed mood, depression, dysphoria, major depression, mood altered, negative thoughts, suicide attempt, suicidal ideation) has been reported with rilpivirine. Patients with severe depressive symptoms should seek immediate medical evaluation to assess the possibility that the symptoms are related to rilpivirine, and if so, to determine whether the risks of continued therapy outweigh the benefits. During the Phase 3 trials in adults (N=1,3…

🤒 Adverse Reactions ~3 min read ▾

6 ADVERSE REACTIONS The following adverse reactions are discussed below and in other sections of the labeling: • Skin and Hypersensitivity Reactions [see Warnings and Precautions (5.1) ] • Hepatotoxicity [see Warnings and Precautions (5.2) ] • Depressive Disorders [see Warnings and Precautions (5.3) ] The most common adverse reactions to rilpivirine (incidence >2%) of at least moderate to severe intensity (≥ Grade 2) were depressive disorders, headache, insomnia and rash. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Laurus Generics Inc. at 1-833-3-LAURUS (1-833-352-8787) 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. Clinical Trials Experience in Adults The safety assessment is based on the Week 96 pooled data from 1,368 patients in the Phase 3 controlled trials TMC278-C209 (ECHO) and TMC278-C215 (THRIVE) in antiretroviral treatment-naïve HIV-1 infected adult patients, 686 of whom received rilpivirine (25 mg once daily) [see Clinical Studies (14.1) ].

The median duration of exposure for patients in the rilpivirine arm and efavirenz arm was 104.3 and 104.1 weeks, respectively. Most adverse reactions occurred in the first 48 weeks of treatment. The proportion of subjects who discontinued treatment with rilpivirine or efavirenz due to adverse reaction, regardless of severity, was 2% and 4%, respectively.

The most common adverse reactions leading to discontinuation were psychiatric disorders: 10 (1%) subjects in the rilpivirine arm and 11 (2%) subjects in the efavirenz arm. Rash led to discontinuation in 1 (<1%) subject in the rilpivirine arm and 10 (2%) subjects in the efavirenz arm. Common Adverse Reactions Adverse reactions of at least moderate intensity (≥Grade 2) reported in at least 2% of adult subjects are presented in Table 3.

Selected laboratory abnormalities are included in Table 4. Table 3: Selected Adverse Reactions of at Least Moderate Intensity * (Grades 2 to 4) Occurring in at Least 2% of Antiretroviral Treatment-Naïve HIV-1 Infected Adult Subjects (Week 96 Analysis) N=total number of subjects per treatment group; BR=background regimen * Intensities are defined as follows: Moderate (discomfort enough to cause interference with usual activity); Severe (incapacitating with inability to work or do usual activity). † Includes adverse reactions reported as depressed mood, depression, dysphoria, major depression, mood altered, negative thoughts, suicide attempt, suicide ideation.

System Organ Class, Preferred Term, % Pooled Data from the Phase 3 TMC278-C209 and TMC278-C215 Trials Rilpivirine + BR N=686 Efavirenz + BR N=682 Gastrointestinal Disorders Abdominal pain 2% 2% Nausea 1% 3% Vomiting 1% 2% General Disorders and Administration Site Conditions Fatigue 2% 2% Nervous System Disorders Headache 3% 4% Dizziness 1% 7% Psychiatric Disorders Depressive disorders † 5% 4% Insomnia 3% 4% Abnormal dreams 2% 4% Skin and Subcutaneous Tissue Disorders Rash 3% 11% No new adverse reaction terms were identified in adult subjects in the Phase 3 TMC278-C209 and TMC278-C215 trials between 48 weeks and 96 weeks nor in the Phase 2b TMC278-C204 trial through 240 weeks.

The incidence of adverse events in the Phase 2b TMC278-C204 trial was similar to the Phase 3 trials through 96 weeks. Less Common Adverse Reactions Adverse reactions of at least moderate intensity (≥Grade 2) occurring in less than 2% of antiretroviral treatment-naïve subjects receiving rilpivirine are listed below by System Organ Class. Some adverse events have been included because of investigator’s assessment of potential causal relationship and were considered serious or have been reported in more than 1 subject treated with rilpivirine.

Gastrointestinal Disord…

🔄 Drug Interactions ~3 min read ▾

7 DRUG INTERACTIONS Rilpivirine is primarily metabolized by cytochrome P450 (CYP)3A, and drugs that induce or inhibit CYP3A may thus affect the clearance of rilpivirine. Coadministration of rilpivirine and drugs that induce CYP3A may result in decreased plasma concentrations of rilpivirine and loss of virologic response and possible resistance to rilpivirine or to the class of NNRTIs. Coadministration of rilpivirine and drugs that inhibit CYP3A may result in increased plasma concentrations of rilpivirine.

Coadministration of rilpivirine with drugs that increase gastric pH may result in decreased plasma concentrations of rilpivirine and loss of virologic response and possible resistance to rilpivirine or to the class of NNRTIs. Rilpivirine at the recommended doses are not likely to have a clinically relevant effect on the exposure of drugs metabolized by CYP enzymes. Table 6 shows the established and other potentially significant drug interactions based on which alterations in dose or regimen of rilpivirine and/or coadministered drug may be recommended.

Drugs that are not recommended for coadministration with rilpivirine are also included in Table 6 [see Dosage and Administration (2) , Contraindications (4) , and Clinical Pharmacology (12.3) ]. Table 6: Established and Other Potentially Significant Drug Interactions: Alterations in Dose or Regimen May Be Recommended Based on Drug Interaction Studies or Predicted Interaction [see Clinical Pharmacology (12.3) ] ↑=increase, ↓=decrease, ↔=no change * The interaction between rilpivirine and the drug was evaluated in a clinical study.

All other drug-drug interactions shown are predicted. † This interaction study has been performed with a dose higher than the recommended dose for rilpivirine assessing the maximal effect on the coadministered drug. The dosing recommendation is applicable to the recommended doses of rilpivirine once daily. Concomitant Drug Class: Drug Name Effect on Concentration of Rilpivirine or Concomitant Drug Clinical Comment Antacids: antacids (e.g., aluminum or magnesium hydroxide, calcium carbonate) ↔ rilpivirine (antacids taken at least 2 hours before or at least 4 hours after rilpivirine) ↓ rilpivirine (concomitant intake) The combination of rilpivirine and antacids should be used with caution as coadministration may cause significant decreases in rilpivirine plasma concentrations (increase in gastric pH).

Antacids should only be administered either at least 2 hours before or at least 4 hours after rilpivirine. Anticonvulsants: carbamazepine oxcarbazepine phenobarbital phenytoin ↓ rilpivirine Coadministration is contraindicated with rilpivirine [see Contraindications (4) ] . Antimycobacterials: rifampin rifapentine ↓ rilpivirine Coadministration is contraindicated with rilpivirine [see Contraindications (4) ] .

Antimycobacterials: rifabutin * ↓ rilpivirine Concomitant use of rilpivirine with rifabutin may cause a decrease in the plasma concentrations of rilpivirine (induction of CYP3A enzymes). Throughout coadministration of rilpivirine with rifabutin, the rilpivirine dose should be increased from 25 mg once daily to 50 mg once daily. When rifabutin coadministration is stopped, the rilpivirine dose should be decreased to 25 mg once daily.

Azole Antifungal Agents: fluconazole itraconazole ketoconazole *† posaconazole voriconazole ↑ rilpivirine ↓ ketoconazole Concomitant use of rilpivirine with azole antifungal agents may cause an increase in the plasma concentrations of rilpivirine (inhibition of CYP3A enzymes). No rilpivirine dose adjustment is required when rilpivirine is coadministered with azole antifungal agents. Clinically monitor for breakthrough fungal infections when azole antifungals are coadministered with rilpivirine.

Glucocorticoid (systemic): dexamethasone (more than a single-dose treatment) ↓ rilpivirine Coadministration is contraindicated with rilpivirine [see Contraindications (4) ] . H 2 -Receptor Antagonists: cimetidine famotidine *† nizatidi…

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS • Pregnancy: Total rilpivirine exposures were generally lower during pregnancy compared to the postpartum period. ( 2.5 , 8.1 , 12.3 ) Additional pediatric use information is approved for Janssen Products LP's Edurant (Rilpivirine) tablets. However, due to Janssen Products LP's marketing exclusivity rights, this drug product is not labeled with that information.

8.1Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to rilpivirine during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) 1-800-258-4263. Risk Summary Available data from the APR show no difference in the overall risk of birth defects for rilpivirine compared with the background rate for major birth defects of 2.7% in the Metropolitan Atlanta Congenital Defects Program (MACDP) reference population (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% to 20%. The background risk for major birth defects and miscarriage for the indicated population is unknown.

Methodologic limitations of the APR include the use of MACDP as the external comparator group. The MACDP population is not disease-specific, evaluates women and infants from a limited geographic area, and does not include outcomes for births that occurred at <20 weeks gestation. In a clinical trial, total rilpivirine exposures were generally lower during pregnancy compared to the postpartum period (see Data).

In animal reproduction studies, no adverse developmental outcomes were observed when rilpivirine was administered orally at exposures up to 15 (rats) and 70 (rabbits) times the exposure in humans (≥12 years of age and weighing at least 32 kg) at the recommended dose of 25 mg once daily (see Data). Clinical Considerations Dosing During Pregnancy and the Postpartum Period Based on the experience of HIV-1-infected pregnant women who completed a clinical trial through the postpartum period with a rilpivirine-based regimen, no dose adjustments are required for pregnant patients who are already on a stable rilpivirine regimen prior to pregnancy and who are virologically suppressed (HIV-1 RNA less than 50 copies per mL) [see Dosage and Administration (2.5) ].

Lower exposures of rilpivirine were observed during pregnancy, therefore viral load should be monitored closely [see Clinical Pharmacology (12.3) ]. Data Human Data Based on prospective reports to the APR of over 550 exposures to rilpivirine during the first trimester of pregnancy resulting in live births, there was no significant difference between the overall risk of birth defects with rilpivirine compared to the background birth defect rate of 2.7% in the U.S. reference population of the MACDP. The prevalence of birth defects in live births was 1.4% (95% CI: 0.6% to 2.8%) and 1.5% (95% CI: 0.3% to 4.3%) following first and second/third trimester exposure, respectively, to rilpivirine-containing regimens.

Rilpivirine in combination with a background regimen was evaluated in a clinical trial of 19 HIV-1 infected pregnant women during the second and third trimesters and postpartum. Each of the women were on a rilpivirine-based regimen at the time of enrollment. Twelve subjects completed the trial through the postpartum period (6 to 12 weeks after delivery) and pregnancy outcomes are missing for six subjects.

The exposure (C 0h and AUC) of total rilpivirine was approximately 30 to 40% lower during pregnancy compared with postpartum (6 to 12 weeks). The protein binding of rilpivirine was similar (>99%) during second trimester, third trimester, and postpartum period. One subject discontinued the trial following spontaneous termination of the pregnancy at 25 weeks gestation due to suspected premature rupture of membranes.

Among the 12 subjects who were virolo…

🤰 Pregnancy ~3 min read ▾

8.1Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to rilpivirine during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) 1-800-258-4263. Risk Summary Available data from the APR show no difference in the overall risk of birth defects for rilpivirine compared with the background rate for major birth defects of 2.7% in the Metropolitan Atlanta Congenital Defects Program (MACDP) reference population (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% to 20%. The background risk for major birth defects and miscarriage for the indicated population is unknown.

Methodologic limitations of the APR include the use of MACDP as the external comparator group. The MACDP population is not disease-specific, evaluates women and infants from a limited geographic area, and does not include outcomes for births that occurred at <20 weeks gestation. In a clinical trial, total rilpivirine exposures were generally lower during pregnancy compared to the postpartum period (see Data).

In animal reproduction studies, no adverse developmental outcomes were observed when rilpivirine was administered orally at exposures up to 15 (rats) and 70 (rabbits) times the exposure in humans (≥12 years of age and weighing at least 32 kg) at the recommended dose of 25 mg once daily (see Data). Clinical Considerations Dosing During Pregnancy and the Postpartum Period Based on the experience of HIV-1-infected pregnant women who completed a clinical trial through the postpartum period with a rilpivirine-based regimen, no dose adjustments are required for pregnant patients who are already on a stable rilpivirine regimen prior to pregnancy and who are virologically suppressed (HIV-1 RNA less than 50 copies per mL) [see Dosage and Administration (2.5) ].

Lower exposures of rilpivirine were observed during pregnancy, therefore viral load should be monitored closely [see Clinical Pharmacology (12.3) ]. Data Human Data Based on prospective reports to the APR of over 550 exposures to rilpivirine during the first trimester of pregnancy resulting in live births, there was no significant difference between the overall risk of birth defects with rilpivirine compared to the background birth defect rate of 2.7% in the U.S. reference population of the MACDP. The prevalence of birth defects in live births was 1.4% (95% CI: 0.6% to 2.8%) and 1.5% (95% CI: 0.3% to 4.3%) following first and second/third trimester exposure, respectively, to rilpivirine-containing regimens.

Rilpivirine in combination with a background regimen was evaluated in a clinical trial of 19 HIV-1 infected pregnant women during the second and third trimesters and postpartum. Each of the women were on a rilpivirine-based regimen at the time of enrollment. Twelve subjects completed the trial through the postpartum period (6 to 12 weeks after delivery) and pregnancy outcomes are missing for six subjects.

The exposure (C 0h and AUC) of total rilpivirine was approximately 30 to 40% lower during pregnancy compared with postpartum (6 to 12 weeks). The protein binding of rilpivirine was similar (>99%) during second trimester, third trimester, and postpartum period. One subject discontinued the trial following spontaneous termination of the pregnancy at 25 weeks gestation due to suspected premature rupture of membranes.

Among the 12 subjects who were virologically suppressed at baseline (less than 50 copies/mL), virologic response was preserved in 10 subjects (83.3%) through the third trimester visit and in 9 subjects (75%) through the 6 to 12 week postpartum visit. Virologic outcomes during the third trimester visit were missing for two subjects who were withdrawn (one subject was nonadherent to the study drug and one subject withdrew consent)…

🧒 Pediatric Use ~1 min read ▾

8.4Pediatric Use The safety and effectiveness of rilpivirine has been established for the treatment of HIV-1 infection in treatment-naïve pediatric patients 12 years of age and older and weighing at least 35 kg. Use of rilpivirine in this population is supported by two trials: TMC278-C213 and MOCHA. Trial TMC278-C213 TMC278-C213 was a single arm, open-label, Phase 2 trial in antiretroviral treatment-naïve HIV-1 infected pediatric subjects, and was divided into two Cohorts. - Cohort 1 evaluated the safety, efficacy and pharmacokinetics of rilpivirine and enrolled 36 children aged 12 to less than 18 years of age and weighing at least 32 kg [see Adverse Reactions (6.1) , Clinical Pharmacology (12.3) , and Clinical Studies (14.3) ].

MOCHA Trial (NCT03497676) The safety, tolerability, and pharmacokinetics of oral and injectable cabotegravir and oral and injectable rilpivirine are being assessed in an ongoing Phase 1/2 multicenter, open-label, non-comparative study, MOCHA (IMPAACT 2017) [see Adverse Reactions (6.1) ] . Refer to the VOCABRIA and CABENUVA prescribing information for additional information when rilpivirine is used in combination with cabotegravir. The safety and effectivness of rilpivirine in these pediatric subjects were similar to that seen in adults, and there were no significant changes on rilpivirine exposures [see Adverse Reactions (6.1) , Clinical Pharmacology (12.3) , and Clinical Studies (14) ].

Safety and effectiveness in pediatric patients less than 2 years of age or weighing less than 14 kg have not been established. Additional pediatric use information is approved for Janssen Products LP's Edurant (Rilpivirine) tablets. However, due to Janssen Products LP's marketing exclusivity rights, this drug product is not labeled with that information.

🧓 Geriatric Use 61 words ▾

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

🆘 Overdosage 89 words ▾

10 OVERDOSAGE There is no specific antidote for overdose with rilpivirine. Human experience of overdose with rilpivirine is limited. Treatment of overdose with rilpivirine consists of general supportive measures including monitoring of vital signs and ECG (QT interval) as well as observation of the clinical status of the patient.

It is advisable to contact a poison control center to obtain the latest recommendations for the management of an overdose. Since rilpivirine is highly bound to plasma protein, dialysis is unlikely to result in significant removal of the active substance.

🧬 Clinical Pharmacology ~3 min read ▾

12 CLINICAL PHARMACOLOGY

12.1Mechanism of Action Rilpivirine is an antiviral drug [see Microbiology (12.4) ] .

12.2Pharmacodynamics Effects on Electrocardiogram The effect of rilpivirine at the recommended dose of 25 mg once daily on the QTcF interval was evaluated in a randomized, placebo and active (moxifloxacin 400 mg once daily) controlled crossover study in 60 healthy adults, with 13 measurements over 24 hours at steady state. The maximum mean time-matched (95% upper confidence bound) differences in QTcF interval from placebo after baseline-correction was 2.0 (5.0) milliseconds (i.e., below the threshold of clinical concern).

When doses of 75 mg once daily and 300 mg once daily of rilpivirine (3 times and 12 times the dose in rilpivirine) were studied in healthy adults, the maximum mean time-matched (95% upper confidence bound) differences in QTcF interval from placebo after baseline-correction were 10.7 (15.3) and 23.3 (28.4) milliseconds, respectively. Steady-state administration of rilpivirine 75 mg once daily and 300 mg once daily resulted in a mean steady-state C max approximately 2.6-fold and 6.7-fold, respectively, higher than the mean C max observed with the recommended 25 mg once daily dose of rilpivirine [see Warnings and Precautions (5.4) ].

12.3Pharmacokinetics Pharmacokinetics in Adults The pharmacokinetic properties of rilpivirine have been evaluated in adult healthy subjects and in adult antiretroviral treatment-naïve HIV-1-infected subjects. Exposure to rilpivirine was generally lower in HIV-1 infected subjects than in healthy subjects. Table 7: Pharmacokinetic Estimates of Rilpivirine 25 mg Once Daily in Antiretroviral Treatment-Naïve HIV-1-Infected Adult Subjects (Pooled Data from Phase 3 Trials through Week 96) Parameter Rilpivirine 25 mg once daily N=679 AUC 24h (ng.h/mL) Mean±Standard Deviation 2,235±851 Median (Range) 2,096 (198 to 7,307) C 0h (ng/mL) Mean±Standard Deviation 79±35 Median (Range) 73 (2 to 288) Absorption and Bioavailability After oral administration, the maximum plasma concentration of rilpivirine is generally achieved within 4 to 5 hours.

The absolute bioavailability of rilpivirine is unknown. Effects of Food on Oral Absorption The exposure to rilpivirine was approximately 40% lower when rilpivirine was taken in a fasted condition as compared to a normal caloric meal (533 kcal) or high-fat high-caloric meal (928 kcal). When rilpivirine was taken with only a protein-rich nutritional drink, exposures were 50% lower than when taken with a meal.

Distribution Rilpivirine is approximately 99.7% bound to plasma proteins in vitro , primarily to albumin. The distribution of rilpivirine into compartments other than plasma (e.g., cerebrospinal fluid, genital tract secretions) has not been evaluated in humans. Metabolism In vitro experiments indicate that rilpivirine primarily undergoes oxidative metabolism mediated by the cytochrome P450 (CYP) 3A system .

Elimination The terminal elimination half-life of rilpivirine is approximately 50 hours. After single dose oral administration of 14 C-rilpivirine, on average 85% and 6.1% of the radioactivity could be retrieved in feces and urine, respectively. In feces, unchanged rilpivirine accounted for on average 25% of the administered dose.

Only trace amounts of unchanged rilpivirine (<1% of dose) were detected in urine. Specific Populations Pregnancy and Postpartum The exposure (C 0h and AUC 24h ) to total rilpivirine after intake of rilpivirine 25 mg once daily as part of an antiretroviral regimen was 30 to 40% lower during pregnancy (similar for the second and third trimester), compared with postpartum (see Table 8). However, the exposure during pregnancy was not significantly different from exposures obtained in Phase 3 trials.

Based on the exposure-response relationship for rilpivirine, this decrease is not considered clinically relevant in patients who are virollogically suppressed. The protein binding of rilpivirine was similar (>99%) during t…

🧬 Mechanism of Action 14 words ▾

12.1Mechanism of Action Rilpivirine is an antiviral drug [see Microbiology (12.4) ] .

📦 How Supplied / Storage and Handling 96 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING Rilpivirine Tablets Rilpivirine 25 mg tablets are supplied as white to off-white, round, biconvex film coated tablets debossed with ‘5L’ on one side and plain on the other side. Each tablet contains 27.5 mg of rilpivirine hydrochloride, which is equivalent to 25 mg of rilpivirine. HDPE bottles without Silica gel canister desiccant Bottles of 30 NDC 42385-999-30 HDPE bottles with Silica gel canister desiccant Bottles of 30 NDC 42385-999-31 Store at 20° to 25°C (68° to 77°F); excursions permitted between 15° to 30°C (59° to 86°F). [See USP Controlled Room Temperature.]

📋 Description 152 words ▾

11 DESCRIPTION Rilpivirine tablets are a non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1 (HIV-1). The chemical name for rilpivirine hydrochloride is 4-[[4-[[4-[(E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile monohydrochloride. Its molecular formula is C 22 H 18 N 6 • HCl and its molecular weight is 402.88.

Rilpivirine hydrochloride has the following structural formula: Rilpivirine hydrochloride is a white to off white solid. It is sparingly soluble in dimethylformamide and practically insoluble in water. Rilpivirine 25 mg tablets are available as a white to off-white, round, biconvex film coated tablets debossed with ‘5L’ on one side and plain on other side.

Each tablet contains 27.5 mg of rilpivirine hydrochloride, which is equivalent to 25 mg of rilpivirine. Each rilpivirine 25 mg tablet also contains the inactive ingredients croscarmellose sodium, lactose monohydrate, magnesium stearate, polysorbate 20, povidone K30 and silicified microcrystalline cellulose. The tablet coating contains hypromellose 2910, polyethylene glycol 8000 and titanium dioxide. rilpivirine-structure

💬 Information for Patients ~3 min read ▾

17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information). Severe Skin and Hypersensitivity Reactions Advise patients to immediately contact their healthcare provider if they develop a rash. Instruct patients to immediately stop taking rilpivirine and seek medical attention if they develop a rash associated with any of the following symptoms as it may be a sign of more serious reactions such as DRESS severe hypersensitivity: fever, blisters, mucosal involvement, eye inflammation (conjunctivitis), severe allergic reaction causing a swelling of the face, eyes, lips, mouth, tongue or throat, which may lead to difficulty swallowing or breathing, and any signs and symptoms of liver problems as it may be a sign of a more serious reaction.

Advise patients that if severe rash occurs, they will be closely monitored, laboratory tests will be performed and appropriate therapy will be initiated [see Warnings and Precautions (5.1) ] . Hepatotoxicity Inform patients that hepatotoxicity has been reported with rilpivirine. Inform patients that laboratory monitoring for hepatotoxicity during therapy with rilpivirine is recommended, especially for patients with underlying liver disease such as hepatitis B or C virus infection [see Warnings and Precautions (5.2) ].

Depressive Disorders Inform patients that depressive disorders (depressed mood, depression, dysphoria, major depression, mood altered, negative thoughts, suicide attempt, suicidal ideation) have been reported with rilpivirine. Advise patients to seek immediate medical evaluation if they experience depressive symptoms [see Warnings and Precautions (5.3) ]. Drug Interactions Rilpivirine 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), and Drug Interactions (7) ] . For patients concomitantly receiving rifabutin, the rilpivirine dose should be increased to 50 mg once daily, taken with a meal. When rifabutin coadministration is stopped, the rilpivirine dose should be decreased to 25 mg once daily, taken with a meal [see Dosage and Administration (2.7) ].

Immune Reconstitution Syndrome Advise patients to inform their healthcare provider immediately of any signs or symptoms of infection as inflammation from previous infection may occur soon after combination antiretroviral therapy, including when rilpivirine is started [see Warnings and Precautions (5.5) ]. Rilpivirine Tablets and EDURANT PED Tablets for Oral Suspension Are Not Substitutable Advise patients that rilpivirine tablets and EDURANT PED have differing pharmacokinetic profiles and are not substitutable on a milligram-per-milligram basis.

Advise patients or their care providers that patients switching from EDURANT PED tablets for oral suspension to rilpivirine tablets must adjust the dose [see Dosage and Administration (2.1) and Warnings and Precautions (5.6) ]. To avoid a dosing error from using the wrong formulation of rilpivirine, strongly advise patients and caregivers to visually inspect the tablets to verify the correct formulation each time the prescription is filled [see Dosage and Administration (2), Warnings and Precautions (5.6) , and How Supplied/Storage and Handling (16) ].

Administration Instructions Advise patients to take rilpivirine with a meal once a day as prescribed. A protein drink or yogurt alone does not replace a meal [see Clinical Pharmacology (12.3) ] . Rilpivirine must always be used in combination with other antiretroviral drugs.

Advise patients not to alter the dose of rilpivirine or discontinue therapy without consulting their physician. If the patient misses a dose of rilpivirine within 12 hours of the time it is usually taken, advise the patient to take rilpivirine with a meal as soon as possible and then take the next dose of ri…

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