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Maraviroc 300 mg Tablet, Film Coated, 60-count — NDC 72865-232-60 (Billing 72865-0232-60)

by XLCare Pharmaceuticals Inc. · 60 TABLET, FILM COATED in 1 BOTTLE

This is a package of 60 tablets of Maraviroc 300 mg Tablet, Film Coated from XLCare Pharmaceuticals Inc., marketed since Jun 2023 and currently FDA-listed. It is this product's only package size.

NDC 72865-0232-60
🏷️ FDA NDC (as labeled) 72865-232-60 billing pads the product segment with a zero
Rx only Generic 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 →

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

Identity & classification

Regulatory identifiers FDA, NLM and CMS codes for this package

FDA NDC (as labeled) 72865-232-60
Product NDC 72865-232
11-digit billing NDC 72865023260
NCPDP billing unit EA — each (per item)
RxCUI 728223, 728225
UNII MD6P741W8A
Application # ANDA203347
SPL Set ID d3a728e2-1866-462e-bfcc-5f3c9dd88794
Established class (EPC) CCR5 Co-receptor Antagonist
Mechanism of action Chemokine Co-receptor 5 Antagonists
DEA schedule Non-controlled
Marketing category ANDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2023-06-01
Route ORAL
Dosage form TABLET, FILM COATED
Substance MARAVIROC
TE code (Orange Book) AB · RLD · RS

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

GPI-14 12102060000330
GCN Seq No 062979
GCN 98739
HICL code 034927
Ingredient (HICL) Maraviroc
HIC1 code W
Therapeutic class — broad (HIC1) Anti-Infecting Agents
HIC2 code W5
Therapeutic class — intermediate (HIC2) Antiviral Agents
HIC3 code W5T
Therapeutic class — specific (HIC3) Antivirals, Hiv-Specific, Ccr5 Co-Receptor Antag.
AHFS code 08:18.08.04
AHFS class Hiv Entry And Fusion Inhibitors
FDB label name MARAVIROC 300 MG TABLET
FDB brand name Maraviroc
Legend status F — Federal legend — prescription drug or device
Quick answers
  • GSN (GCN sequence number): 062979
  • GCN: 98739
  • GPI-14 (Medi-Span): 12102060000330
  • HICL (First Databank): 034927
  • AHFS class code: 08:18.08.04
  • RxCUI (RxNorm): 728223
Why two NDCs? The FDA registers this code as 72865-232-60 — 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 → 72865-0232-60. 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 CCR5 Co-receptor Antagonist class.

Pharmacologic class CCR5 Co-receptor Antagonist
Drug family (ATC) Other antivirals
How it works Chemokine Co-receptor 5 Antagonists
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 MARAVIROC 300 MG TABLET Ingredient Maraviroc
📗 Our plain-language guide HelloPharmacist
  • Maraviroc is not a cure for HIV. It's an antiviral medication that helps control CCR5-tropic HIV-1 by blocking the virus from entering your immune cells. When taken consistently as...
  • What exactly is maraviroc treating — is it a cure for HIV?
  • Maraviroc only works against one specific type of HIV called CCR5-tropic HIV-1. Some people have a strain that uses a different receptor (CXCR4-tropic) or one that uses both — and...
  • Why do I need a test before I can even start this medication?
📖 Read our full Maraviroc 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 $17.26 $1,035.74 / 60 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
72865-0232-60 You're viewing this Main listing 60 TABLET, FILM COATED in 1 BOTTLE 2023-06-01 — Active

Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Maraviroc 300 mg 31722-0580-60 Camber 60 tablets $6.339 AB Availability likely —
Maraviroc 300 mg 70710-1931-06 Zydus 60 tablets $6.339 AB Availability likely —
Maraviroc 300 mg 72319-0025-02 i3 60 tablets $6.339 AB Availability likely —
Selzentry 300 mg 49702-0224-18 ViiV 60 tablets $28.131 AB Availability likely —
Maraviroc 300 mg 68475-0007-01 Navinta 60 tablets — AB FDA listed —
Maraviroc 300 mg 68554-3080-00 Hetero 60 tablets — AB Discontinued —
Maraviroc 300 mgthis 72865-0232-60 XLCare 60 tablets — AB FDA listed —
Maraviroc 300 mg 73141-0025-02 A2A 60 tablets — AB FDA listed —
Maraviroc 300 mg 50090-8005-00 A-S 60 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

🏛️
2023
On the market since
Jun 2023
📍
2026
Currently FDA-listed
3 years listed
🔓
·
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.

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 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 1DI56QDM62
    A natural fatty substance from soybeans that helps mix oil and water-based ingredients together. It acts as an emulsifier and lubricant in medicines to improve texture and help the product break down properly in your 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 3WJQ0SDW1A
    Polyethylene glycol is a synthetic liquid or solid polymer used in medicines as a solvent, lubricant, and humectant. It helps dissolve active ingredients, reduces friction during manufacturing, and retains moisture in the final product.
  • 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 5856J3G2A2
    A starch-based powder made from potatoes and processed with sodium. It acts as a disintegrant, helping the tablet or capsule break apart quickly in the stomach so the medicine can be absorbed.
  • 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.

10 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

LabelerXLCare Pharmaceuticals Inc.
Application holderHETERO LABS LTD UNIT III
FDA applicationANDA203347 (ANDA)
Labeler code72865
First marketedJun 2023
Product typeHuman Prescription Drug
Portfolio67 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.

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.
🚨 Boxed Warning 🎯 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 🍼 Nursing Mothers 🧬 Pharmacokinetics 🧬 Pharmacodynamics 🔬 Clinical Studies 🔒 Drug Abuse and Dependence 🔒 Controlled Substance 🧪 Nonclinical Toxicology 📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 📚 References 📄 Package Label / Principal Display Panel
🚨 Boxed Warning 118 words ▾

WARNING: HEPATIC TOXICITY WARNING: HEPATOTOXICITY Hepatotoxicity has been reported with use of maraviroc tablets. Severe rash or evidence of a systemic allergic reaction (e.g., fever, eosinophilia, or elevated IgE) prior to the development of hepatotoxicity may occur. Patients with signs or symptoms of hepatitis or allergic reaction following use of maraviroc tablets should be evaluated immediately [see Warnings and Precautions ( 5.1 )].

WARNING: HEPATOTOXICITY See full prescribing information for complete boxed warning. • Hepatotoxicity has been reported which may be preceded by severe rash or other features of a systemic allergic reaction (e.g., fever, eosinophilia, or elevated IgE). ( 5.1 ) • Immediately evaluate patients with signs or symptoms of hepatitis or allergic reaction. ( 5.1 )

🎯 Indications and Usage 121 words ▾

1 INDICATIONS AND USAGE Maraviroc tablets are indicated in combination with other antiretroviral agents for the treatment of only CCR5-tropic human immunodeficiency virus type 1 (HIV-1) infection in adult and pediatric patients 2 years of age and older weighing at least 10 kg. Limitations of Use: • Maraviroc tablets are not recommended in patients with dual/mixed- or CXCR4-tropic HIV-1 [see Microbiology ( 12.4 )]. Maraviroc tablet is a CCR5 co-receptor antagonist indicated in combination with other antiretroviral agents for the treatment of only CCR5-tropic HIV-1 infection in adults and pediatric patients 2 years of age and older weighing at least 10 kg.

( 1 ) Limitations of Use: • Not recommended in patients with dual/mixed- or CXCR4-tropic HIV-1. ( 1 )

⏱️ Dosage and Administration ~3 min read ▾

2 DOSAGE AND ADMINISTRATION • Prior to initiation of maraviroc tablets for treatment of HIV-1 infection, test all patients for CCR5 tropism using a highly sensitive tropism assay. ( 2.1 ) • Maraviroc tablets are taken twice daily by mouth and may be taken with or without food. Maraviroc tablets must be given in combination with other antiretroviral medications.

( 2.2 ) Recommended Dosage in Adult Patients: ( 2.3 ) Concomitant Medications Dosage of Maraviroc tablets When given with potent cytochrome P450 (CYP)3A inhibitors (with or without potent CYP3A inducers) including PIs (except tipranavir/ritonavir) ( 2.3 , 7.1 ) 150 mg twice daily With NRTIs, tipranavir/ritonavir, nevirapine, raltegravir, and other drugs that are not potent CYP3A inhibitors or CYP3A inducers ( 2.3 , 7.1 ) 300 mg twice daily With potent and moderate CYP3A inducers including efavirenz (without a potent CYP3A inhibitor) ( 2.3 , 7.1 ) 600 mg twice daily A more complete list of coadministered drugs is listed in Dosage and Administration.

( 2 ) Recommended Dosage in Pediatric Patients 2 years and older and weighing at Least 10 kg: Administer twice daily. Dosage should be based on body weight (kg) and concomitant medications and should not exceed the recommended adult dose. ( 2.4 ) Recommended Dosage in Patients with Renal Impairment: Dose adjustment may be necessary in adult patients with renal impairment.

( 2.5 )

2.1Testing prior to Initiation of Maraviroc Tablets Prior to initiation of maraviroc tablets for treatment of HIV-1 infection, test all patients for CCR5 tropism using a highly sensitive tropism assay. Maraviroc tablets are recommended for patients with only CCR5-tropic HIV-1 infection. Outgrowth of pre-existing low-level CXCR4- or dual/mixed-tropic HIV-1 not detected by tropism testing at screening has been associated with virologic failure on maraviroc tablets [ see Microbiology ( 12.4 ), Clinical Studies ( 14.1 ) ].

Monitor patients for ALT, AST, and bilirubin prior to initiation of maraviroc tablets and at other time points during treatment as clinically indicated [see Warnings and Precautions ( 5.1 )].

2.2General Dosing Recommendations • Maraviroc tablets are taken twice daily by mouth and may be taken with or without food. • Maraviroc tablets must be given in combination with other antiretroviral medications. • The recommended dosage of maraviroc tablets differs based on concomitant medications due to drug interactions.

2.3Recommended Dosage in Adult Patients with Normal Renal Function Table 1 displays oral dosage of maraviroc tablets based on different concomitant medications [see Drug Interactions ( 7.1 )]. Table 1. Recommended Dosage in Adults Concomitant Medications Dosage of Maraviroc Tablets Potent cytochrome P450 (CYP)3A inhibitors (with or without a potent CYP3A inducer) a 150 mg twice daily Noninteracting concomitant medications b 300 mg twice daily Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor) c 600 mg twice daily a Potent CYP3A inhibitors (with or without a potent CYP3A inducer) including: clarithromycin, cobicistat, elvitegravir/ritonavir, itraconazole, ketoconazole, nefazodone, protease inhibitors (except tipranavir/ritonavir), telithromycin. b Noninteracting concomitant medications include all medications that are not potent CYP3A inhibitors or inducers such as: dolutegravir, enfuvirtide, nevirapine, all nucleoside reverse transcriptase inhibitors (NRTIs), raltegravir, and tipranavir/ritonavir. c Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor) including: carbamazepine, efavirenz, etravirine, phenobarbital, phenytoin, and rifampin.

2.4Recommended Dosage in Pediatric Patients with Normal Renal Function The recommended dosage of maraviroc tablets should be based on body weight (kg) and should not exceed the recommended adult dose. The recommended dosage also differs based on concomitant medications due to drug interactions (Table 2 and Table 3) [see Drug Interactions ( 7.1 ), Use in S… [Excerpted — this section continues on DailyMed.]

💊 Dosage Forms and Strengths 62 words ▾

3 DOSAGE FORMS AND STRENGTHS • 150 mg white to off-white colored, oval, biconvex, film coated tablets debossed with ‘J’ on one side and ‘62’ on the other side. • 300 mg white to off-white colored, oval, biconvex, film coated tablets debossed with ‘J’ on one side and ‘63’ on the other side. Tablets: 150 mg and 300 mg ( 3 )

⛔ Contraindications 72 words ▾

4 CONTRAINDICATIONS Maraviroc tablets are contraindicated in patients with severe renal impairment or ESRD (CrCl less than 30 mL per minute) who are concomitantly taking potent CYP3A inhibitors or inducers [see Warnings and Precautions ( 5.3 )]. • Maraviroc tablets are contraindicated in patients with severe renal impairment or end-stage renal disease (ESRD) (CrCl less than 30 mL per minute) who are concomitantly taking potent CYP3A inhibitors or inducers. ( 4 )

⚠️ Warnings and Cautions ~3 min read ▾

5 WARNINGS AND PRECAUTIONS • Hepatotoxicity accompanied by severe rash or systemic allergic reaction, including potentially life-threatening events, has been reported. Hepatic laboratory parameters including ALT, AST, and bilirubin should be obtained prior to starting maraviroc tablets and at other time points during treatment as clinically indicated. If rash or symptoms or signs of hepatitis or allergic reaction develop, hepatic laboratory parameters should be monitored and discontinuation of treatment should be considered.

When administering maraviroc tablets to patients with pre-existing liver dysfunction or who are co-infected with hepatitis B and/or C virus, additional monitoring may be warranted. ( 5.1 ) • Severe and potentially life-threatening skin and hypersensitivity reactions have been reported in patients taking maraviroc. This includes cases of Stevens-Johnson syndrome, hypersensitivity reaction, and toxic epidermal necrolysis.

Immediately discontinue maraviroc and other suspected agents if signs or symptoms of severe skin or hypersensitivity reactions develop and monitor clinical status, including liver aminotransferases, closely. ( 5.2 ) • More cardiovascular events, including myocardial ischemia and/or infarction, were observed in treatment-experienced subjects who received maraviroc. Additional monitoring may be warranted.

( 5.3 ) • If patients with severe renal impairment or ESRD receiving maraviroc (without concomitant CYP3A inducers or inhibitors) experience postural hypotension, the dose of maraviroc should be reduced from 300 mg twice daily to 150 mg twice daily. ( 5.3 )

5.1Hepatotoxicity Hepatotoxicity with allergic features including life-threatening events has been reported in clinical trials and postmarketing. Severe rash or evidence of systemic allergic reaction including drug-related rash with fever, eosinophilia, elevated IgE, or other systemic symptoms have been reported in conjunction with hepatotoxicity [see Warnings and Precautions ( 5.2 )]. These events occurred approximately 1 month after starting treatment.

Among reported cases of hepatitis, some were observed in the absence of allergic features or with no pre-existing hepatic disease. Appropriate laboratory testing including ALT, AST, and bilirubin should be conducted prior to initiating therapy with maraviroc and at other time points during treatment as clinically indicated. Hepatic laboratory parameters should be obtained in any patient who develops rash, or signs or symptoms of hepatitis, or allergic reaction.

Discontinuation of maraviroc should be considered in any patient with signs or symptoms of hepatitis, or with increased liver transaminases combined with rash or other systemic symptoms. When administering maraviroc to patients with pre-existing liver dysfunction or who are co-infected with hepatitis B and/or C virus, additional monitoring may be warranted. The safety and efficacy of maraviroc have not been specifically studied in patients with significant underlying liver disorders.

5.2Severe Skin and Hypersensitivity Reactions Severe, potentially life-threatening skin and hypersensitivity reactions have been reported in patients taking maraviroc, in most cases concomitantly with other drugs associated with these reactions. These include cases of Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), and drug rash with eosinophilia and systemic symptoms (DRESS) [ see Adverse Reactions (6.3) ]. The cases were characterized by features including rash, constitutional findings, and sometimes organ dysfunction, including hepatic failure.

Discontinue maraviroc and other suspected agents immediately if signs or symptoms of severe skin or hypersensitivity reactions develop (including, but not limited to, severe rash or rash accompanied by fever, malaise, muscle or joint aches, blisters, oral lesions, conjunctivitis, facial edema, lip swelling, eosinophilia). Delay in stopping treatment with maraviroc or other suspect drugs af… [Excerpted — this section continues on DailyMed.]

🤒 Adverse Reactions ~3 min read ▾

6 ADVERSE REACTIONS The following adverse reactions are discussed in other sections of the labeling: • Hepatotoxicity [see Boxed Warning, Warnings and Precautions ( 5.1 )] • Severe Skin and Hypersensitivity Reactions [see Warnings and Precautions ( 5.2 )] • Cardiovascular Events [see Warnings and Precautions ( 5.3 )] • The most common adverse events in treatment-experienced adult subjects (greater than 8% incidence) which occurred at a higher frequency compared with placebo are upper respiratory tract infections, cough, pyrexia, rash, and dizziness.

( 6.1 ) • The most common adverse events in treatment-naive adult subjects (greater than 8% incidence) which occurred at a higher frequency than the comparator arm are upper respiratory tract infections, bronchitis, flatulence, bloating and distention, upper respiratory tract signs and symptoms, and gastrointestinal atonic and hypomotility disorders. ( 6.1 ) • The most common adverse reactions in treatment-experienced pediatric subjects (greater than or equal to 3% incidence) are vomiting, abdominal pain, diarrhea, nausea, and dizziness.

( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact XLCare Pharmaceuticals, Inc. at 1-866-495-1995 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 with rates in the clinical trials of another drug and may not reflect the rates observed in practice. Clinical Trials Experience in Adult Subjects Treatment-Experienced Subjects: The safety profile of maraviroc is primarily based on 840 HIV-1-infected subjects who received at least 1 dose of maraviroc during two Phase 3 trials.

A total of 426 of these subjects received the indicated twice-daily dosing regimen. Assessment of treatment-emergent adverse events is based on the pooled data from 2 trials in subjects with CCR5-tropic HIV-1 (A4001027 and A4001028). The median duration of therapy with maraviroc for subjects in these trials was 48 weeks, with the total exposure on maraviroc twice daily at 309 patient-years versus 111 patient-years on placebo each administered with optimized background therapy (OBT).

The population was 89% male and 84% white, with mean age of 46 years (range: 17 to 75 years). Subjects received dose equivalents of 300 mg maraviroc once or twice daily. The most common adverse events reported with twice-daily therapy with maraviroc with frequency rates higher than placebo, regardless of causality, were upper respiratory tract infections, cough, pyrexia, rash, and dizziness.

In these 2 trials, the rate of discontinuation due to adverse events was 5% for subjects who received maraviroc twice daily + OBT as well as those who received placebo + OBT. Most of the adverse events reported were judged to be mild to moderate in severity. The data described below occurred with twice-daily dosing of maraviroc.

The total numbers of subjects reporting infections were 233 (55%) and 84 (40%) in the group receiving maraviroc twice daily and the placebo group, respectively. Correcting for the longer duration of exposure on maraviroc compared with placebo, the exposure-adjusted frequency (rate per 100 subject-years) of these events was 133 for both maraviroc twice daily and placebo. Dizziness or postural dizziness occurred in 8% of subjects on either maraviroc or placebo, with 2 subjects (0.5%) on maraviroc permanently discontinuing therapy (1 due to syncope, 1 due to orthostatic hypotension) versus 1 subject on placebo (0.5%) permanently discontinuing therapy due to dizziness.

Treatment-emergent adverse events, regardless of causality, from Trials A4001027 and A4001028 are summarized in Table 5. Selected events occurring at greater than or equal to 2% of subjects and at a numerically higher rate in subjects treated with maraviroc are included; events that occurred at the same or higher rate on placebo are… [Excerpted — this section continues on DailyMed.]

🔄 Drug Interactions 199 words ▾

7 DRUG INTERACTIONS • Coadministration with CYP3A inhibitors, including protease inhibitors (except tipranavir/ritonavir), will increase the concentration of maraviroc. ( 7.1 ) • Coadministration with CYP3A inducers, including efavirenz, may decrease the concentration of maraviroc. ( 7.1 ) • Coadministration with St. John’s wort is not recommended. ( 7.1 ).

7.1Effect of Concomitant Drugs on the Pharmacokinetics of Maraviroc Maraviroc is metabolized by CYP3A and is also a substrate for P-glycoprotein (P-gp), organic anion-transporting polypeptide (OATP)1B1, and multidrug resistance-associated protein (MRP)2. The pharmacokinetics of maraviroc are likely to be modulated by inhibitors and inducers of CYP3A and P-gp and may be modulated by inhibitors of OATP1B1 and MRP2. Therefore, a dosage adjustment may be required when maraviroc is coadministered with those drugs [see Dosage and Administration ( 2.3 , 2.4 )].

Concomitant use of maraviroc and St. John's wort ( Hypericum perforatum ) or products containing St. John's wort is not recommended.

Coadministration of maraviroc with St. John's wort is expected to substantially decrease maraviroc concentrations and may result in suboptimal levels of maraviroc and lead to loss of virologic response and possible resistance to maraviroc. Additional drug interaction information is available [see Clinical Pharmacology ( 12.3 )].

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS • Lactation: Women infected with HIV should be instructed not to breastfeed due to the potential for HIV transmission. ( 8.2 )

8.1Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to maraviroc during pregnancy. Physicians are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263. Risk Summary Limited data on the use of maraviroc during pregnancy from the APR and case reports are not sufficient to inform a drug-associated risk of birth defects and miscarriage.

In animal reproduction studies, no evidence of adverse developmental outcomes was observed with maraviroc. During organogenesis in the rat and rabbit, systemic exposures (AUC) to maraviroc were approximately 20 times (rats) and 5 times (rabbits) the exposure in humans at the recommended 300-mg twice-daily dose. In the rat pre- and post-natal development study, maternal systemic exposure (AUC) to maraviroc was approximately 14 times the exposure in humans at the recommended 300-mg twice-daily dose (see Data).

The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

Data Animal Data: Maraviroc was administered orally to pregnant rats (up to 1,000 mg per kg per day) and rabbits (up to 75 mg per kg per day) on gestation Days 6 to 17 and 7 to 19, respectively. No adverse effects on embryo-fetal development were observed at these dose levels, resulting in exposures (AUC) approximately 20 times (rats) and 5 times (rabbits) higher than human exposures at the recommended daily dose. In the rat pre- and post-natal development study, maraviroc was administered orally at up to 1,000 mg per kg per day on gestation Day 6 to lactation/post-partum Day 20, with development of the offspring (including fertility and reproductive performance) unaffected by maternal administration of maraviroc at an exposure (AUC) approximately 14 times higher than human exposure at the recommended daily dose.

8.2Lactation Risk Summary The Centers for Disease Control and Prevention recommend that HIV-1–infected mothers in the United States not breastfeed their infants to avoid risking postnatal transmission of HIV-1 infection. There are no data on the presence of maraviroc in human milk, the effects on the breastfed infant, or the effects on milk production. When administered to lactating rats, maraviroc was present in milk (see Data) .

Because of the potential for (1) HIV transmission (in HIV-negative infants), (2) developing viral resistance (in HIV-positive infants), and (3) serious adverse reactions in a breastfed infant similar to those seen in adults, instruct mothers not to breastfeed if they are receiving maraviroc. Data Maraviroc (and related metabolites) was excreted into the milk of lactating rats following a single oral dose of maraviroc (100 mg per kg) on lactation Day 12, with a maximal milk concentration achieved one hour post-administration at a milk concentration approximately 2.5 times that of maternal plasma concentrations.

8.3 Nursing Mothers

8.4Pediatric Use The safety and efficacy of maraviroc have been established in pediatric patients aged from aged 2 to less than 18 years. The use of maraviroc in pediatric patients was supported by pharmacokinetic and safety data described below and by previous demonstration of efficacy in adult patients [see Indications and Usage (1)], Dosage and Administration ( 2.4 )] . HIV-1–Infected Pediatric Patients Aged 2 to Less Than 18 Years : The safety, pharmacokinetic profile, and antiviral activity of maraviroc were evaluated in treatment-experienced, CCR5- tropic, HIV-1–infected… [Excerpted — this section continues on DailyMed.]

🤰 Pregnancy ~2 min read ▾

8.1Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to maraviroc during pregnancy. Physicians are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263. Risk Summary Limited data on the use of maraviroc during pregnancy from the APR and case reports are not sufficient to inform a drug-associated risk of birth defects and miscarriage.

In animal reproduction studies, no evidence of adverse developmental outcomes was observed with maraviroc. During organogenesis in the rat and rabbit, systemic exposures (AUC) to maraviroc were approximately 20 times (rats) and 5 times (rabbits) the exposure in humans at the recommended 300-mg twice-daily dose. In the rat pre- and post-natal development study, maternal systemic exposure (AUC) to maraviroc was approximately 14 times the exposure in humans at the recommended 300-mg twice-daily dose (see Data).

The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

Data Animal Data: Maraviroc was administered orally to pregnant rats (up to 1,000 mg per kg per day) and rabbits (up to 75 mg per kg per day) on gestation Days 6 to 17 and 7 to 19, respectively. No adverse effects on embryo-fetal development were observed at these dose levels, resulting in exposures (AUC) approximately 20 times (rats) and 5 times (rabbits) higher than human exposures at the recommended daily dose. In the rat pre- and post-natal development study, maraviroc was administered orally at up to 1,000 mg per kg per day on gestation Day 6 to lactation/post-partum Day 20, with development of the offspring (including fertility and reproductive performance) unaffected by maternal administration of maraviroc at an exposure (AUC) approximately 14 times higher than human exposure at the recommended daily dose.

🧒 Pediatric Use ~1 min read ▾

8.4Pediatric Use The safety and efficacy of maraviroc have been established in pediatric patients aged from aged 2 to less than 18 years. The use of maraviroc in pediatric patients was supported by pharmacokinetic and safety data described below and by previous demonstration of efficacy in adult patients [see Indications and Usage (1)], Dosage and Administration ( 2.4 )] . HIV-1–Infected Pediatric Patients Aged 2 to Less Than 18 Years : The safety, pharmacokinetic profile, and antiviral activity of maraviroc were evaluated in treatment-experienced, CCR5- tropic, HIV-1–infected pediatric subjects aged 2 to less than 18 years weighing at least 10 kg in an open-label, multicenter clinical trial, A4001031 [see Adverse Reactions ( 6.1 ), Clinical Studies ( 14.2 )].

Pharmacokinetics were evaluated in a total of 98 pediatric subjects: 85 subjects received maraviroc and concomitant medications that included potent CYP3A inhibitors with or without potent CYP3A inducers, 10 subjects received maraviroc and noninteracting medications (not containing potent CYP3A inhibitors or potent CYP3A inducers), and three subjects received maraviroc and medications that included potent CYP3A inducers without potent CYP3A inhibitors [see Clinical Pharmacology ( 12.3 )]. There are insufficient data to make dosing recommendations for use of maraviroc in pediatric patients concomitantly receiving potent CYP3A inhibitors and weighing less than 10 kg, or in any pediatric patients concomitantly receiving potent CYP3A inducers without a potent CYP3A inhibitor [see Dosage and Administration ( 2.4 , 2.5 )].

Maraviroc is not recommended in pediatric patients weighing less than 10 kg.

🧓 Geriatric Use 56 words ▾

8.5Geriatric Use There were insufficient numbers of subjects aged 65 and over in the clinical trials to determine whether they respond differently from younger subjects. In general, caution should be exercised when administering maraviroc in elderly patients, also reflecting the greater frequency of decreased hepatic and renal function, of concomitant disease and other drug therapies.

🆘 Overdosage 209 words ▾

10 OVERDOSAGE The highest single dose administered in clinical trials was 1,200 mg. The dose-limiting adverse event was postural hypotension, which was observed at 600 mg. While the recommended dose for maraviroc in patients receiving a CYP3A inducer without a CYP3A inhibitor is 600 mg twice daily, this dose is appropriate due to enhanced metabolism.

Prolongation of the QT interval was seen in dogs and monkeys at plasma concentrations 6 and 12 times, respectively, those expected in humans at the intended exposure of 300-mg equivalents twice daily. However, no significant QT prolongation was seen in the trials in treatment-experienced subjects with HIV using the recommended doses of maraviroc, or in a specific pharmacokinetic trial to evaluate the potential of maraviroc to prolong the QT interval [ see Clinical Pharmacology ( 12.2 ) ]. There is no specific antidote for overdose with maraviroc.

Treatment of overdose should consist of general supportive measures including keeping the patient in a supine position, careful assessment of patient vital signs, blood pressure, and ECG. Administration of activated charcoal may also be used to aid in removal of unabsorbed drug. Hemodialysis had a minimal effect on maraviroc clearance and exposure in a trial in subjects with ESRD [ see Clinical Pharmacology ( 12.3 ) ].

🧬 Clinical Pharmacology ~3 min read ▾

12 CLINICAL PHARMACOLOGY

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

12.2Pharmacodynamics Exposure-Response Relationship in Treatment-Experienced Adult Subjects The relationship between maraviroc, modeled plasma trough concentration (C min ) (1 to 9 samples per subject taken on up to 7 visits), and virologic response was evaluated in 973 treatment-experienced HIV-1-infected subjects with varied optimized background antiretroviral regimens in Trials A4001027 and A4001028. The C min , baseline viral load, baseline CD4+ cell count, and overall sensitivity score (OSS) were found to be important predictors of virologic success (defined as viral load less than 400 copies per mL at 24 weeks).

Table 9 illustrates the proportions of subjects with virologic success (%) within each C min quartile for 150-mg twice-daily and 300-mg twice-daily groups. Table 9. Treatment-Experienced Subjects with Virologic Success by Cmin Quartile (Q1 to Q4) 150 mg Twice Daily (with CYP3A Inhibitors) 300 mg Twice Daily (without CYP3A Inhibitors) n Median C min % Subjects with Virologic Success n Median C min % Subjects with Virologic Success Placebo 160 - 30.6 35 -

28.6Q1 78 33 52.6 22 13

50.0Q2 77 87 63.6 22 29

68.2Q3 78 166 78.2 22 46

63.6Q4 78 279 74.4 22 97

68.2Exposure-Response Relationship in Treatment-Naive Adult Subjects The relationship between maraviroc, modeled plasma trough concentration (C min ) (1 to 12 samples per subject taken on up to 8 visits), and virologic response was evaluated in 294 treatment-naive HIV-1-infected subjects receiving maraviroc 300 mg twice daily in combination with lamivudine/zidovudine in Trial A4001026. Table 10 illustrates the proportion (%) of subjects with virologic success less than 50 copies per mL at 48 weeks within each C min quartile for the 300-mg twice-daily dose.

Table 10. Treatment-Naive Subjects with Virologic Success by C min Quartile (Q1 to Q4) 300 mg Twice Daily n Median C min % Subjects with Virologic Success Q1 75 23

57.3 Q2 72 39

72.2 Q3 73 56

74.0 Q4 74 81

83.8Eighteen of 75 (24%) subjects in Q1 had no measurable maraviroc concentration on at least one occasion versus 1 of 73 and 1 of 74 in Q3 and Q4, respectively. Effects on Electrocardiogram A placebo-controlled, randomized, crossover trial to evaluate the effect on the QT interval of healthy male and female volunteers was conducted with 3 single oral doses of maraviroc and moxifloxacin. The placebo-adjusted mean maximum (upper 1-sided 95% CI) increases in QTc from baseline after 100, 300, and 900 mg of maraviroc were -2 (0), -1 (1), and 1 (3) msec, respectively, and 13 (15) msec for moxifloxacin 400 mg.

No subject in any group had an increase in QTc of greater than or equal to 60 msec from baseline. No subject experienced an interval exceeding the potentially clinically relevant threshold of 500 msec.

12.3Pharmacokinetics Table 11. Mean Maraviroc Pharmacokinetic Parameters in Adults Patient Population Maraviroc Dose n AUC 12 (ng.h/mL) C max (ng/mL) C min (ng/mL) Healthy volunteers (Phase 1) 300 mg twice daily 64 2,908 888

43.1 Asymptomatic HIV subjects (Phase 2a) 300 mg twice daily 8 2,550 618

33.6Treatment-experienced HIV subjects (Phase 3)a 300 mg twice daily 94 1,513 266 37.2 150 mg twice daily (+ CYP3A inhibitor) 375 2,463 332 101 Treatment-naiveHIV subjects (Phase 2b/3)a 300 mg twice daily 344 1,865 287 60 a The estimated exposure is lower compared with other trials possibly due to sparse sampling, food effect, compliance, and concomitant medications. Absorption Peak maraviroc plasma concentrations are attained 0.5 to 4 hours following single oral doses of 1 to1,200 mg administered to uninfected volunteers.

The pharmacokinetics of oral maraviroc are not dose proportional over the dose range. The absolute bioavailability of a 100-mg dose is 23% and is predicted to be 33% at 300 mg. Maraviroc is a substrate for the efflux transporter P-gp.

Effect of Food on Oral Absorption: Coadministr… [Excerpted — this section continues on DailyMed.]

🧬 Mechanism of Action 17 words ▾

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

📦 How Supplied / Storage and Handling 89 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING Maraviroc film-coated tablets are available as follows: 150 mg white to off-white colored, oval, biconvex, film coated tablets debossed with 'J' on one side and '62' on the other side. Bottle of 60 tablets (NDC 72865-231-60 ) 300 mg white to off-white colored, oval, biconvex, film coated tablets debossed with 'J' on one side and '63' on the other side. Bottle of 60 tablets (NDC 72865-232-60) Maraviroc film-coated tablets should be stored at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]

📋 Description 130 words ▾

11 DESCRIPTION Maraviroc is a selective, slowly reversible, small molecule antagonist of the interaction between human CCR5 and HIV-1 gp120. Blocking this interaction prevents CCR5-tropic HIV-1 entry into cells. Maraviroc is available as film-coated tablets for oral administration containing either 150 or 300 mg of maraviroc and the following inactive ingredients: colloidal silicon dioxide, lactose monohydrate, magnesium stearate, microcrystalline cellulose, sodium starch glycolate.

The tablets are coated with, Opadry II White contains lecithin, polyethylene glycol, polyvinyl alcohol, talc and titanium dioxide. Maraviroc is chemically described as 4,4-Difluoro-N-[(1S)-3-[(3-exo)-3-[3-methyl-5- (1-methylethyl)-4H-1,2,4-triazol-4-yl]-8-azabicyclo[3.2.1]oct-8-yl]-1-phenylpropyl]-cyclohexane carboxamide. The molecular formula is C 29 H 41 F 2 N 5 O and the structural formula is: Maraviroc is a white to pale colored powder with a molecular weight of 513.67.

It is freely soluble in methanol and hygroscopic. maraviroctabletstructure

💬 Information for Patients ~2 min read ▾

17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Medication Guide). Hepatotoxicity Inform patients that hepatotoxicity, including life-threatening cases, has been reported with maraviroc tablets; therefore, it is important to inform the healthcare professional if patients have underlying hepatitis B or C or elevations in liver-associated tests prior to treatment. Inform patients to stop maraviroc tablets and seek medical evaluation immediately if they develop signs or symptoms of hepatitis or allergic reaction following use of maraviroc tablets.

Advise patients that laboratory tests for liver enzymes and bilirubin will be ordered prior to starting maraviroc tablets, at other times during treatment, and if they develop severe rash or signs and symptoms of hepatitis or an allergic reaction on treatment [ see Dosage and Administration ( 2.1 ), Warnings and Precautions ( 5.1 , 5.2 ) ]. Cardiovascular Events When administering maraviroc tablets in patients with cardiovascular comorbidities, a history of postural hypotension or receiving concomitant medication known to lower blood pressure, advise patients that they may be at increased risk for cardiovascular events.

Advise patients to avoid driving or operating machinery if they experience dizziness while taking maraviroc tablets [ see Warnings and Precautions ( 5.3 ) ]. Drug Interactions Advise patients to inform their healthcare provider of concomitant HIV medications as dosage of maraviroc tablets may be modified depending on other HIV medications taken with maraviroc tablets. Advise patients that coadministration of maraviroc tablets with St.

John’s wort is not recommended as it can lead to loss of virologic response and possible resistance to maraviroc tablets [ see Dosage and Administration ( 2.2 ), Drug Interactions ( 7.1 ) ]. Missed Dosage Inform patients that it is important to take maraviroc tablets in combination with other antiretroviral medications on a regular dosing schedule with or without food. Advise patients to avoid missing doses as it can result in development of resistance.

Instruct patients that if they miss a dose, to take it as soon as they remember. Advise patients not to double their next dose or take more than the prescribed dose [ see Dosage and Administration ( 2.2 ) ]. Pregnancy Inform patients that there is insufficient data on the safety of maraviroc tablets in pregnancy.

Inform patients that there is an antiretroviral pregnancy registry that monitors pregnancy outcomes in women exposed to maraviroc tablets during pregnancy [ 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 ) ]. The brands listed are trademarks of their respective owners and are not trademarks of XLCare Pharmaceuticals, Inc.

Manufactured for: XLCare Pharmaceuticals, Inc. 242 South Culver Street, Suite 202 Lawrenceville, GA 30046. Manufactured by: Evaric Pharmaceuticals Inc.

155 Commerce Drive, Hauppauge, New York 11788, United States (USA). Issued: 05/2023

🍼 Nursing Mothers 3 words ▾

8.3 Nursing Mothers

🧬 Pharmacokinetics ~3 min read ▾

12.3Pharmacokinetics Table 11. Mean Maraviroc Pharmacokinetic Parameters in Adults Patient Population Maraviroc Dose n AUC 12 (ng.h/mL) C max (ng/mL) C min (ng/mL) Healthy volunteers (Phase 1) 300 mg twice daily 64 2,908 888

43.1 Asymptomatic HIV subjects (Phase 2a) 300 mg twice daily 8 2,550 618

33.6Treatment-experienced HIV subjects (Phase 3)a 300 mg twice daily 94 1,513 266 37.2 150 mg twice daily (+ CYP3A inhibitor) 375 2,463 332 101 Treatment-naiveHIV subjects (Phase 2b/3)a 300 mg twice daily 344 1,865 287 60 a The estimated exposure is lower compared with other trials possibly due to sparse sampling, food effect, compliance, and concomitant medications. Absorption Peak maraviroc plasma concentrations are attained 0.5 to 4 hours following single oral doses of 1 to1,200 mg administered to uninfected volunteers.

The pharmacokinetics of oral maraviroc are not dose proportional over the dose range. The absolute bioavailability of a 100-mg dose is 23% and is predicted to be 33% at 300 mg. Maraviroc is a substrate for the efflux transporter P-gp.

Effect of Food on Oral Absorption: Coadministration of a 300-mg tablet with a high-fat breakfast reduced maraviroc Cmax and AUC by 33% and coadministration of 75 mg of oral solution with a high-fat breakfast reduced maraviroc AUC by 73% in healthy adult volunteers. Studies with the tablet formulation demonstrated a reduced food effect at higher doses. There were no food restrictions in the adult trials (using the tablet formulation) or in the pediatric trial (using both tablet and oral solution formulations) that demonstrated the efficacy/antiviral activity and safety of maraviroc [ see Clinical Studies ( 14.1 , 14.2 ) ].

Distribution Maraviroc is bound (approximately 76%) to human plasma proteins, and shows moderate affinity for albumin and alpha-1 acid glycoprotein. The volume of distribution of maraviroc is approximately 194 L. Elimination Metabolism : Trials in humans and in vitro studies using human liver microsomes and expressed enzymes have demonstrated that maraviroc is principally metabolized by the cytochrome P450 system to metabolites that are essentially inactive against HIV-1.

In vitro studies indicate that CYP3A is the major enzyme responsible for maraviroc metabolism. In vitro studies also indicate that polymorphic enzymes CYP2C9, CYP2D6, and CYP2C19 do not contribute significantly to the metabolism of maraviroc. Maraviroc is the major circulating component (~42% drug-related radioactivity) following a single oral dose of 300 mg [14C]-maraviroc.

The most significant circulating metabolite in humans is a secondary amine (~22% radioactivity) formed by N-dealkylation. This polar metabolite has no significant pharmacological activity. Other metabolites are products of mono-oxidation and are only minor components of plasma drug-related radioactivity.

Excretion: The terminal half-life of maraviroc following oral dosing to steady state in healthy subjects was 14 to 18 hours. A mass balance/excretion trial was conducted using a single 300-mg dose of 14C-labeled maraviroc. Approximately 20% of the radiolabel was recovered in the urine and 76% was recovered in the feces over 168 hours.

Maraviroc was the major component present in urine (mean of 8% dose) and feces (mean of 25% dose). The remainder was excreted as metabolites. Specific Populations Patients with Hepatic Impairment: Maraviroc is primarily metabolized and eliminated by the liver.

A trial compared the pharmacokinetics of a single 300-mg dose of maraviroc in subjects with mild (Child-Pugh Class A, n = 8) and moderate (Child-Pugh Class B, n = 8) hepatic impairment with pharmacokinetics in healthy subjects (n = 8). The mean Cmax and AUC were 11% and 25% higher, respectively, for subjects with mild hepatic impairment, and 32% and 46% higher, respectively, for subjects with moderate hepatic impairment compared with subjects with normal hepatic function. These changes do not warrant a dose adjustment.

Maraviroc concentratio… [Excerpted — this section continues on DailyMed.]

🧬 Pharmacodynamics ~2 min read ▾

12.2Pharmacodynamics Exposure-Response Relationship in Treatment-Experienced Adult Subjects The relationship between maraviroc, modeled plasma trough concentration (C min ) (1 to 9 samples per subject taken on up to 7 visits), and virologic response was evaluated in 973 treatment-experienced HIV-1-infected subjects with varied optimized background antiretroviral regimens in Trials A4001027 and A4001028. The C min , baseline viral load, baseline CD4+ cell count, and overall sensitivity score (OSS) were found to be important predictors of virologic success (defined as viral load less than 400 copies per mL at 24 weeks).

Table 9 illustrates the proportions of subjects with virologic success (%) within each C min quartile for 150-mg twice-daily and 300-mg twice-daily groups. Table 9. Treatment-Experienced Subjects with Virologic Success by Cmin Quartile (Q1 to Q4) 150 mg Twice Daily (with CYP3A Inhibitors) 300 mg Twice Daily (without CYP3A Inhibitors) n Median C min % Subjects with Virologic Success n Median C min % Subjects with Virologic Success Placebo 160 - 30.6 35 -

28.6Q1 78 33 52.6 22 13

50.0Q2 77 87 63.6 22 29

68.2Q3 78 166 78.2 22 46

63.6Q4 78 279 74.4 22 97

68.2Exposure-Response Relationship in Treatment-Naive Adult Subjects The relationship between maraviroc, modeled plasma trough concentration (C min ) (1 to 12 samples per subject taken on up to 8 visits), and virologic response was evaluated in 294 treatment-naive HIV-1-infected subjects receiving maraviroc 300 mg twice daily in combination with lamivudine/zidovudine in Trial A4001026. Table 10 illustrates the proportion (%) of subjects with virologic success less than 50 copies per mL at 48 weeks within each C min quartile for the 300-mg twice-daily dose.

Table 10. Treatment-Naive Subjects with Virologic Success by C min Quartile (Q1 to Q4) 300 mg Twice Daily n Median C min % Subjects with Virologic Success Q1 75 23

57.3 Q2 72 39

72.2 Q3 73 56

74.0 Q4 74 81

83.8Eighteen of 75 (24%) subjects in Q1 had no measurable maraviroc concentration on at least one occasion versus 1 of 73 and 1 of 74 in Q3 and Q4, respectively. Effects on Electrocardiogram A placebo-controlled, randomized, crossover trial to evaluate the effect on the QT interval of healthy male and female volunteers was conducted with 3 single oral doses of maraviroc and moxifloxacin. The placebo-adjusted mean maximum (upper 1-sided 95% CI) increases in QTc from baseline after 100, 300, and 900 mg of maraviroc were -2 (0), -1 (1), and 1 (3) msec, respectively, and 13 (15) msec for moxifloxacin 400 mg.

No subject in any group had an increase in QTc of greater than or equal to 60 msec from baseline. No subject experienced an interval exceeding the potentially clinically relevant threshold of 500 msec.

🔬 Clinical Studies ~3 min read ▾

14 CLINICAL STUDIES

14.1Clinical Studies in Adult Subjects The clinical efficacy and safety of maraviroc are derived from analyses of data from 3 trials in adult subjects infected with CCR5-tropic HIV-1: Trials A4001027 and A4001028 in antiretroviral treatment-experienced adult subjects and Trial A4001026 in treatment-naive subjects. These trials were supported by a 48-week trial in antiretroviral treatment-experienced adult subjects infected with dual/mixed-tropic HIV-1, Trial A4001029. Trials in CCR5-Tropic, Treatment-Experienced Subjects Trials A4001027 and A4001028 were double-blind, randomized, placebo-controlled, multicenter trials in subjects infected with CCR5-tropic HIV-1.

Subjects were required to have an HIV-1 RNA greater than 5,000 copies per mL despite at least 6 months of prior therapy with at least 1 agent from 3 of the 4 antiretroviral drug classes (greater than or equal to 1 NRTI, greater than or equal to 1 NNRTI, greater than or equal to 2 PIs, and/or enfuvirtide) or documented resistance to at least 1 member of each class. All subjects received an optimized background regimen consisting of 3 to 6 antiretroviral agents (excluding low-dose ritonavir) selected on the basis of the subject’s prior treatment history and baseline genotypic and phenotypic viral resistance measurements.

In addition to the optimized background regimen, subjects were then randomized in a 2:2:1 ratio to maraviroc 300 mg once daily, maraviroc 300 mg twice daily, or placebo. Doses were adjusted based on background therapy as described in Dosage and Administration ( 2 ) , Table 1. In the pooled analysis for Trials A4001027 and A4001028, the demographics and baseline characteristics of the treatment groups were comparable (Table 16).

Of the 1,043 subjects with a CCR5-tropism result at screening, 7.6% had a dual/mixed-tropism result at the baseline visit 4 to 6 weeks later. This illustrates the background change from CCR5- to dual/mixed-tropism result over time in this treatment-experienced population, prior to a change in antiretroviral regimen or administration of a CCR5 co-receptor antagonist. Table 16.

Demographic and Baseline Characteristics of Subjects in Trials A4001027 and A4001028 Maraviroc Twice Daily (n = 426) Placebo (n = 209) Age (years) Mean (range) 46.3 (21-73) 45.7 (29-72) Sex: Male 382 (89.7%) 185 (88.5%) Female 44 (10.3%) 24 (11.5%) Race: White 363 (85.2%) 178 (85.2%) Black 51 (12.0%) 26 (12.4%) Other 12 (2.8%) 5 (2.4%) Region: U.S. 276 (64.8%) 135 (64.6%) Non-U.S. 150 (35.2%) 74 (35.4%) Subjects with previous enfuvirtide use 142 (33.3%) 62 (29.7%) Subjects with enfuvirtide as part of OBT 182 (42.7%) 91 (43.5%) Baseline plasma HIV-1 RNA (log 10 copies/mL) Mean (range) 4.85 (2.96-6.88) 4.86 (3.46-7.07) Subjects with screening viral load ≥100,000 copies/mL 179 (42.0%) 84 (40.2%) Baseline CD4+ cell count (cells/mm 3 ) Median (range) 167 (2-820) 171 (1-675) Subjects with baseline CD4+ cell count ≤200 cells/mm 3 ) 250 (58.7%) 118 (56.5%) Subjects with Overall Susceptibility Score (OSS): a 0 1 2 ≥3 57 (13.4%) 136 (31.9%) 104 (24.4%) 125 (29.3%) 35 (16.7%) 44 (21.1%) 59 (28.2%) 66 (31.6%) Subjects with enfuvirtide resistance substitutions 90 (21.2%) 45 (21.5%) Median number of resistance-associated: b PI substitutions NNRTI substitutions NRTI substitutions 10 1 6 10 1 6 a OSS - Sum of active drugs in OBT based on combined information from genotypic and phenotypic testing. b Resistance substitutions based on IAS guidelines.

1 The Week 48 results for the pooled Trials A4001027 and A4001028 are shown in Table 17. Table 17. Outcomes of Randomized Treatment at Week 48 in Trials A4001027 and A4001028 Outcome Maraviroc Twice Daily (n = 426) Placebo (n = 209) Mean Difference Mean change from Baseline to Week 48 inHIV-1 RNA (log 10 copies/mL) -1.84 -0.78 -1.05 <400 copies/mL at Week 48 239 (56%) 47 (22%) 34% <50 copies/mL at Week 48 194 (46%) 35 (17%) 29% Discontinuations: Insufficient clinical response Adverse events Other 97 (23%) 19 (4… [Excerpted — this section continues on DailyMed.]

🔒 Drug Abuse and Dependence 10 words ▾

9 DRUG ABUSE AND DEPENDENCE

9.1 Controlled Substance

9.2 Abuse

🔒 Controlled Substance 3 words ▾

9.1 Controlled Substance

🧪 Nonclinical Toxicology 172 words ▾

13 NONCLINICAL TOXICOLOGY

13.1Carcinogenesis ,Mutagenesis, Impairment Of Fertility Carcinogenesis Long-term oral carcinogenicity studies of maraviroc were carried out in rasH2 transgenic mice (6 months) and in rats for up to 96 weeks (females) and 104 weeks (males). No drug-related increases in tumor incidence were found in mice at 1,500 mg per kg per day and in male and female rats at 900 mg per kg per day. The highest exposures in rats were approximately 11 times those observed in humans at the therapeutic dose of 300 mg twice daily for the treatment of HIV-1 infection.

Mutagenesis Maraviroc was not genotoxic in the reverse mutation bacterial test (Ames test in Salmonella and E. coli), a chromosome aberration test in human lymphocytes, and mouse bone marrow micronucleus test. Impairment of Fertility Maraviroc did not impair mating or fertility of male or female rats and did not affect sperm of treated male rats at approximately 20-fold higher exposures (AUC) than in humans given the recommended 300-mg twice-daily dose.

13.2 Animal Pharmacology & OR Toxicology

📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 163 words ▾

13.1Carcinogenesis ,Mutagenesis, Impairment Of Fertility Carcinogenesis Long-term oral carcinogenicity studies of maraviroc were carried out in rasH2 transgenic mice (6 months) and in rats for up to 96 weeks (females) and 104 weeks (males). No drug-related increases in tumor incidence were found in mice at 1,500 mg per kg per day and in male and female rats at 900 mg per kg per day. The highest exposures in rats were approximately 11 times those observed in humans at the therapeutic dose of 300 mg twice daily for the treatment of HIV-1 infection.

Mutagenesis Maraviroc was not genotoxic in the reverse mutation bacterial test (Ames test in Salmonella and E. coli), a chromosome aberration test in human lymphocytes, and mouse bone marrow micronucleus test. Impairment of Fertility Maraviroc did not impair mating or fertility of male or female rats and did not affect sperm of treated male rats at approximately 20-fold higher exposures (AUC) than in humans given the recommended 300-mg twice-daily dose.

📚 References 9 words ▾

15 REFERENCES 1. IAS-USA Drug Resistance Mutations Figures. http://www.iasusa.org/pub/topics/2006/issue3/125.pdf

📄 Package Label / Principal Display Panel 16 words ▾

PACKAGE LABEL.PRINCIPAL DISPLAY PANEL Maraviroc Tablet 150 mg Label Maraviroc Tablet 300 mg Label maraviroctablet150mglabel maraviroctablet300mglabel

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 Maraviroc — the program that covers self-administered drugs. 3 manufacturers.
⚠️ 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 Maraviroc. 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
$3.24M
Claims incl. refills
3.4K
Beneficiaries
1.3K
Spend / beneficiary
$2,439.54
Spend / claim
$965.08
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.

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Package photos — Not published for this NDC No photo available yet for this listing.
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 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 XLCare Pharmaceuticals Inc.. Listing status can change — the directory data on this page refreshes weekly.
Who lists this product with the FDA?
XLCare Pharmaceuticals Inc. 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.
← 72865-0231-60 · XLCare 72865-0233-01 · XLCare →
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.