Maraviroc (2 brand names, 2 dosage forms, 1 route)
Available dosage forms: TABLET, SOLUTION.
Routes of administration: ORAL.
Brand Names
- MARAVIROC
- SELZENTRY
Boxed Warning
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)].
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) ].
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) ].
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) ]
Mechanism of Action
Maraviroc is an HIV-1 antiviral drug [ see Microbiology ( 12.4) ].
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) ].