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HIGHLIGHTS OF PRESCRIBING INFORMATION
These highlights do not include all the information needed to use SELZENTRY safely and effectively. See full prescribing information for SELZENTRY.
SELZENTRY (maraviroc) Tablets
Initial U.S. Approval: 2007
SELZENTRY (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.
SELZENTRY is available as film-coated tablets for oral administration containing either 150 or 300 mg of maraviroc and the following inactive ingredients: microcrystalline cellulose, dibasic calcium phosphate (anhydrous), sodium starch glycolate, and magnesium stearate. The film coat [Opadry® II Blue (85G20583)] contains FD&C blue #2 aluminum lake, soya lecithin, polyethylene glycol (macrogol 3350), polyvinyl alcohol, talc and titanium dioxide.
Mechanism of Action
Maraviroc is an antiviral drug.
Maraviroc is a member of a therapeutic class called CCR5 co-receptor antagonists. Maraviroc selectively binds to the human chemokine receptor CCR5 present on the cell membrane, preventing the interaction of HIV-1 gp120 and CCR5 necessary for CCR5-tropic HIV-1 to enter cells. CXCR4-tropic and dual-tropic HIV-1 entry is not inhibited by maraviroc.
INDICATIONS AND USAGE
SELZENTRY, in combination with other antiretroviral agents, is indicated for adult patients infected with only CCR5-tropic HIV-1.
This indication is based on analyses of plasma HIV-1 RNA levels in two controlled studies of SELZENTRY in treatment-experienced subjects and one study in treatment-naïve subjects. Both studies in treatment-experienced subjects were conducted in clinically advanced, 3-class antiretroviral-experienced (NRTI, NNRTI, PI, or enfuvirtide) adults with evidence of HIV-1 replication despite ongoing antiretroviral therapy.
The following points should be considered when initiating therapy with SELZENTRY:
--Adult patients infected with only CCR5-tropic HIV-1 should use SELZENTRY.
--Tropism testing must be conducted with a highly sensitive tropism assay that has demonstrated the ability to identify patients appropriate for SELZENTRY use. 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 SELZENTRY.
--Use of SELZENTRY is not recommended in subjects with dual/mixed or CXCR4-tropic HIV-1 as efficacy was not demonstrated in a phase 2 study of this patient group.
--The safety and efficacy of SELZENTRY have not been established in pediatric patients.
--In treatment-naïve subjects, more subjects treated with SELZENTRY experienced virologic failure and developed lamivudine resistance compared to efavirenz.
SELZENTRY should not be used in patients with severe renal impairment or end-stage renal disease (ESRD) (CrCl < 30 mL/min) who are taking potent CYP3A inhibitors or inducers.
WARNINGS AND PRECAUTIONS
--Use caution when administering SELZENTRY to patients with pre-existing liver dysfunction or who are co-infected with viral hepatitis B or C.
--More cardiovascular events including myocardial ischemia and/or infarction were observed in treatment-experienced subjects who received SELZENTRY. Use with caution in patients at increased risk of cardiovascular events .
--If patients with severe renal impairment or end-stage renal disease (ESRD) receiving SELZENTRY (without concomitant CYP3A inducers or inhibitors) experience postural hypotension the SELZENTRY dose should be reduced from 300 mg twice daily to 150 mg twice daily.
--Coadministration with CYP3A inhibitors, including protease inhibitors (except tipranavir/ritonavir) and delavirdine, will increase the concentration of SELZENTRY.
--Coadministration with CYP3A inducers, including efavirenz, may decrease the concentration of SELZENTRY.
USE IN SPECIFIC POPULATIONS
--SELZENTRY should only be used in pregnant women if the potential benefit justifies the potential risk to the fetus.
--There are no data available in pediatric patients; therefore, SELZENTRY should not be used in patients <16 years of age.
The most common adverse events in treatment-experienced subjects (>8% incidence) which occurred at a higher frequency compared to placebo are upper respiratory tract infections, cough, pyrexia, rash, and dizziness.
To report SUSPECTED ADVERSE REACTIONS, contact Pfizer at 1-800-438-1985 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch
DOSAGE AND ADMINISTRATION
Dose Recommendations for Patients with Normal Renal Function
The recommended dose of SELZENTRY differs based on concomitant medications due to drug interactions (see Table 1). SELZENTRY can be taken with or without food. SELZENTRY must be given in combination with other antiretroviral medications.
Table 1 gives the recommended dose adjustments.
Table 1 Recommended Dosing Regimen
Dose Recommendations for Patients with Renal Impairment
Table 2 provides dosing recommendations for patients based on renal function and concomitant medications.
Table 2 Recommended Dosing Regimens Based on Renal Function
DOSAGE FORMS AND STRENGTHS
Tablets: 150 mg and 300 mg
Package Insert data:
PRINCIPAL DISPLAY PANEL - 150 mg Tablet Bottle Label
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