Selzentry Generic Name & Formulations
Legal Class
Rx
General Description
Maraviroc 25mg, 75mg, 150mg, 300mg; tabs.
Pharmacological Class
CCR5 co-receptor antagonist.
See Also
How Supplied
Tabs 25mg, 75mg—120; 150mg, 300mg—60; Soln (w. oral syringe)—230mL
Manufacturer
Generic Availability
NO
Selzentry Indications
Indications
In combination with other antiretrovirals, in patients ≥2yrs and weighing ≥10kg infected with only CCR5-tropic HIV-1.
Limitations of Use
Not recommended in patients with dual/mixed- or CXCR4-tropic HIV-1.
Selzentry Dosage and Administration
Adult
Test all patients for CCR5 tropism prior to initiation. Swallow tabs whole. Concomitant potent CYP3A inhibitors (eg, PIs [except tipranavir/ritonavir], delavirdine, elvitegravir/ritonavir, ketoconazole, itraconazole, clarithromycin, nefazodone, telithromycin, boceprevir) (with or without a potent CYP3A inducer): 150mg twice daily. Noninteracting concomitant drugs, including tipranavir/ritonavir, nevirapine, raltegravir, NRTIs, enfuvirtide: 300mg twice daily. Concomitant potent CYP3A inducers (eg, efavirenz, rifampin, etravirine, carbamazepine, phenobarbital, phenytoin) (without a potent CYP3A inhibitor): 600mg twice daily. Severe renal impairment (CrCl <30mL/min) or ESRD (without potent CYP3A inhibitors or inducers): reduce dose from 300mg twice daily to 150mg twice daily if postural hypotension occurs; others: see full labeling.
Children
<2yrs: not established. Test all patients for CCR5 tropism prior to initiation. Swallow tabs whole; if unable to swallow, use oral soln. ≥2yrs: Concomitant potent CYP3A inhibitors (eg, PIs [except tipranavir/ritonavir], delavirdine, elvitegravir/ritonavir, ketoconazole, itraconazole, clarithromycin, nefazodone, telithromycin, boceprevir) (with or without a potent CYP3A inducer): (10–<20kg): 50mg or 2.5mL twice daily; (20–<30kg): 75mg or 4mL twice daily; (30–<40kg): 100mg or 5mL twice daily; (≥40kg): 150mg or 7.5mL twice daily. Noninteracting concomitant drugs, including tipranavir/ritonavir, nevirapine, raltegravir, NRTIs, enfuvirtide: (10–<30kg): not recommended; (≥30kg): 300mg or 15mL twice daily. Concomitant potent CYP3A inducers (eg, efavirenz, rifampin, etravirine, carbamazepine, phenobarbital, phenytoin) (without a potent CYP3A inhibitor): not recommended.
Selzentry Contraindications
Contraindications
Severe renal impairment or ESRD (CrCl <30mL/min) in patients taking concomitant potent CYP3A inhibitors or inducers.
Selzentry Boxed Warnings
Boxed Warning
Hepatotoxicity.
Selzentry Warnings/Precautions
Warnings/Precautions
Hepatotoxicity (may be preceded by systemic allergic reaction; immediately evaluate if occurs); obtain ALT, AST, and bilirubin prior to initiating and during therapy; consider discontinuing if hepatitis or elevated liver transaminases with rash or other systemic symptoms develop. Pre-existing liver dysfunction or co-infected with hepatitis B and/or C virus; monitor more frequently. Increased risk of cardiovascular events (eg, myocardial ischemia and/or infarction); monitor more frequently. Postural hypotension (esp. with severe renal insufficiency or ESRD). Monitor for infections, malignancies. Pregnancy. Nursing mothers: not recommended.
Selzentry Pharmacokinetics
See Literature
Selzentry Interactions
Interactions
See Adult, Children. Concomitant St. John's wort: not recommended. May affect, or be affected by, inhibitors or inducers of CYP3A and P-gp (eg, potentiated by ketoconazole, boceprevir, lopinavir/ritonavir, ritonavir, darunavir/ritonavir, saquinavir/ritonavir, atazanavir; antagonized by rifampin, etravirine, efavirenz). May be affected by inhibitors of OATP1B1 and MRP2. Caution with antihypertensives.
Selzentry Adverse Reactions
Adverse Reactions
Upper respiratory tract infections, cough, pyrexia, rash, dizziness, constipation, bronchitis, flatulence, bloating, distention, GI atonic, hypomotility disorders; severe skin and hypersensitivity reactions (eg, Stevens-Johnson syndrome, toxic epidermal necrolysis; discontinue immediately if develop), immune reconstitution syndrome; also Peds: vomiting, abdominal pain, diarrhea, nausea.
Selzentry Clinical Trials
See Literature
Selzentry Note
Notes
Register pregnant patients exposed to maraviroc by calling (800) 258-4263.
Selzentry Patient Counseling
See Literature