CCR5 Antagonist Characterstics Adult and Adolescent ARV Guidelines

Appendix B: Drug Characteristics Tables

Last Updated: March 27, 2012; Last Reviewed: April 8, 2015

Appendix B, Table 6. Characteristics of CCR5 Antagonist
Generic Name (Abbreviation) Trade Name	Formulation	Dosing Recommendations^a	Serum Half-Life	Elimination/ Metabolic Pathway	Adverse Events^b
Maraviroc (MVC) Selzentry	150 and 300 mg tablets	150 mg BID when given with drugs that are strong CYP3A inhibitors (with or without CYP3A inducers) including PIs (except TPV/r) 300 mg BID when given with NRTIs, T20, TPV/r, NVP, RAL, and other drugs that are not strong CYP3A inhibitors or inducers 600 mg BID when given with drugs that are CYP3A inducers, including EFV, ETR, etc. (without a CYP3A inhibitor) Take without regard to meals.	14-18 hours	CYP3A4 substrate	Abdominal pain Cough Dizziness Musculoskeletal symptoms Pyrexia Rash Upper respiratory tract infections Hepatotoxicity, which may be preceded by severe rash or other signs of systemic allergic reactions Orthostatic hypotension, especially in patients with severe renal insufficiency
^a For dosage adjustment in hepatic insufficiency, see Appendix B, Table 7. ^b Also see Table 14. Key to Abbreviations: BID = twice daily; CYP = cytochrome P; EFV = efavirenz; ETR = etravirine; MVC = maraviroc; NRTI = nucleoside reverse transcriptase inhibitor; NVP = nevirapine; PI = protease inhibitor; RAL = raltegravir; T20 = enfuvirtide; TPV/r = tipranavir/ritonavir