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Table of Contents

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents

Appendix B: Drug Characteristics Tables

Characteristics of CCR5 Antagonist

(Last updated: March 27, 2012; last reviewed: May 1, 2014)

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Appendix B, Table 6. Characteristics of CCR5 Antagonist
Generic Name (Abbreviation)/ Trade Name Formulation Dosing Recommendationsa
Serum Half-Life Elimination/
Metabolic Pathway
Adverse Eventsb
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, 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 = ritonavir-boosted tipranavir 

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