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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: April 8, 2015)

Appendix B, Table 6. Characteristics of CCR5 Antagonist
Generic Name
Trade Name
Formulation Dosing Recommendationsa
Serum Half-Life Elimination/
Metabolic Pathway
Adverse Eventsb
  • 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

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