What is the role of pharmacokinetic enhancers in antiretroviral therapy of HIV infection?

Updated: Apr 18, 2019
  • Author: R Chris Rathbun, PharmD, BCPS (AQ-ID), AAHIVP; Chief Editor: John Bartlett, MD  more...
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Cobicistat (Tybost) is a CYP3A inhibitor. As a single agent, it is indicated to increase systemic exposure of atazanavir or darunavir (once-daily dosing regimen) in combination with other antiretroviral agents. It is more commonly used in co-formulations with these protease inhibitors (darunavir/cobicistat [Prezcobix], atazanavir/cobicistat [Evotaz]) or as a component of several elvitegravir-containing fixed dose combinations (elvitegravir/cobicistat/emtricitabine/tenofovir DF [Stribild], elvitegravir/cobicistat/emtricitabine/tenofovir AF [Genvoya]).

Cobicistat may be used for treatment-naïve or experienced patients (without darunavir resistance-associated substitutions). The dosage is 150 mg PO once daily when used with atazanavir (300 mg PO once daily), darunavir (800 mg PO once daily) or elvitegravir (150 mg PO once daily).

Ritonavir is also a potent CYP3A4 inhibitor that is in many combination productions and included in many HIV treatment regimens to augment systemic exposure to other antiretroviral agents.

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