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Cobicistat is a selective inhibitor of cytochrome P450 (CYP) 3A enzymes with IC50 values ranging from 0.03 to 0.285μM [1].

Cobicistat is a selective CYP3A inhibitor without intrinsic anti-HIV activity and is indicated in EU as a pharmacokinetic enhancer of the HIV-1 protease inhibitors atazanavir and darunavir in adults. Cobicistat is also developed to form a fixed-dose tablet in combination with elvitegravir, emtricitabine and TDF. Cobicistat inhibits CYP3A in vitro across a variety of substrates with IC50 values ranging from 0.03 to 0.285μM. Cobicistat is absorbed rapidly after oral administration in patients infected with HIV-1 with the Cmax of 1.2μg/ml. In the 48-week analysis of the phase III study, once-daily oral cobicistat is generally well tolerated. The tolerability of the cobicistat-boosted atazanavir remains similar longer term, with jaundice, ocular icterus and nausea in a 96-week analysis of the phase III study [1

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