Drug intelligence / Profile preview

elvitegravir + cobicistat

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral
01

Overview

Elvitegravir + cobicistat is a fixed-dose combination of two antiretroviral agents used in the treatment of human immunodeficiency virus (HIV) infection. Elvitegravir is an integrase strand transfer inhibitor that blocks the integration of viral DNA into the host genome, thereby inhibiting HIV replication. Cobicistat acts as a pharmacokinetic enhancer by selectively inhibiting cytochrome P450 3A4 (CYP3A4), which increases plasma concentrations of elvitegravir and enhances its antiviral effect. Cobicistat itself has no direct anti-HIV activity but boosts the effectiveness of other antiretrovirals by slowing their metabolism[5][6]. This combination is often co-formulated with other antiretrovirals for once-daily oral administration in HIV therapy.

02

Targets

CYP2D6 (Cytochrome P450 2D6)SLCO1B3 (Organic anion transporting polypeptide 1B3)OATP1B1 (Organic anion transporting polypeptide 1B1)ABCB1 (P-glycoprotein)CYP3A4 (Cytochrome P450 3A4)ABCG2 (Breast cancer resistance protein)Integrase allosteric pocket (HIV)CYP3A (CYP3A family)

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