Drug intelligence / Profile preview

elvitegravir + cobicistat + emtricitabine + tenofovir alafenamide (Gilead Sciences)

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

Overview

**Elvitegravir + cobicistat + emtricitabine + tenofovir alafenamide** is a fixed-dose, four-drug oral antiretroviral regimen marketed as **Genvoya** by Gilead Sciences. Elvitegravir is an HIV-1 integrase strand transfer inhibitor that blocks proviral DNA integration; emtricitabine and tenofovir alafenamide are nucleoside/nucleotide reverse transcriptase inhibitors whose active intracellular metabolites inhibit HIV-1 reverse transcriptase and terminate viral DNA synthesis. Cobicistat is a CYP3A inhibitor included as a pharmacokinetic booster to increase elvitegravir exposure. It is approved as a complete regimen for treatment of HIV-1 infection in treatment-naive adults and pediatric patients weighing at least 25 kg, and for eligible virologically suppressed patients switching from a stable regimen. ([gilead.com](https://www.gilead.com/~/media/files/pdfs/medicines/hiv/genvoya/genvoya_pi.pdf))

Brand names
Genvoya
Other names
E/C/F/TAFEVG/COBI/FTC/TAFelvitegravir/cobicistat/emtricitabine/tenofovir alafenamide
02

Targets

ABCG2 (Breast cancer resistance protein)Integrase allosteric pocket (HIV)Human immunodeficiency virus type 1 reverse transcriptaseHIV-2 reverse transcriptaseHBV Pol (Hepatitis B virus polymerase)ABCB1 (P-glycoprotein)CYP2C19 (Cytochrome P450 2C19)CYP3A4 (Cytochrome P450 3A4)CYP3A5 (Cytochrome P450 family 3 subfamily A member 5)RAG1 (Recombination Activating Gene 1)

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