Drug intelligence / Profile preview

elvitegravir + cobicistat + emtricitabine + tenofovir alafenamide + darunavir

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

Overview

A five-drug oral fixed-dose antiretroviral combination designed for the treatment of HIV-1 infection, consisting of **elvitegravir** (an integrase strand transfer inhibitor), **cobicistat** (pharmacokinetic enhancer/CYP3A inhibitor), **emtricitabine** (nucleoside reverse transcriptase inhibitor), **tenofovir alafenamide** (nucleotide reverse transcriptase inhibitor), and **darunavir** (protease inhibitor). This combination contains agents targeting different critical steps of HIV viral replication and metabolism: elvitegravir blocks HIV integrase, darunavir inhibits HIV protease, both emtricitabine and tenofovir alafenamide inhibit HIV reverse transcriptase, and cobicistat enhances exposures of elvitegravir and darunavir by inhibiting CYP3A-mediated metabolism. It is designed to minimize pill burden and increase convenience but is not available as a branded, approved fixed-dose tablet; branded four-drug combinations exist (Genvoya, Symtuza), but not with all five. Used as a fully suppressive regimen for HIV-1, including treatment-naive and certain treatment-experienced patients. Developed by combining agents from Gilead (elvitegravir, cobicistat, emtricitabine, tenofovir alafenamide) and Janssen (darunavir).

Other names
elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide + darunavirE/C/F/TAF + DRV
02

Targets

Integrase allosteric pocket (HIV)Human immunodeficiency virus type 1 reverse transcriptaseCYP3A (CYP3A family)PR (Progesterone receptor)

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