Drug intelligence / Profile preview

elvitegravir + cobicistat + emtricitabine + tenofovir alafenamide + atazanavir

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

Overview

This is a **combination of five antiretroviral drugs**: elvitegravir (an HIV-1 integrase strand transfer inhibitor), cobicistat (a pharmacokinetic enhancer serving as a CYP3A inhibitor), emtricitabine (a nucleoside reverse transcriptase inhibitor), tenofovir alafenamide (a nucleotide reverse transcriptase inhibitor prodrug), and atazanavir (an HIV-1 protease inhibitor). While fixed-dose combinations of the first four (e.g., Genvoya) exist and fixed-dose combinations of cobicistat and atazanavir are approved and marketed (e.g., Evotaz), **this specific five-drug combination does not have an established fixed-dose product or unique marketed brand in major regulatory regions**. However, all components are used for the **treatment of HIV-1 infection** as part of combination antiretroviral therapy regimens.

02

Targets

SLC47A1 (Multidrug and toxin extrusion transporter 1)ABCG2 (Breast cancer resistance protein)ABCB1 (P-glycoprotein)Human immunodeficiency virus type 1 reverse transcriptaseOATP1B1 (Organic anion transporting polypeptide 1B1)CYP3A5 (Cytochrome P450 family 3 subfamily A member 5)Integrase allosteric pocket (HIV)PR (Progesterone receptor)

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