Drug intelligence / Profile preview

cobicistat + darunavir + 2 nucleoside reverse transcriptase inhibitors

Development stage
Unknown
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination antiretroviral regimen used for the treatment of HIV-1 infection. It consists of **cobicistat** (a pharmacokinetic booster that inhibits CYP3A to increase exposure of other co-administered drugs), **darunavir** (an HIV-1 protease inhibitor that prevents viral replication by inhibiting the cleavage of Gag-Pol polyprotein), and **two nucleoside reverse transcriptase inhibitors (NRTIs)**, which inhibit HIV reverse transcriptase by acting as chain terminators during viral DNA synthesis. This multi-drug regimen suppresses HIV replication via distinct and complementary mechanisms, thereby improving treatment efficacy and minimizing resistance development.

02

Targets

SLC47A1 (Multidrug and toxin extrusion transporter 1)ABCB1 (P-glycoprotein)Human immunodeficiency virus type 1 reverse transcriptaseOATP1B1 (Organic anion transporting polypeptide 1B1)ABCG2 (Breast cancer resistance protein)CYP3A7 (Cytochrome P450 3A7)PR (Progesterone receptor)

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