Drug intelligence / Profile preview

cobicistat + atazanavir + 2 nucleoside reverse transcriptase inhibitors

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

This regimen refers to the **co-administration of cobicistat (a pharmacokinetic enhancer/CYP3A inhibitor), atazanavir (an HIV-1 protease inhibitor), and two nucleoside reverse transcriptase inhibitors (NRTIs)** as a complete antiretroviral therapy (ART) for the treatment of HIV-1 infection. - **Cobicistat** acts by inhibiting cytochrome P450 3A enzymes, thereby increasing and sustaining the plasma levels of atazanavir. - **Atazanavir** inhibits the HIV-1 protease enzyme, preventing cleavage of viral polyproteins, leading to the production of immature, noninfectious viral particles. - The two NRTIs, though not specified by name here, function by inhibiting the reverse transcriptase enzyme, which blocks conversion of viral RNA into DNA, a critical step in the HIV replication cycle. - This combination is designed to maximize viral suppression, reduce risk of resistance, and is frequently used where cobicistat and atazanavir are combined as a fixed-dose tablet (marketed as Evotaz), taken together with a separate NRTI backbone to form a complete regimen[1][2][3][6].

02

Targets

CYP3A (CYP3A family)PR (Progesterone receptor)Human immunodeficiency virus type 1 reverse transcriptase

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