Drug intelligence / Profile preview

atazanavir + tenofovir + ritonavir

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

Overview

atazanavir + tenofovir + ritonavir is a combination antiretroviral regimen used for the treatment of HIV-1 infection. It consists of two protease inhibitors, atazanavir and ritonavir, and one nucleotide reverse transcriptase inhibitor (NRTI), tenofovir disoproxil fumarate. Atazanavir selectively inhibits the HIV-1 protease, an enzyme required for the proteolytic cleavage of viral polyprotein precursors into individual functional proteins, thereby preventing the formation of mature infectious virions. Tenofovir disoproxil fumarate is a prodrug of tenofovir, which inhibits HIV-1 reverse transcriptase by competing with deoxyadenosine 5'-triphosphate and causing DNA chain termination. Ritonavir is included at a low dose primarily as a pharmacokinetic enhancer; it inhibits the CYP3A4 isoenzyme, which is responsible for the metabolism of atazanavir, thereby increasing atazanavir's systemic exposure and allowing for once-daily dosing. This specific combination was evaluated in Phase 1 clinical trials by Asan Medical Center to investigate pharmacokinetic differences and potential drug-drug interactions between Korean and Caucasian populations.

Other names
atazanavir + tenofovir disoproxil fumarate + ritonavirATV + TDF + RTV
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseCYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)

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