Drug intelligence / Profile preview

atazanavir + ritonavir + tenofovir

Development stage
Phase 2
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

This is a fixed-dose combination regimen of three antiretroviral drugs used in the treatment of human immunodeficiency virus (HIV) infection. Atazanavir is a protease inhibitor that blocks the HIV protease enzyme, preventing viral replication. Ritonavir acts as a pharmacokinetic enhancer by inhibiting cytochrome P450 3A4 (CYP3A4), thereby increasing plasma concentrations of atazanavir. Tenofovir disoproxil fumarate is a nucleotide reverse transcriptase inhibitor (NRTI) that inhibits HIV reverse transcriptase by competing with natural substrates and causing DNA chain termination. This combination is indicated for use in adults and children with HIV-1 infection and forms part of highly active antiretroviral therapy (HAART). The regimen has clinically significant drug-drug interactions; coadministration alters the pharmacokinetics of both atazanavir and tenofovir[1][2][5]. Patients should be monitored for adverse effects such as renal toxicity from tenofovir and hyperbilirubinemia from atazanavir.

Brand names
Reyataz (for atazanavir)Norvir (for ritonavir)Viread (for tenofovir disoproxil fumarate)
Other names
atazanavir sulfate + ritonavir + tenofovir disoproxil fumarate
02

Targets

CYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)Human immunodeficiency virus type 1 reverse transcriptase

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