Drug intelligence / Profile preview

atazanavir + ritonavir + efavirenz

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

Overview

This is a combination of three antiretroviral drugs used in the treatment of HIV infection. Atazanavir is an azapeptide HIV-1 protease inhibitor that blocks the activity of the viral protease enzyme, preventing maturation of infectious virus particles. Ritonavir is also a protease inhibitor but is primarily used here as a pharmacokinetic booster to increase plasma concentrations of atazanavir by inhibiting CYP3A4-mediated metabolism. Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that binds directly to reverse transcriptase and inhibits its activity, thereby blocking viral RNA-dependent DNA polymerization. This combination targets different stages in the HIV replication cycle and may be used as part of highly active antiretroviral therapy regimens for people living with HIV[1][5][6].

Brand names
Reyataz (atazanavir)Norvir (ritonavir)Sustiva (efavirenz)
Other names
ATV (atazanavir)RTV (ritonavir)EFV (efavirenz)
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseCYP3A4 (Cytochrome P450 3A4)RYR2 (Ryanodine receptor 2)PR (Progesterone receptor)

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