Drug intelligence / Profile preview

atazanavir + ritonavir + omeprazole

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

Overview

Atazanavir is a protease inhibitor used in combination with other antiretroviral agents, such as ritonavir, for the treatment of human immunodeficiency virus (HIV) infection. Ritonavir acts primarily as a pharmacokinetic enhancer by inhibiting cytochrome P450 3A4 (CYP3A4), thereby increasing plasma concentrations of coadministered protease inhibitors like atazanavir. Omeprazole is a proton pump inhibitor that reduces gastric acid secretion by irreversibly inhibiting the H+/K+ ATPase in gastric parietal cells. Atazanavir exhibits pH-dependent solubility; thus, concomitant use with omeprazole can significantly decrease its absorption and plasma concentration due to increased gastric pH. Clinical studies have shown that coadministration of standard doses of omeprazole with atazanavir/ritonavir leads to substantial reductions in atazanavir exposure, which may compromise antiviral efficacy[1][5][6][8]. This combination is generally not recommended unless no alternatives exist and strict dosing adjustments and monitoring are implemented.

Other names
ATV/rATVRTV
02

Targets

CYP3A4 (Cytochrome P450 3A4)ATP4A (Potassium–transporting ATPase alpha chain 1)PR (Progesterone receptor)

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