Drug intelligence / Profile preview

protease inhibitor + ritonavir

Development stage
Unknown
Lead developer
Abbott
Modality
Small Molecules
Administration
Oral
01

Overview

This refers to a combination therapy consisting of any HIV protease inhibitor co-administered with ritonavir. Ritonavir is itself a protease inhibitor but is primarily used at low doses as a pharmacokinetic booster. It potently inhibits the cytochrome P450 3A4 (CYP3A4) enzyme, thereby increasing the plasma concentrations and half-life of other co-administered protease inhibitors such as lopinavir, atazanavir, darunavir, indinavir, or saquinavir. This boosting effect enhances the efficacy and durability of antiretroviral regimens for HIV/AIDS by maintaining higher drug levels and reducing dosing frequency. The combination is widely used in antiretroviral therapy (ART) for HIV infection and has also been utilized in some antiviral regimens for COVID-19 (e.g., nirmatrelvir/ritonavir). Common side effects include gastrointestinal disturbances, hepatotoxicity, lipid abnormalities, and significant drug-drug interactions due to CYP3A4 inhibition[2][4][6].

Other names
protease inhibitor + ritonavirPI/rboosted protease inhibitor
02

Targets

CYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)

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