Drug intelligence / Profile preview

ritonavir + rosuvastatin

Development stage
Unknown
Lead developer
Juan A. Arnaiz
Modality
Small Molecules
Administration
Oral
01

Overview

This combination therapy involves the co-administration of ritonavir, a pharmacokinetic enhancer and HIV protease inhibitor, and rosuvastatin, a synthetic lipid-lowering agent. Ritonavir is a peptidomimetic inhibitor of the HIV-1 protease and a potent inhibitor of the cytochrome P450 3A4 (CYP3A4) enzyme; it is primarily used to 'boost' the plasma concentrations of other protease inhibitors in antiretroviral therapy (ART). Rosuvastatin is a statin that competitively inhibits 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme in cholesterol biosynthesis, thereby reducing LDL cholesterol and total cholesterol levels. This specific regimen was evaluated in a Phase 4 clinical trial led by Juan A. Arnaiz to determine if adding rosuvastatin to an existing ritonavir-boosted protease inhibitor regimen is an effective alternative to switching the protease inhibitor for managing hypercholesterolemia in HIV-infected patients, a common side effect of certain ART components.

Brand names
NorvirCrestor
02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)ABCG2 (Breast cancer resistance protein)CYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)

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