Drug intelligence / Profile preview

rosuvastatin + darunavir + ritonavir

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

Overview

This is a combination of three small molecule drugs: - **Rosuvastatin** is an HMG-CoA reductase inhibitor (statin) used to lower cholesterol and triglycerides in the blood. It works by inhibiting the enzyme HMG-CoA reductase, which plays a central role in the production of cholesterol. - **Darunavir** is an HIV-1 protease inhibitor used as part of antiretroviral therapy for HIV infection. It prevents viral replication by inhibiting the protease enzyme necessary for processing viral polyproteins. - **Ritonavir** is also an HIV-1 protease inhibitor but is primarily used at low doses as a pharmacokinetic enhancer ("booster") to increase plasma concentrations of other protease inhibitors like darunavir by inhibiting cytochrome P450 3A4 (CYP3A4). When coadministered, darunavir/ritonavir significantly increases plasma levels of rosuvastatin due to inhibition of drug transporters and metabolic enzymes, potentially increasing risk for adverse effects such as myopathy or liver toxicity. The lipid-lowering efficacy of rosuvastatin may be blunted when combined with darunavir/ritonavir[1][2][5]. This combination should be used with caution and under close monitoring.

Other names
darunavir/ritonavir/rosuvastatin combination
02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)ABCG2 (Breast cancer resistance protein)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)CYP3A4 (Cytochrome P450 3A4)ABCB1 (P-glycoprotein)PR (Progesterone receptor)

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