Drug intelligence / Profile preview

rosuvastatin + rifampin

Development stage
Phase 4
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination of two pharmaceutical drugs, rosuvastatin and rifampin. Rosuvastatin is a statin (HMG-CoA reductase inhibitor) used primarily to lower cholesterol and reduce cardiovascular risk by inhibiting the enzyme HMG-CoA reductase, which plays a central role in the production of cholesterol in the liver. It also has pleiotropic effects such as improving endothelial function and reducing inflammation. Rifampin is an antibiotic mainly used to treat tuberculosis and eliminate Neisseria meningitidis carriage; it works by binding to bacterial DNA-dependent RNA polymerase, thereby inhibiting RNA synthesis. When coadministered, there may be pharmacokinetic interactions due to rifampin's induction of hepatic enzymes and transporters; however, studies show that while individual responses vary, on average rosuvastatin exposure is not significantly altered by rifampin pretreatment[1][6][7]. Coadministration should be monitored for potential hepatotoxicity or muscle-related adverse effects.

02

Targets

PXR (Pregnane X receptor)rpoB (DNA-directed RNA polymerase subunit beta)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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