Drug intelligence / Profile preview

rosuvastatin + BI 1323495

Development stage
Phase 1
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

Rosuvastatin + BI 1323495 is a combination of two investigational and approved agents. Rosuvastatin is an FDA-approved statin medication used to lower cholesterol and prevent cardiovascular events by inhibiting HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis. It increases hepatic LDL receptor expression, enhancing clearance of LDL from plasma[3][5][7]. BI 1323495 is an investigational small molecule developed by Boehringer Ingelheim, characterized as an inhibitor of P-glycoprotein (P-gp), organic anion transporting polypeptide 1B1 (OATP1B1), and breast cancer resistance protein (BCRP) in vitro[8]. Clinical trials have evaluated the safety, tolerability, pharmacokinetics, and pharmacodynamics of this combination in healthy volunteers and patients with non-cystic fibrosis bronchiectasis or for drug-drug interaction studies[2][4][8].

02

Targets

HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)ABCB1 (P-glycoprotein)ABCG2 (Breast cancer resistance protein)

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