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berberine + atorvastatin + rosuvastatin

Development stage: Preclinical
Lead developer: Pfizer
Modality: Small Molecules
Administration: Oral

Overview

A combination therapy consisting of berberine (a natural alkaloid) and two statin medications (atorvastatin and rosuvastatin). This combination potentially offers enhanced lipid-lowering effects through complementary mechanisms. Berberine promotes OATP1B1 expression and increases statin uptake by hepatocytes, while the statins inhibit HMG-CoA reductase. The combination may allow for lower statin doses while maintaining or improving efficacy in treating hyperlipidemia and reducing cardiovascular risk.

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)CYP3A4 (Cytochrome P450 3A4)ABCB1 (P-glycoprotein)NR1H3 (Liver X receptor beta)

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