Drug intelligence / Profile preview

fluvastatin + ezetimibe

Development stage
Phase 4
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

Fluvastatin + ezetimibe is a combination of two cholesterol-lowering medications used to treat high blood cholesterol and reduce cardiovascular risk. Fluvastatin is an HMG-CoA reductase inhibitor (statin) that works by inhibiting the enzyme responsible for cholesterol synthesis in the liver, thereby lowering LDL ("bad") cholesterol and triglycerides while increasing HDL ("good") cholesterol[1][5][8]. Ezetimibe is a cholesterol absorption inhibitor that blocks the Niemann-Pick C1-like 1 (NPC1L1) protein on intestinal epithelial cells, reducing the absorption of dietary and biliary cholesterol from the small intestine[2][3][6]. The combination targets both endogenous production and exogenous absorption of cholesterol, providing an additive effect in lowering plasma lipid levels. This therapy is primarily indicated for hypercholesterolemia, mixed dyslipidemia, and prevention of cardiovascular events in patients at risk.

02

Targets

HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)NPC1L1 (Niemann-pick C1-Like 1 transporter)

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