Drug intelligence / Profile preview

statins + ezetimibe

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

Overview

Statins + ezetimibe is a fixed-dose combination therapy used to lower cholesterol and triglyceride levels in the blood. Statins (such as simvastatin, atorvastatin, or rosuvastatin) inhibit HMG-CoA reductase in the liver to reduce endogenous cholesterol synthesis. Ezetimibe selectively inhibits intestinal absorption of cholesterol by blocking the Niemann–Pick C1–like 1 (NPC1L1) protein on enterocytes. The combination provides dual inhibition of both cholesterol production and absorption, resulting in greater reductions in LDL-C than either agent alone. It is indicated for patients with hypercholesterolemia (including familial forms), those at high risk for atherosclerotic cardiovascular disease who do not reach lipid targets with statin monotherapy or cannot tolerate high-dose statin therapy[1][2][3][4][5]. Combination therapy has demonstrated improved lipid profiles and additional ASCVD risk reduction compared to statin monotherapy[2][3][5].

Brand names
VytorinRoszet
Other names
simvastatin + ezetimibeatorvastatin + ezetimiberosuvastatin + ezetimibe
02

Targets

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

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