Drug intelligence / Profile preview

ezetimibe + simvastatin + niacin

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

Overview

Ezetimibe + simvastatin + niacin is a combination therapy used to treat high cholesterol and triglyceride levels in the blood, particularly in patients with hypercholesterolemia or at risk of cardiovascular disease. Ezetimibe acts as a dietary cholesterol absorption inhibitor, reducing the amount of cholesterol absorbed from the intestine. Simvastatin is an HMG-CoA reductase inhibitor (statin) that decreases endogenous cholesterol synthesis by inhibiting the rate-limiting enzyme in hepatic cholesterol production. Niacin (vitamin B3) lowers LDL-cholesterol and triglycerides while raising HDL-cholesterol by inhibiting hepatic diacylglycerol acyltransferase-2, decreasing VLDL synthesis, and reducing lipolysis in adipose tissue. This triple combination targets multiple pathways involved in lipid metabolism for comprehensive lipid control[1][2][4][5][8].

02

Targets

NPC1L1 (Niemann-pick C1-Like 1 transporter)HCAR2 (Hydroxycarboxylic acid receptor 2)DGAT2 (Hepatic diacylglycerol acyltransferase 2)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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