High Quality 99% White Powder Ezetimibe CAS 163222-33-1

Ezetimibe More Info

Ezetimibe is a lipid-lowering medication primarily used to manage hypercholesterolemia by selectively inhibiting intestinal cholesterol absorption.

Mechanism of Action

Ezetimibe works by targeting the Niemann-Pick C1-Like 1 (NPC1L1) sterol transporter located at the brush border of the small intestine. It inhibits the interaction between the NPC1L1/cholesterol complex and the clathrin/AP2 endocytic machinery, thereby preventing the endocytosis and uptake of cholesterol into enterocytes. This leads to reduced intestinal absorption of dietary and biliary cholesterol without affecting the absorption of fat-soluble vitamins or triglycerides.
The reduced cholesterol absorption decreases the delivery of cholesterol to the liver, which in turn increases hepatic clearance of cholesterol from the blood, lowering plasma levels of total cholesterol, low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (apo B), and non-high-density lipoprotein cholesterol (non-HDL-C). Ezetimibe typically lowers LDL-C by 13% to 20% when used as monotherapy and has additive effects when combined with statins or fenofibrate.

Applications

Primary hyperlipidemia (high cholesterol)
Mixed hyperlipidemia
Homozygous familial hypercholesterolemia (HoFH)
Homozygous sitosterolemia (phytosterolemia)
Adjunct therapy with statins or fenofibrate to enhance cholesterol lowering
Used in fixed-dose combinations with statins such as simvastatin or rosuvastatin for enhanced effect.

Routes of Administration and Dosage

Route: Oral tablets
Dose: Usually 10 mg once daily
Can be taken with or without food; food does not significantly affect the extent of absorption, though high-fat meals can increase peak plasma concentration by about 38%.
When combined with bile acid sequestrants, ezetimibe should be taken at least 2 hours before or 4 hours after the sequestrant to avoid interference with absorption.