Drug intelligence / Profile preview

ezetimibe + fenofibrate

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

Overview

Ezetimibe + fenofibrate is a fixed-dose combination of two lipid-lowering agents used primarily for the treatment of mixed hyperlipidemia and high triglycerides. Ezetimibe acts as a cholesterol absorption inhibitor by selectively blocking the Niemann-Pick C1-Like 1 (NPC1L1) protein in the small intestine, thereby reducing intestinal uptake of dietary and biliary cholesterol. Fenofibrate is a peroxisome proliferator-activated receptor alpha (PPAR-alpha) agonist that increases tissue lipoprotein lipase activity and enhances the breakdown of triglyceride-rich particles such as very low-density lipoproteins (VLDL). The combination provides additive or synergistic effects on lowering LDL cholesterol, non-HDL cholesterol, total cholesterol, apo B, and triglycerides while increasing HDL cholesterol. It is approved for use in patients with mixed dyslipidemia who require both LDL-C and triglyceride reduction[2][5][6]. Clinical studies have shown that this combination improves lipid profiles more effectively than either agent alone[4][5]. Common side effects include gastrointestinal symptoms and muscle pain; there may be an increased risk of cholelithiasis when used together[8].

Brand names
EzefenoStanlip EZFibral EZ
Other names
fenofibrate + ezetimibefenofibrate/ezetimibe
02

Targets

NPC1L1 (Niemann-pick C1-Like 1 transporter)PPARA (Peroxisome proliferator-activated receptor alpha)

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