Drug intelligence / Profile preview

lomitapide + ezetimibe

Development stage
Phase 2
Lead developer
Chiesi
Modality
Small Molecules
Administration
Oral
01

Overview

lomitapide + ezetimibe is an investigational combination therapy developed by Aegerion Pharmaceuticals for the treatment of hyperlipidemia and moderate hypercholesterolemia. Lomitapide (AEGR-733) is a small molecule inhibitor of microsomal triglyceride transfer protein (MTP), which is essential for the assembly and secretion of apolipoprotein B-containing lipoproteins, such as VLDL in the liver and chylomicrons in the intestine. Ezetimibe is a selective cholesterol absorption inhibitor that targets the Niemann-Pick C1-Like 1 (NPC1L1) protein in the small intestine. By combining these two distinct mechanisms—reducing the production of lipoproteins and inhibiting the absorption of dietary and biliary cholesterol—the therapy aims to achieve additive reductions in LDL-cholesterol levels. Clinical evaluation has also focused on the combination's safety profile regarding hepatic fat accumulation.

Other names
AEGR-733 and ezetimibeAEGR733 and ezetimibeAEGR 733 and ezetimibelomitapide and ezetimibe
02

Targets

MTTP (Microsomal triglyceride transfer protein large subunit)NPC1L1 (Niemann-pick C1-Like 1 transporter)

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