Drug intelligence / Profile preview

lomitapide + fenofibrate

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

Overview

Lomitapide + fenofibrate is a combination of two lipid-lowering agents used to manage severe dyslipidemias. Lomitapide is a small molecule inhibitor of microsomal triglyceride transfer protein (MTP), which blocks the assembly and secretion of apolipoprotein B-containing lipoproteins in the liver and intestines. This results in reduced production of very low-density lipoprotein (VLDL) and chylomicrons, leading to lower plasma levels of LDL cholesterol and triglycerides[3][5][6]. It is primarily indicated for homozygous familial hypercholesterolemia (HoFH). Fenofibrate is a fibrate that acts as an agonist at peroxisome proliferator-activated receptor alpha (PPARα), increasing lipolysis by activating lipoprotein lipase and reducing apoprotein C-III. This leads to decreased levels of LDL cholesterol and triglycerides while raising HDL cholesterol[2]. The combination may be considered in patients with severe or refractory mixed dyslipidemia under specialist supervision.

02

Targets

PPARA (Peroxisome proliferator-activated receptor alpha)MTTP (Microsomal triglyceride transfer protein large subunit)

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