Drug intelligence / Profile preview

implitapide

Development stage
Discontinued
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral
01

Overview

Implitapide is a small molecule inhibitor of the microsomal triglyceride transfer protein (MTP), which plays a critical role in the assembly and secretion of apolipoprotein B-containing lipoproteins. By inhibiting MTP, the drug prevents the formation of chylomicrons in the intestine and very low-density lipoproteins (VLDL) in the liver, effectively lowering plasma levels of low-density lipoprotein cholesterol (LDL-C) and triglycerides. It was primarily developed for the treatment of severe lipid disorders, including homozygous and heterozygous familial hypercholesterolemia and severe hypertriglyceridemia. Clinical development was conducted by Bayer and Medical Research Laboratories International, but the program was largely discontinued due to side effects common to the MTP inhibitor class, such as hepatic fat accumulation and gastrointestinal issues.

Other names
(2S)-2-cyclopentyl-2-{4-[(2,4-dimethyl-9H-pyrido[2,3-b]indol-9-yl)methyl]phenyl}-N-[(1S)-2-hydroxy-1-phenylethyl]ethanamide
02

Targets

MTTP (Microsomal triglyceride transfer protein large subunit)

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