Drug intelligence / Profile preview

pactimibe

Development stage
Discontinued
Lead developer
Daiichi Sankyo
Modality
Small Molecules
Administration
Oral
01

Overview

Pactimibe is a small molecule drug that acts as a dual inhibitor of acyl-coenzyme A:cholesterol acyltransferases (ACAT1 and ACAT2). It was developed by Daiichi Sankyo for the treatment of atherosclerosis and coronary heart disease. The drug works by inhibiting cholesterol absorption from the intestine, reducing cholesteryl ester formation in the liver and macrophages, enhancing cholesterol elimination from the body, and inhibiting secretion of very low density lipoprotein cholesterol from the liver. These mechanisms contribute to its hypocholesterolemic and anti-atherosclerotic effects. Clinical development reached up to phase III trials for atherosclerosis but was discontinued due to lack of efficacy on secondary endpoints compared to standard care[3][4][5][6].

Other names
pactimibaPactimibe [INN:BAN]Pactimibe free base(7-(2,2-Dimethylpropanamido)-4,6-dimethyl-1-octylindolin-5-yl)acetic acid
02

Targets

SOAT2 (Acyl-coenzyme A:cholesterol acyltransferase 2)ACAT1 (Acyl-coenzyme A:cholesterol O-acyltransferase 1)

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