SCH-48461

SCH-48461 is a small molecule cholesterol absorption inhibitor developed by Schering-Plough Corporation. It belongs to the 2-azetidinone chemical class and functions by inhibiting the Niemann-Pick C1-like protein 1 (NPC1L1), which is the primary biological target responsible for the intestinal uptake of dietary and biliary cholesterol. SCH-48461 was the first compound in its class to enter clinical development and served as the prototypical precursor to the more potent successor, ezetimibe. In clinical trials, it demonstrated significant efficacy in reducing LDL cholesterol, total cholesterol, and apolipoprotein B levels. Although it reached Phase II clinical trials for the treatment of primary hypercholesterolemia, its development was ultimately discontinued in favor of ezetimibe.

Other names

(3R,4S)-1,4-bis-(4-methoxyphenyl)-3-(3-phenylpropyl)-2-azetidinone