SCH 45581

SCH 45581 is a small molecule cholesterol absorption inhibitor belonging to the 2-azetidinone class, developed by Schering-Plough. It was identified as a key metabolite of the earlier lead compound SCH 48461 and served as a critical structural template during the discovery program that eventually led to ezetimibe (SCH 58235). SCH 45581 exerts its effect by inhibiting the Niemann-Pick C1-Like 1 (NPC1L1) transport protein located on the apical membrane of enterocytes in the small intestine, thereby reducing the uptake of dietary and biliary cholesterol. Although it demonstrated potent hypocholesterolemic activity in animal models, it was not progressed to clinical use as further optimization led to the development of ezetimibe, which possesses superior metabolic stability and potency.

Other names

4-hydroxyphenyl analog of SCH 484614-hydroxy-SCH 48461