SC-435

SC-435 is a potent, minimally absorbed, small-molecule inhibitor of the apical sodium-dependent bile acid transporter (ASBT), also known as the ileal bile acid transporter (IBAT). Originally developed by Searle (later Pfizer) and subsequently investigated by Satiogen, Lumena, Shire, and Mirum Pharmaceuticals, SC-435 acts locally in the gastrointestinal tract to block the reabsorption of bile acids in the terminal ileum. By interrupting the enterohepatic circulation of bile acids, SC-435 increases fecal bile acid excretion, depletes the systemic bile acid pool, and stimulates de novo bile acid synthesis from cholesterol in the liver. This mechanism has been explored preclinically for the treatment of hypercholesterolemia, atherosclerosis, type 2 diabetes, obesity, non-alcoholic fatty liver disease (NAFLD/NASH), and cholestatic liver diseases such as sclerosing cholangitis.

Other names

1-[4-[4-[(4R,5R)-3,3-dibutyl-7-(dimethylamino)-2,3,4,5-tetrahydro-4-hydroxy-1,1-dioxido-1-benzothiepin-5-yl]phenoxy]butyl]-4-aza-1-azoniabicyclooctane methanesulfonateSC-435 mesylateSC435 mesylateSC 435 mesylate