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Cyclobutyrol is a small molecule choleretic agent used in bile therapy. It increases bile flow while uniquely inhibiting the secretion of biliary lipids, specifically cholesterol and phospholipids, without affecting bile acid secretion. This effect is believed to be due to an uncoupling of cholesterol and phospholipid secretion from that of bile acids at the level of the canalicular membrane in hepatocytes. Cyclobutyrol also depresses biliary outputs of certain canalicular membrane enzymes such as 5'-nucleotidase and alkaline phosphodiesterase I[2][3][10]. Its primary clinical investigation has been for disorders involving bile composition or flow.
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