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Bile Salt Export Pump (BSEP), encoded by the ABCB11 gene, is a critical ATP-dependent efflux transporter located on the canalicular membrane of hepatocytes. It facilitates the export of conjugated bile acids from hepatocytes into bile, driving bile formation and enterohepatic circulation. Impairment or inhibition of BSEP function leads to intrahepatic cholestasis and drug-induced liver injury. BSEP expression is regulated by several nuclear receptors, including FXR, AMPK, LRH-1 and Nrf2. Several marketed drugs have been implicated in BSEP inhibition and subsequent liver injury.
Inhibition of bile salt export from hepatocytes into the bile canaliculi
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