Target intelligence / Profile preview

Bile Salt Export Pump (BSEP)

Target
BSEP
Molecular classification
Transporter, ATP-binding cassette transporter
01

Overview

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.

Other names
ABCB11ATP-binding cassette sub-family B member 11
02

Mechanism of action

Inhibition of bile salt export from hepatocytes into the bile canaliculi

03

Biological functions

Bile acid transportEnterohepatic circulation
04

Disease associations

Intrahepatic cholestasisDrug-induced liver injuryProgressive familial intrahepatic cholestasis type II
05

Safety considerations

HepatotoxicityDrug-induced liver injuryInterspecies differences in drug response
06

Interacting drugs

Pravastatin

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