The human ATP dependent efflux transporter BSEP (Bile Salt Export Pump) is the major canalicular bile salt export pump responsible for active transport of bile salts across the hepatocyte canalicular membrane into bile. Mutations in the BSEP gene are associated with cholestatic liver diseases of varying severity, but also BSEP inhibition by a drug or its metabolites can lead to cholestasis and drug-induced liver injury (DILI).

Main localization:
Transporter assay:
Vesicle-based transporter assay (potential substrates and inhibitors)
Probe substrates:
Probe inhibitors:
Cyclosporine, glibenclamide, rifampicin
Regulatory relevance:
EMA guidance
Important interacting drugs:
Pravastatin, atorvastatin, cerivastatin, clofazimine, cyclosporine, glibenclamide, reserpine, rifampicin, troglitazone, valinomycin

Concentration dependent inhibition of hBSEP-mediated Taurocholate uptake by the probe inhibitor Cyclosporine

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