Drug-induced perturbations of the bile acid pool, cholestasis, and hepatotoxicity: mechanistic considerations beyond the direct inhibition of the bile salt export pump.

@article{Rodrigues2014DruginducedPO,
  title={Drug-induced perturbations of the bile acid pool, cholestasis, and hepatotoxicity: mechanistic considerations beyond the direct inhibition of the bile salt export pump.},
  author={A. David Rodrigues and Yurong Lai and Mary Ellen Cvijic and Lisa Elkin and Tatyana A Zvyaga and Matthew G. Soars},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2014},
  volume={42 4},
  pages={566-74}
}
The bile salt export pump (BSEP) is located on the canalicular plasma membrane of hepatocytes and plays an important role in the biliary clearance of bile acids (BAs). Therefore, any drug or new chemical entity that inhibits BSEP has the potential to cause cholestasis and possibly liver injury. In reality, however, one must consider the complexity of the BA pool, BA enterohepatic recirculation (EHR), extrahepatic (renal) BA clearance, and the interplay of multiple participant transporters and… CONTINUE READING

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