In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.

@article{Dawson2012InVI,
  title={In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.},
  author={Sarah Dawson and Simone Stahl and Nikki R. Paul and Jane Barber and J. Gerald Kenna},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2012},
  volume={40 1},
  pages={130-8}
}
Inhibition of the activity of the human bile salt export pump (BSEP: ABCB11) has been proposed to play a role in drug-induced liver injury (DILI). To enhance understanding of the relationship between BSEP inhibition and DILI, inhibition of human BSEP (hBSEP) and its rat ortholog (rBsep) by 85 pharmaceuticals was investigated in vitro. This was explored using assays that quantified inhibition of ATP-dependent [(3)H]taurocholate uptake into inverted plasma membrane vesicles from Sf21 insect cells… CONTINUE READING
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