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Interference with Bile Salt Export Pump Function Is a Susceptibility Factor for Human Liver Injury in Drug Development

Morgan, Ryan E., Trauner, Michael, van Staden, Carlo J., Lee, Paul H., Ramachandran, Bharath, Eschenberg, Michael, Afshari, Cynthia A., Qualls, Charles W., Lightfoot-Dunn, Ruth, Hamadeh, Hisham K.·2010·Toxicological Sciences
DOI 10.1093/toxsci/kfq269
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Abstract

The bile salt export pump (BSEP) is an efflux transporter, driving the elimination of endobiotic and xenobiotic substrates from hepatocytes into the bile. More specifically, it is responsible for the elimination of monovalent, conjugated bile salts, with little or no assistance from other apical transporters. Disruption of BSEP activity through genetic disorders is known to manifest in clinical liver injury such as progressive familial intrahepatic cholestasis type 2. Drug-induced disruption of BSEP is hypothesized to play a role in the development of liver injury for several marketed or withdrawn therapeutics. Unfortunately, preclinical animal models have been poor predictors of the liver injury associated with BSEP interference observed for humans, possibly because of interspecies differences in bile acid composition, differences in hepatobiliary transporter modulation or constitutive expression, as well as other mechanisms. Thus, a BSEP-mediated liver liability may go undetected until the later stages of drug development, such as during clinical trials or even postlicensing. In the absence of a relevant preclinical test system for BSEP-mediated liver injury, the toxicological relevance of available in vitro models to human health rely on the use of benchmark compounds with known clinical outcomes, such as marketed or withdrawn drugs. In this study, membrane vesicles harvested from BSEP-transfected insect cells were used to assess the activity of more than 200 benchmark com…

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Metadata

Authors
Morgan, R. E., Trauner, M., van Staden, C. J., Lee, P. H., Ramachandran, B., Eschenberg, M., Afshari, C. A., Qualls, C. W., Lightfoot-Dunn, R., & Hamadeh, H. K.
Venue
Toxicological Sciences
Publisher
Oxford University Press (OUP)
Published
2010-09-09
Volume
118
Issue
2
Pages
485-500
ISSN
  • 1096-6080
  • 1096-0929
DOI
10.1093/toxsci/kfq269
Cited by
325
References
4
Language
en

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