Chapter 16. Drug-Induced Intrahepatic Cholestasis by Interaction with the Hepatic Bile Salt Export Pump (BSEP)

  1. Saura C. Sahu
  1. Christoph Funk,
  2. Johannes Noé,
  3. Renée Portmann,
  4. Rubén Alvarez-Sánchez,
  5. Florian Klammers,
  6. Christiane Lamy,
  7. Axel Paehler and
  8. Michael Pantze

Published Online: 27 FEB 2008

DOI: 10.1002/9780470516751.ch16



How to Cite

Funk, C., Noé, J., Portmann, R., Alvarez-Sánchez, R., Klammers, F., Lamy, C., Paehler, A. and Pantze, M. (2007) Drug-Induced Intrahepatic Cholestasis by Interaction with the Hepatic Bile Salt Export Pump (BSEP), in Hepatotoxicity (ed S. C. Sahu), John Wiley & Sons, Ltd, Chichester, UK. doi: 10.1002/9780470516751.ch16

Editor Information

  1. Division of Toxicology, Office of Toxicology, Office of Applied Research and Safety Assessment, Center for Food Safety and Applied Nutrition, US Food and Drug Administration, 8301 Muirkirk Road, Laurel, MD 20708, USA

Author Information

  1. F. Hoffman-La Roche Ltd, Non-Clinical Development – Drug Safety, PRBN-D 69/154, 4070 Basel, Switzerland

Publication History

  1. Published Online: 27 FEB 2008
  2. Published Print: 14 DEC 2007

ISBN Information

Print ISBN: 9780470057162

Online ISBN: 9780470516751



  • polymorphic expression;
  • multifactorial toxicities;
  • covalent binding and immune-mediated responses;
  • drug metabolizing enzymes;
  • monooxygenases and glucuronosyl transferases;
  • cellular uptake carriers and cellular exporters;
  • hepatobiliary transport functions;
  • intrahepatic cholestasis;
  • cholestatic drugs;
  • cellular necrosis and mitochondrial dysfunction


This chapter contains sections titled:

  • Introduction

  • Cholestatic Potential of Selected Drugs

  • Species Differences in Bsep/BSEP Inhibition

  • Regulation of BSEP Expression

  • Genetic Origin of Intrahepatic Cholestasis

  • Addressing BSEP Inhibition in Drug Discovery and Development to Reduce the Cholestatic Properties of New Molecular Entities

  • Abbreviations

  • References