The role of hepatic transporters in drug elimination

Expert Opinion on Drug Metabolism & Toxicology
Christoph Funk

Abstract

Hepatic drug transporters of the solute carrier (OATPs, OAT2, OCT1, NTCP) and ABC transporter superfamilies (MDR1, MRPs, BCRP, BSEP) can significantly modulate drug ADME routes. The currently available literature was reviewed with focus on hepatic drug transporters, related drug-drug interactions and available tools for transporter assessment and extrapolation to in vivo. Hepatic drug transporters have gained additional importance in drug clearance by optimization for basic DMPK properties early on in drug research. However, the lack of selective substrates and inhibitors, proper assessment of the kinetic properties due to interfering passive permeability and multiple binding sites, as well as endogenous transporters present in many cellular assays, are some of the hurdles in studying active drug transport processes. Therefore, data from these in vitro assays have to be carefully evaluated to allow sound extrapolation to the in vivo situation.

References

May 10, 1991·Deutsche medizinische Wochenschrift·U SpreckelsenH Haacke
Jan 1, 1994·Advances in Enzyme Regulation·M BöhmeD Keppler
Apr 1, 1996·Pharmaceutical Research·M YamazakiY Sugiyama
Apr 1, 1996·Diabetes Care·N KrivoyG Alroy
May 1, 1996·Seminars in Liver Disease·B Hagenbuch, P J Meier
Oct 1, 1996·Clinical and Experimental Pharmacology & Physiology·A M Evans
Apr 1, 1997·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·J A Silverman, D Schrenk
Aug 1, 1997·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·Y BacqF Dubois
Oct 22, 1998·The New England Journal of Medicine·M TraunerJ L Boyer
Mar 31, 1999·Journal of Biochemical and Molecular Toxicology·E G Schuetz, A H Schinkel
Jul 14, 1999·Toxicology Letters·P ZimniakY C Awasthi
Aug 28, 1999·Gastroenterology·C M Rodrigues, C J Steer
Oct 16, 1999·Journal of Controlled Release : Official Journal of the Controlled Release Society·L Z BenetV J Wacher
Nov 24, 1999·Free Radical Biology & Medicine·D Keppler
Mar 23, 2000·Journal of Hepatology·G A Kullak-UblickG Paumgartner
Aug 17, 2000·Journal of the National Cancer Institute·P BorstJ Wijnholds
Aug 23, 2000·Pflügers Archiv : European journal of physiology·T SekineH Endou
Oct 19, 2000·Journal of the National Cancer Institute·J W JonkerA H Schinkel
Nov 15, 2000·Seminars in Liver Disease·D Keppler, J König
Nov 15, 2000·Seminars in Liver Disease·G A Kullak-UblickP J Meier
Feb 17, 2001·Clinical Pharmacology and Therapeutics·D DürrK Fattinger
Mar 10, 2001·Clinics in Liver Disease·G A Kullak-Ublick, P J Meier
Aug 2, 2001·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·G T TuckerS M Huang
Aug 2, 2001·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·M G Donner, D Keppler
Aug 18, 2001·BMJ : British Medical Journal·F Charatan
Sep 25, 2001·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·A Ayrton, P Morgan
Feb 5, 2002·Annual Review of Physiology·Peter J Meier, B Stieger
May 8, 2002·British Journal of Clinical Pharmacology·Siegfried DrescherMartin F Fromm
Jul 11, 2002·Biochemical Pharmacology·Konrad A BodeDietrich Keppler
Oct 3, 2002·Annual Review of Pharmacology and Toxicology·Matthias SchwabMartin F Fromm
Oct 31, 2002·Gastroenterology·Johannes NoéPeter J Meier
Oct 31, 2002·Advanced Drug Delivery Reviews·Martin F Fromm
Dec 31, 2002·Toxicology·Yukio KatoYuichi Sugiyama
Dec 31, 2002·Toxicology·Richard B Kim
Jan 22, 2003·Advanced Drug Delivery Reviews·Jiunn H Lin

❮ Previous
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Citations

Nov 26, 2009·Journal of Pharmacokinetics and Pharmacodynamics·Agnès PoirierThierry Lavé
Dec 23, 2011·The Journal of Pharmacology and Experimental Therapeutics·Karelle MénochetAleksandra Galetin
Nov 15, 2012·Drug Metabolism and Pharmacokinetics·Andrée-Anne BoivinMichel Roger
Apr 11, 2012·International Journal of Molecular Sciences·Katharine BriggsJörg D Wichard
Nov 16, 2013·Toxicological Sciences : an Official Journal of the Society of Toxicology·Philip M E ProbertMatthew C Wright
Apr 17, 2014·European Journal of Drug Metabolism and Pharmacokinetics·Wen Jin HuaChen Yan
Dec 24, 2009·Drug Metabolism Reviews·Bruno Stieger
Feb 2, 2013·Drug Metabolism Reviews·Eva RamboerMathieu Vinken
Mar 29, 2014·Drug Metabolism Reviews·Ursula Gundert-RemyPeter H Roos
Sep 30, 2009·Expert Opinion on Drug Metabolism & Toxicology·Olivier Fardel, Marc Le Vée
Aug 12, 2009·Expert Opinion on Drug Metabolism & Toxicology·Edmund Jon Deoon LeeLie Michael George Limenta
Jul 16, 2009·Drug Metabolism Reviews·Margherita Strolin BenedettiJean-Baptiste Watelet
Jul 23, 2009·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·E FlobyA-K Sohlenius-Sternbeck
Mar 20, 2013·Molecular Aspects of Medicine·Hermann Koepsell
Feb 12, 2013·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Gregory NoelOlivier Fardel
Oct 16, 2015·Biochemical Pharmacology·Abdullah MayatiOlivier Fardel
Nov 26, 2009·Chemistry & Biodiversity·Agnès PoirierThierry Lavé
Aug 11, 2011·British Journal of Pharmacology·K ManderyM F Fromm
Mar 5, 2010·Fundamental & Clinical Pharmacology·Marc Le VeeOlivier Fardel
Jan 28, 2014·Journal of Biochemical and Molecular Toxicology·Simon BucherOlivier Fardel
Dec 25, 2012·Biochemical and Biophysical Research Communications·Geun Hye JangJi Ha Choi
Nov 24, 2011·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Jian Yin, Qin Meng
Nov 15, 2011·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Katherine S FennerHugh A Barton
Apr 12, 2015·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Marc Le VeeOlivier Fardel
Jul 16, 2013·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Marc Le VeeOlivier Fardel
Oct 1, 2013·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Erik SjögrenHans Lennernäs
Dec 19, 2009·Clinical Pharmacology and Therapeutics·S-M HuangK M Giacomini
Jul 8, 2016·Journal of Clinical Pharmacology·Vikram Arya, Jennifer J Kiser
Dec 15, 2015·Biopharmaceutics & Drug Disposition·Seung Jun YangHyo-Kyung Han
Dec 31, 2016·Pharmaceutics·Elodie JouanOlivier Fardel
Apr 12, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Mariline GameiroFernando Remião
Mar 3, 2018·Basic & Clinical Pharmacology & Toxicology·Yu ChenChunhua Xia
Nov 26, 2009·Chemistry & Biodiversity·Christopher Kohl
Sep 18, 2010·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Hayley S BrownJ Brian Houston
Aug 8, 2009·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Marc Le VeeOlivier Fardel

❮ Previous
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