2017 APRIL

Hepatic transporters in drug development and discovery

  • Toxicol Lett. 2016;263:58-67. Both cholestatic and steatotic drugs trigger extensive alterations in the mRNA level of biliary transporters in rat hepatocytes: Application to develop new predictive biomarkers for early drug development. Donato MT, López-Riera M2, Castell JV1, Gómez-Lechón MJ3, Jover R4. PubMed
  • Drug Metab Pharmacokinet. 2016;31:333-339. Appropriate risk criteria for OATP inhibition at the drug discovery stage based on the clinical relevancy between OATP inhibitors and drug-induced adverse effect. Nakakariya M, Goto A, Amano N. PubMed
  • Expert Opin Drug Metab Toxicol. 2016;12:201-16. Hepatic drug transporters: the journey so far. Riley RJ, Foley SA, Barton P, Soars MG, Williamson B. PubMed
  • Drug Metab Dispos. 2016;44:83-101. Key findings from preclinical and clinical Drug interaction studies presented in New Drug and Biological License Applications approved by the Food and Drug Administration in 2014. Yu J, Ritchie TK, Zhou Z, Ragueneau-Majlessi I. PubMed
  • J Clin Pharmacol. 2016;56 Suppl 7:S99-S109. Transporter-enzyme interplay: Deconvoluting effects of hepatic transporters and enzymes on drug disposition using static and dynamic mechanistic models. Varma MV, El-Kattan AF. PubMed
  • Curr Pharm Des. 2016;22:5817-5829. Importance of ABC transporters in drug development. Benadiba M1, Maor Y. PubMed
  • Clin Pharmacol Ther. 2016;99:224-34. Mechanistic understanding of the nonlinear pharmacokinetics and intersubject variability of simeprevir: A PBPK-guided drug development approach. Snoeys J, Beumont M, Monshouwer M, Ouwerkerk-Mahadevan S. PubMed
  • Clin Pharmacol Ther. 2016;100:479-488. Imaging. Imaging transporters: Transforming diagnostic and therapeutic development. Mann A, Han H, Eyal S. PubMed
  • Curr Drug Targets. 2015;16:582-91. Imaging. PET and SPECT imaging for the acceleration of anti-cancer drug development. Hillyar CR, Knight JC, Vallis KA, Cornelissen B. PubMed
  • Pharm Res. 2015;32:3785-802. Predicting clearance mechanism in drug discovery: Extended Clearance Classification System (ECCS). Varma MV, Steyn SJ, Allerton C, El-Kattan AF. PubMed
  • Methods Mol Biol. 2014;1113:471-83. Case study 5. Deconvoluting hyperbilirubinemia: differentiating between hepatotoxicity and reversible inhibition of UGT1A1, MRP2, or OATP1B1 in drug development. Templeton I, Eichenbaum G, Sane R, Zhou J. PubMed
  • Future Med Chem. 2014;6:1995-2012. Practical permeability-based hepatic clearance classification system (HepCCS) in drug discovery. Fan PW, Song Y, Berezhkovskiy LM, Cheong J, Plise EG, Khojasteh SC. PubMed
  • Clin Pharmacokinet. 2014;53:659-78. Prediction of pharmacokinetics and drug-drug interactions when hepatic transporters are involved. Li R, Barton HA, Varma MV. PubMed
  • Expert Opin Drug Discov. 2014;9:873-90. In vitro and in vivo approaches to characterize transporter-mediated disposition in drug discovery. Feng B, Varma MV, Costales C, Zhang H, Tremaine L. PubMed
  • Curr Pharm Des. 2014;20:1577-94. Beyond the ITC white paper: emerging sciences in drug transporters and opportunities for drug development. Lai Y, Hsiao P. PubMed
  • Clin Pharmacol Ther. 2013;94:3-9. Transporters in drug development and clinical pharmacology. Giacomini KM, Huang SM. PubMed
  • Mol Pharm. 2013;10:4207-15. Quantitative prediction of renal transporter-mediated clinical drug-drug interactions. Feng B, Hurst S, Lu Y, Varma MV, Rotter CJ, El-Kattan A, Lockwood P, Corrigan B. PubMed
  • Curr Top Med Chem. 2013;13:857-66. Medicinal chemistry design principles for liver targeting through OATP transporters. Tu M, Mathiowetz AM, Pfefferkorn JA, Cameron KO, Dow RL, Litchfield J, Di L, Feng B, Liras S. PubMed
  • Expert Opin Drug Metab Toxicol. 2013;9:459-72. Model-based approaches to predict drug-drug interactions associated with hepatic uptake transporters: preclinical, clinical and beyond. Barton HA, Lai Y, Goosen TC, Jones HM, El-Kattan AF, Gosset JR, Lin J, Varma MV. PubMed
  • Curr Pharm Des. 2014;20:793-807. ABC transporters in multidrug resistance and pharmacokinetics, and strategies for drug development. Choi YH, Yu AM. PubMed
  • Nucl Med Biol. 2013;40:643-50. Imaging. Drugs interacting with organic anion transporter-1 affect uptake of Tc-99m-mercaptoacetyl-triglycine (MAG3) in the human kidney: therapeutic drug interaction in Tc-99m-MAG3 diagnosis of renal function and possible application of Tc-99m-MAG3 for drug development. Takahara N, Saga T, Inubushi M, Kusuhara H, Seki C, Ito S, Oyama N, Yokoyama O, Sugiyama Y, Fujibayashi Y. PubMed
  • Clin Pharmacol Ther. 2013;94:33-6. Imaging in the study of membrane transporters. Kusuhara H. PubMed
  • Clin Pharmacol Ther. 2012;92:584-98. Understanding the critical disposition pathways of statins to assess drug-drug interaction risk during drug development: it's not just about OATP1B1. Elsby R, Hilgendorf C, Fenner K. PubMed
  • Eur J Med Chem. 2012;57:441-8. Mechanistic insights from comparing intrinsic clearance values between human liver microsomes and hepatocytes to guide drug design. Di L, Keefer C, Scott DO, Strelevitz TJ, Chang G, Bi YA, Lai Y, Duckworth J, Fenner K, Troutman MD, Obach RS. PubMed
  • Adv Pharmacol. 2012;63:1-42. Membrane transporters in drug development. Keogh JP. PubMed
  • Expert Opin Drug Metab Toxicol. 2012;8:1131-55. Probe ADME and test hypotheses: a PATH beyond clearance in vitro-in vivo correlations in early drug discovery. Bell LC, Wang J. PubMed
  • Expert Opin Drug Metab Toxicol. 2012;8:723-43. Impact of drug transporter pharmacogenomics on pharmacokinetic and pharmacodynamic variability - considerations for drug development. Lai Y, Varma M, Feng B, Stephens JC, Kimoto E, El-Kattan A, Ichikawa K, Kikkawa H, Ono C, Suzuki A, Suzuki M, Yamamoto Y, Tremaine L. PubMed
  • Biopharm Drug Dispos. 2012;33:179-94. Predicting human hepatic clearance from in vitro drug metabolism and transport data: a scientific and pharmaceutical perspective for assessing drug-drug interactions. Camenisch G, Umehara K. PubMed
  • Drug Metab Dispos. 2012;40:1085-92. In vitro evaluation of hepatic transporter-mediated clinical drug-drug interactions: hepatocyte model optimization and retrospective investigation. Bi YA, Kimoto E, Sevidal S, Jones HM, Barton HA, Kempshall S, Whalen KM, Zhang H, Ji C, Fenner KS, El-Kattan AF, Lai Y. PubMed
  • Drug Metab Lett. 2012;6:285-91. A transcellular assay to assess the P-gp inhibition in early stage of drug development. Taur JS, Schuck EL, Wong NY. PubMed
  • Methods Mol Biol. 2010;637:1-21. Membrane transporters and drug development: relevance to pharmacogenomics, nutrigenomics, epigenetics, and systems biology. Yan Q. PubMed
  • Nat Rev Drug Discov. 2010;9:215-36. Membrane transporters in drug development. International Transporter Consortium, Giacomini KM, Huang SM, Tweedie DJ, Benet LZ, Brouwer KL, Chu X, Dahlin A, Evers R, Fischer V, Hillgren KM, Hoffmaster KA, Ishikawa T, Keppler D, Kim RB, Lee CA, Niemi M, Polli JW, Sugiyama Y, Swaan PW, Ware JA, Wright SH, Yee SW, Zamek-Gliszczynski MJ, Zhang L. PubMed
  • Curr Drug Discov Technol. 2010;7:188-98. Hepatocytes as a tool in drug metabolism, transport and safety evaluations in drug discovery. Sahi J, Grepper S, Smith C. PubMed
  • Eur J Pharm Sci. 2010;40:282-8. Screening of OATP1B1/3 and OCT1 inhibitors in cryopreserved hepatocytes in suspension. Badolo L, Rasmussen LM, Hansen HR, Sveigaard C. PubMed
  • Clin Exp Pharmacol Physiol. 2010;37:115-20. Multidrug resistance-associated proteins and implications in drug development. Liu YH, Di YM, Zhou ZW, Mo SL, Zhou SF. PubMed
  • Mol Pharm. 2009;6:1662-77. Impact of hepatic uptake transporters on pharmacokinetics and drug-drug interactions: use of assays and models for decision making in the pharmaceutical industry. Soars MG, Webborn PJ, Riley RJ. PubMed
  •  Curr Med Chem. 2008;15:1981-2039. Substrates and inhibitors of human multidrug resistance associated proteins and the implications in drug development. Zhou SF, Wang LL, Di YM, Xue CC, Duan W, Li CG, Li Y. PubMed