Membrane transporters in drug development

Kathleen M. Giacomini, Shiew Mei Huang, Donald J. Tweedie, Leslie Z. Benet, Kim L.R. Brouwer, Xiaoyan Chu, Amber Dahlin, Raymond Evers, Volker Fischer, Kathleen M. Hillgren, Keith A. Hoffmaster, Toshihisa Ishikawa, Dietrich Keppler, Richard B. Kim, Caroline A. Lee, Mikko Niemi, Joseph W. Polli, Yuicchi Sugiyama, Peter W. Swaan, Joseph A. WareStephen H. Wright, Sook Wah Yee, MacIej J. Zamek-Gliszczynski, Lei Zhang

Research output: Contribution to journalReview articlepeer-review

2740 Scopus citations


Membrane transporters can be major determinants of the pharmacokinetic, safety and efficacy profiles of drugs. This presents several key questions for drug development, including which transporters are clinically important in drug absorption and disposition, and which in vitro methods are suitable for studying drug interactions with these transporters. In addition, what criteria should trigger follow-up clinical studies, and which clinical studies should be conducted if needed. In this article, we provide the recommendations of the International Transporter Consortium on these issues, and present decision trees that are intended to help guide clinical studies on the currently recognized most important drug transporter interactions. The recommendations are generally intended to support clinical development and filing of a new drug application. Overall, it is advised that the timing of transporter investigations should be driven by efficacy, safety and clinical trial enrolment questions (for example, exclusion and inclusion criteria), as well as a need for further understanding of the absorption, distribution, metabolism and excretion properties of the drug molecule, and information required for drug labelling.

Original languageEnglish (US)
Pages (from-to)215-236
Number of pages22
JournalNature Reviews Drug Discovery
Issue number3
StatePublished - Mar 2010

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery


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