Transporters in Drug Development

Discovery, Optimization, Clinical Study and Regulation

  • Yuichi Sugiyama
  • Bente Steffansen

Part of the AAPS Advances in the Pharmaceutical Sciences Series book series (AAPS, volume 7)

Table of contents

  1. Front Matter
    Pages i-xiii
  2. Bente Steffansen, Carsten Uhd Nielsen, Birger Brodin
    Pages 1-22
  3. Bente Steffansen, Anne Sophie Grandvuinet
    Pages 23-35
  4. Per Artursson, Pär Matsson, Maria Karlgren
    Pages 37-65
  5. Hiroyuki Kusuhara, Kenta Yoshida, Yuichi Sugiyama
    Pages 67-97
  6. Larissa M. Balogh, Yurong Lai
    Pages 99-119
  7. Sibylle Neuhoff, Lu Gaohua, Howard Burt, Masoud Jamei, Linzhong Li, Geoffrey T. Tucker et al.
    Pages 155-177
  8. Ikumi Tamai, Takeo Nakanishi
    Pages 179-199
  9. Kyunghee Yang, Kathleen Köck, Kim L. R. Brouwer
    Pages 201-233
  10. Frans G. M. Russel, Rosalinde Masereeuw
    Pages 235-256
  11. Mitchell E. Taub, Naoki Ishiguro, Olaf Schaefer, Donald J. Tweedie
    Pages 285-307
  12. Yuichi Sugiyama, Bente Steffansen
    Pages E1-E1
  13. Back Matter
    Pages 309-317

About this book


Transporters in Drug Development examines how membrane transporters can be dealt with in academic-industrial drug discovery and pharmaceutical development as well as from a regulatory perspective. The book describes methods and examples of in vitro characterization of single transporters in the intestines, liver, and kidneys as well as characterization of substrate overlap between various transporters. Furthermore, probes and biomarkers are suggested for studies of the transporters’ impact on the pharmacokinetics of drug substrates/candidates interacting on transporters. The challenges of translating in vitro observed interaction of transporters into in vivo relevance are explored, and the book highlights perspectives of applying targeted proteomics and mechanistic modeling in this process.



Yuichi Sugiyama is head of Sugiyama Laborator at RIKEN Innovation Center, RIKEN Research Cluster for Innovation in Yokohama, Japan, and previously professor in the Department of Molecular Pharmacokinetics at the University of Tokyo from 1991 through to his retirement from the University in 2012. He is coauthor of more than 580 publications in international journals as well as 270 book chapters and review articles. His work is internationally recognized by prestigious awards, including AAPS Distinguished Pharmaceutical Scientist Award (2003), FIP Hoest Madsen Gold Medal (2009), “Medal with Purple Ribbon” given by the government in 2010, and the B. Brodie Award from ASPET (2012). Professor Sugiyama has been ranked as the top-cited scientist in the field of Pharmacology & Toxicology (1997–2007). He served as the chairman of the Board of Pharmaceutical Sciences in FIP and was also the president of both the International Society for the Study of Xenobiotics (ISSX) and Japanese Society for Xenobiotic Metabolism and Disposition (JSSX).


Bente Steffansen is associate professor in transporters in ADME at the Faculty of Health and Medical Sciences, University of Copenhagen. She graduated with MSc (pharm) in 1989 from the Royal Danish School of Pharmacy and obtained her PhD in 1994 under the Danish Research Academy within the field of prodrug design aimed for improved drug delivery. Dr. Steffansen has published more than 60 research articles, edited a book, and serves as the program director for pharmaceutical education at the University of Copenhagen. She is a member of the Chemical Committee under the National Pharmacopeia Board and a member of the European BioSim network of excellence.


AAPS Development Drug Steffansen Sugiyama Transporters

Editors and affiliations

  • Yuichi Sugiyama
    • 1
  • Bente Steffansen
    • 2
  1. 1.The University of Tokyo Graduate School of Pharmac. SciencesTokyoJapan
  2. 2.Pharma, Drug Transporters in ADME Department of PharmacyUniversity of Copenhagen Faculty of Health and Medical SciencesCopenhagenDenmark

Bibliographic information