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Optimizing the “Drug-Like” Properties of Leads in Drug Discovery pp 423–459Cite as

The Relevance of Transporters in Determining Drug Disposition

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Part of the book series: Biotechnology: Pharmaceutical Aspects ((PHARMASP,volume IV))

Abstract

Membrane transporters represent an important class of proteins responsible for regulating cellular and physiological solute and fluid balance. With the sequencing of the human genome, it has been estimated that approximately 500 to 1,200 genes code for transport proteins (Venter et al., 2001). In terms of xenobiotic disposition, a smaller fraction of these transporters are currently known to significantly interact with drugs. In particular, transporters that are localized at key gateway tissues within the body such as the intestine (Tsuji and Tamai, 1996; Suzuki and Sugiyama, 2000b), liver (Keppler and Konig, 2000; Suzuki and Sugiyama, 2000a), kidney (Inui et al., 2000; Dresser et al., 2001), placenta (Ganapathy et al., 2000), and brain (Tamai and Tsuji, 2000; Gao and Meier, 2001) are critical modulators of drug absorption, tissue distribution and elimination and have been the subject of recent reviews.

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Authors and Affiliations

  1. Division of Clinical Pharmacology, Vanderbilt University School of Medicine, Nashville, TN

    Hartmut Glaeser Ph.D. & Richard B. Kim M.D.

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  1. Hartmut Glaeser Ph.D.
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  2. Richard B. Kim M.D.
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Editors and Affiliations

  1. University of Kansas, Lawrence, KS, 66045, USA

    Ronald T. Borchardt

  2. Wyeth Research, Monmouth Junction, NJ, 08852, USA

    Edward H. Kerns

  3. Pfizer, Inc., Kalamazoo, MI, 49007, USA

    Michael J. Hageman

  4. University of North Carolina, Chapel Hill, NC, 27599, USA

    Dhiren R. Thakker

  5. Eli Lilly Research Laboratory, Greenfield, IN, 46285, USA

    James L. Stevens

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© 2006 American Association of Pharmaceutical Scientists

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Glaeser, H., Kim, R.B. (2006). The Relevance of Transporters in Determining Drug Disposition. In: Borchardt, R.T., Kerns, E.H., Hageman, M.J., Thakker, D.R., Stevens, J.L. (eds) Optimizing the “Drug-Like” Properties of Leads in Drug Discovery. Biotechnology: Pharmaceutical Aspects, vol IV. Springer, New York, NY. https://doi.org/10.1007/978-0-387-44961-6_18

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