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In vitro methods to support transporter evaluation in drug discovery and development


Brouwer, K L R; Keppler, D; Hoffmaster, K A; Bow, D A J; Cheng, Y; Lai, Y; Palm, J E; Stieger, B; Evers, R (2013). In vitro methods to support transporter evaluation in drug discovery and development. Clinical Pharmacology and Therapeutics, 94(1):95-112.

Abstract

This white paper addresses current approaches and knowledge gaps concerning methods to assess the role of transport proteins in drug/metabolite disposition in humans. The discussion focuses on in vitro tools to address key questions in drug development, including vesicle- and cell-based systems. How these methods can be used to assess the liability of compounds for transporter-based drug-drug interactions (DDIs) in vivo is also explored. Existing challenges and approaches to examine the involvement of transporters in drug disposition are discussed.

Abstract

This white paper addresses current approaches and knowledge gaps concerning methods to assess the role of transport proteins in drug/metabolite disposition in humans. The discussion focuses on in vitro tools to address key questions in drug development, including vesicle- and cell-based systems. How these methods can be used to assess the liability of compounds for transporter-based drug-drug interactions (DDIs) in vivo is also explored. Existing challenges and approaches to examine the involvement of transporters in drug disposition are discussed.

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Additional indexing

Item Type:Journal Article, refereed, further contribution
Communities & Collections:04 Faculty of Medicine > University Hospital Zurich > Clinic for Clinical Pharmacology and Toxicology
08 Research Priority Programs > Integrative Human Physiology
Dewey Decimal Classification:610 Medicine & health
Scopus Subject Areas:Life Sciences > Pharmacology
Health Sciences > Pharmacology (medical)
Language:English
Date:2013
Deposited On:27 Feb 2014 09:26
Last Modified:11 Jul 2024 01:37
Publisher:Nature Publishing Group
ISSN:0009-9236
OA Status:Green
Publisher DOI:https://doi.org/10.1038/clpt.2013.81
PubMed ID:23588315
  • Content: Accepted Version