title: In vitro methods to support transporter evaluation in drug discovery and development.
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.
authors.affiliation: Division of Pharmacotherapy and Experimental Therapeutics, UNC Eshelman School of Pharmacy, The University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA. kbrouwer@unc.edu
authors.forename: K L R
authors.initials: KL
authors.lastname: Brouwer
authors.forename: D
authors.initials: D
authors.lastname: Keppler
authors.forename: K A
authors.initials: KA
authors.lastname: Hoffmaster
authors.forename: D A J
authors.initials: DA
authors.lastname: Bow
authors.forename: Y
authors.initials: Y
authors.lastname: Cheng
authors.forename: Y
authors.initials: Y
authors.lastname: Lai
authors.forename: J E
authors.initials: JE
authors.lastname: Palm
authors.forename: B
authors.initials: B
authors.lastname: Stieger
authors.forename: R
authors.initials: R
authors.lastname: Evers
mesh_terms: D001692:Biological Transport / Q000187:drug effects*; D055808:Drug Discovery / Q000379:methods*; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004347:Drug Interactions; D006801:Humans; D026901:Membrane Transport Proteins / Q000378:metabolism*
chemical_list: D026901:Membrane Transport Proteins