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Research ArticleMinireview

Breast Cancer Resistance Protein (ABCG2) in Clinical Pharmacokinetics and Drug Interactions: Practical Recommendations for Clinical Victim and Perpetrator Drug-Drug Interaction Study Design

Caroline A. Lee, Meeghan A. O’Connor, Tasha K. Ritchie, Aleksandra Galetin, Jack A. Cook, Isabelle Ragueneau-Majlessi, Harma Ellens, Bo Feng, Mitchell E. Taub, Mary F. Paine, Joseph W. Polli, Joseph A. Ware and Maciej J. Zamek-Gliszczynski
Drug Metabolism and Disposition April 2015, 43 (4) 490-509; DOI: https://doi.org/10.1124/dmd.114.062174
Caroline A. Lee
Drug Metabolism and Pharmacokinetics, QPS LLC, Research Triangle Park, North Carolina (C.A.L.); Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut (M.A.O., M.E.T.); Centre for Applied Pharmacokinetic Research, Manchester Pharmacy School, The University of Manchester, Manchester, United Kingdom (A.G.); Pharmacokinetics and Drug Metabolism (B.F.) and Clinical Pharmacology, Global Innovative Pharma Business (J.A.C.), Pfizer Inc., Groton, Connecticut; School of Pharmacy, University of Washington, Seattle, Washington (I.R.-M., T.K.R.); Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, North Carolina (M.J.Z.-G., J.W.P.) and King of Prussia, Pennsylvania (H.E.); College of Pharmacy, Washington State University, Spokane, Washington (M.F.P.); and Clinical Pharmacology, Genentech, South San Francisco, California (J.A.W.)
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Meeghan A. O’Connor
Drug Metabolism and Pharmacokinetics, QPS LLC, Research Triangle Park, North Carolina (C.A.L.); Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut (M.A.O., M.E.T.); Centre for Applied Pharmacokinetic Research, Manchester Pharmacy School, The University of Manchester, Manchester, United Kingdom (A.G.); Pharmacokinetics and Drug Metabolism (B.F.) and Clinical Pharmacology, Global Innovative Pharma Business (J.A.C.), Pfizer Inc., Groton, Connecticut; School of Pharmacy, University of Washington, Seattle, Washington (I.R.-M., T.K.R.); Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, North Carolina (M.J.Z.-G., J.W.P.) and King of Prussia, Pennsylvania (H.E.); College of Pharmacy, Washington State University, Spokane, Washington (M.F.P.); and Clinical Pharmacology, Genentech, South San Francisco, California (J.A.W.)
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Tasha K. Ritchie
Drug Metabolism and Pharmacokinetics, QPS LLC, Research Triangle Park, North Carolina (C.A.L.); Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut (M.A.O., M.E.T.); Centre for Applied Pharmacokinetic Research, Manchester Pharmacy School, The University of Manchester, Manchester, United Kingdom (A.G.); Pharmacokinetics and Drug Metabolism (B.F.) and Clinical Pharmacology, Global Innovative Pharma Business (J.A.C.), Pfizer Inc., Groton, Connecticut; School of Pharmacy, University of Washington, Seattle, Washington (I.R.-M., T.K.R.); Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, North Carolina (M.J.Z.-G., J.W.P.) and King of Prussia, Pennsylvania (H.E.); College of Pharmacy, Washington State University, Spokane, Washington (M.F.P.); and Clinical Pharmacology, Genentech, South San Francisco, California (J.A.W.)
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Aleksandra Galetin
Drug Metabolism and Pharmacokinetics, QPS LLC, Research Triangle Park, North Carolina (C.A.L.); Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut (M.A.O., M.E.T.); Centre for Applied Pharmacokinetic Research, Manchester Pharmacy School, The University of Manchester, Manchester, United Kingdom (A.G.); Pharmacokinetics and Drug Metabolism (B.F.) and Clinical Pharmacology, Global Innovative Pharma Business (J.A.C.), Pfizer Inc., Groton, Connecticut; School of Pharmacy, University of Washington, Seattle, Washington (I.R.-M., T.K.R.); Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, North Carolina (M.J.Z.-G., J.W.P.) and King of Prussia, Pennsylvania (H.E.); College of Pharmacy, Washington State University, Spokane, Washington (M.F.P.); and Clinical Pharmacology, Genentech, South San Francisco, California (J.A.W.)
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Jack A. Cook
Drug Metabolism and Pharmacokinetics, QPS LLC, Research Triangle Park, North Carolina (C.A.L.); Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut (M.A.O., M.E.T.); Centre for Applied Pharmacokinetic Research, Manchester Pharmacy School, The University of Manchester, Manchester, United Kingdom (A.G.); Pharmacokinetics and Drug Metabolism (B.F.) and Clinical Pharmacology, Global Innovative Pharma Business (J.A.C.), Pfizer Inc., Groton, Connecticut; School of Pharmacy, University of Washington, Seattle, Washington (I.R.-M., T.K.R.); Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, North Carolina (M.J.Z.-G., J.W.P.) and King of Prussia, Pennsylvania (H.E.); College of Pharmacy, Washington State University, Spokane, Washington (M.F.P.); and Clinical Pharmacology, Genentech, South San Francisco, California (J.A.W.)
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Isabelle Ragueneau-Majlessi
Drug Metabolism and Pharmacokinetics, QPS LLC, Research Triangle Park, North Carolina (C.A.L.); Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut (M.A.O., M.E.T.); Centre for Applied Pharmacokinetic Research, Manchester Pharmacy School, The University of Manchester, Manchester, United Kingdom (A.G.); Pharmacokinetics and Drug Metabolism (B.F.) and Clinical Pharmacology, Global Innovative Pharma Business (J.A.C.), Pfizer Inc., Groton, Connecticut; School of Pharmacy, University of Washington, Seattle, Washington (I.R.-M., T.K.R.); Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, North Carolina (M.J.Z.-G., J.W.P.) and King of Prussia, Pennsylvania (H.E.); College of Pharmacy, Washington State University, Spokane, Washington (M.F.P.); and Clinical Pharmacology, Genentech, South San Francisco, California (J.A.W.)
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Harma Ellens
Drug Metabolism and Pharmacokinetics, QPS LLC, Research Triangle Park, North Carolina (C.A.L.); Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut (M.A.O., M.E.T.); Centre for Applied Pharmacokinetic Research, Manchester Pharmacy School, The University of Manchester, Manchester, United Kingdom (A.G.); Pharmacokinetics and Drug Metabolism (B.F.) and Clinical Pharmacology, Global Innovative Pharma Business (J.A.C.), Pfizer Inc., Groton, Connecticut; School of Pharmacy, University of Washington, Seattle, Washington (I.R.-M., T.K.R.); Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, North Carolina (M.J.Z.-G., J.W.P.) and King of Prussia, Pennsylvania (H.E.); College of Pharmacy, Washington State University, Spokane, Washington (M.F.P.); and Clinical Pharmacology, Genentech, South San Francisco, California (J.A.W.)
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Bo Feng
Drug Metabolism and Pharmacokinetics, QPS LLC, Research Triangle Park, North Carolina (C.A.L.); Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut (M.A.O., M.E.T.); Centre for Applied Pharmacokinetic Research, Manchester Pharmacy School, The University of Manchester, Manchester, United Kingdom (A.G.); Pharmacokinetics and Drug Metabolism (B.F.) and Clinical Pharmacology, Global Innovative Pharma Business (J.A.C.), Pfizer Inc., Groton, Connecticut; School of Pharmacy, University of Washington, Seattle, Washington (I.R.-M., T.K.R.); Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, North Carolina (M.J.Z.-G., J.W.P.) and King of Prussia, Pennsylvania (H.E.); College of Pharmacy, Washington State University, Spokane, Washington (M.F.P.); and Clinical Pharmacology, Genentech, South San Francisco, California (J.A.W.)
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Mitchell E. Taub
Drug Metabolism and Pharmacokinetics, QPS LLC, Research Triangle Park, North Carolina (C.A.L.); Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut (M.A.O., M.E.T.); Centre for Applied Pharmacokinetic Research, Manchester Pharmacy School, The University of Manchester, Manchester, United Kingdom (A.G.); Pharmacokinetics and Drug Metabolism (B.F.) and Clinical Pharmacology, Global Innovative Pharma Business (J.A.C.), Pfizer Inc., Groton, Connecticut; School of Pharmacy, University of Washington, Seattle, Washington (I.R.-M., T.K.R.); Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, North Carolina (M.J.Z.-G., J.W.P.) and King of Prussia, Pennsylvania (H.E.); College of Pharmacy, Washington State University, Spokane, Washington (M.F.P.); and Clinical Pharmacology, Genentech, South San Francisco, California (J.A.W.)
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Mary F. Paine
Drug Metabolism and Pharmacokinetics, QPS LLC, Research Triangle Park, North Carolina (C.A.L.); Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut (M.A.O., M.E.T.); Centre for Applied Pharmacokinetic Research, Manchester Pharmacy School, The University of Manchester, Manchester, United Kingdom (A.G.); Pharmacokinetics and Drug Metabolism (B.F.) and Clinical Pharmacology, Global Innovative Pharma Business (J.A.C.), Pfizer Inc., Groton, Connecticut; School of Pharmacy, University of Washington, Seattle, Washington (I.R.-M., T.K.R.); Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, North Carolina (M.J.Z.-G., J.W.P.) and King of Prussia, Pennsylvania (H.E.); College of Pharmacy, Washington State University, Spokane, Washington (M.F.P.); and Clinical Pharmacology, Genentech, South San Francisco, California (J.A.W.)
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Joseph W. Polli
Drug Metabolism and Pharmacokinetics, QPS LLC, Research Triangle Park, North Carolina (C.A.L.); Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut (M.A.O., M.E.T.); Centre for Applied Pharmacokinetic Research, Manchester Pharmacy School, The University of Manchester, Manchester, United Kingdom (A.G.); Pharmacokinetics and Drug Metabolism (B.F.) and Clinical Pharmacology, Global Innovative Pharma Business (J.A.C.), Pfizer Inc., Groton, Connecticut; School of Pharmacy, University of Washington, Seattle, Washington (I.R.-M., T.K.R.); Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, North Carolina (M.J.Z.-G., J.W.P.) and King of Prussia, Pennsylvania (H.E.); College of Pharmacy, Washington State University, Spokane, Washington (M.F.P.); and Clinical Pharmacology, Genentech, South San Francisco, California (J.A.W.)
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Joseph A. Ware
Drug Metabolism and Pharmacokinetics, QPS LLC, Research Triangle Park, North Carolina (C.A.L.); Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut (M.A.O., M.E.T.); Centre for Applied Pharmacokinetic Research, Manchester Pharmacy School, The University of Manchester, Manchester, United Kingdom (A.G.); Pharmacokinetics and Drug Metabolism (B.F.) and Clinical Pharmacology, Global Innovative Pharma Business (J.A.C.), Pfizer Inc., Groton, Connecticut; School of Pharmacy, University of Washington, Seattle, Washington (I.R.-M., T.K.R.); Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, North Carolina (M.J.Z.-G., J.W.P.) and King of Prussia, Pennsylvania (H.E.); College of Pharmacy, Washington State University, Spokane, Washington (M.F.P.); and Clinical Pharmacology, Genentech, South San Francisco, California (J.A.W.)
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Maciej J. Zamek-Gliszczynski
Drug Metabolism and Pharmacokinetics, QPS LLC, Research Triangle Park, North Carolina (C.A.L.); Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut (M.A.O., M.E.T.); Centre for Applied Pharmacokinetic Research, Manchester Pharmacy School, The University of Manchester, Manchester, United Kingdom (A.G.); Pharmacokinetics and Drug Metabolism (B.F.) and Clinical Pharmacology, Global Innovative Pharma Business (J.A.C.), Pfizer Inc., Groton, Connecticut; School of Pharmacy, University of Washington, Seattle, Washington (I.R.-M., T.K.R.); Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, North Carolina (M.J.Z.-G., J.W.P.) and King of Prussia, Pennsylvania (H.E.); College of Pharmacy, Washington State University, Spokane, Washington (M.F.P.); and Clinical Pharmacology, Genentech, South San Francisco, California (J.A.W.)
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Article Information

vol. 43 no. 4 490-509
DOI 
https://doi.org/10.1124/dmd.114.062174
PubMed 
25587128

Published By 
American Society for Pharmacology and Experimental Therapeutics
Print ISSN 
0090-9556
Online ISSN 
1521-009X
History 
  • Received November 16, 2014
  • Accepted January 9, 2015
  • Published online February 20, 2015.

Article Versions

  • Earlier version (January 13, 2015 - 08:06).
  • Earlier version (January 16, 2015 - 05:12).
  • You are viewing the most recent version of this article.
Copyright & Usage 
Copyright © 2015 by The American Society for Pharmacology and Experimental Therapeutics

Author Information

  1. Caroline A. Lee1,
  2. Meeghan A. O’Connor,
  3. Tasha K. Ritchie,
  4. Aleksandra Galetin,
  5. Jack A. Cook,
  6. Isabelle Ragueneau-Majlessi,
  7. Harma Ellens,
  8. Bo Feng,
  9. Mitchell E. Taub,
  10. Mary F. Paine,
  11. Joseph W. Polli,
  12. Joseph A. Ware, and
  13. Maciej J. Zamek-Gliszczynski
  1. Drug Metabolism and Pharmacokinetics, QPS LLC, Research Triangle Park, North Carolina (C.A.L.); Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut (M.A.O., M.E.T.); Centre for Applied Pharmacokinetic Research, Manchester Pharmacy School, The University of Manchester, Manchester, United Kingdom (A.G.); Pharmacokinetics and Drug Metabolism (B.F.) and Clinical Pharmacology, Global Innovative Pharma Business (J.A.C.), Pfizer Inc., Groton, Connecticut; School of Pharmacy, University of Washington, Seattle, Washington (I.R.-M., T.K.R.); Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, North Carolina (M.J.Z.-G., J.W.P.) and King of Prussia, Pennsylvania (H.E.); College of Pharmacy, Washington State University, Spokane, Washington (M.F.P.); and Clinical Pharmacology, Genentech, South San Francisco, California (J.A.W.)
  1. Address correspondence to:
    Dr. Maciej J. Zamek-Gliszczynski, GlaxoSmithKline, Drug Metabolism and Pharmacokinetics, 5 Moore Drive, P.O. Box 13398, Research Triangle Park, NC 27709-3398. E-mail: maciej.x.zamek-gliszczynski{at}gsk.com
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Drug Metabolism and Disposition: 43 (4)
Drug Metabolism and Disposition
Vol. 43, Issue 4
1 Apr 2015
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Research ArticleMinireview

BCRP Clinical DDI Study Design Recommendations

Caroline A. Lee, Meeghan A. O’Connor, Tasha K. Ritchie, Aleksandra Galetin, Jack A. Cook, Isabelle Ragueneau-Majlessi, Harma Ellens, Bo Feng, Mitchell E. Taub, Mary F. Paine, Joseph W. Polli, Joseph A. Ware and Maciej J. Zamek-Gliszczynski
Drug Metabolism and Disposition April 1, 2015, 43 (4) 490-509; DOI: https://doi.org/10.1124/dmd.114.062174

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Research ArticleMinireview

BCRP Clinical DDI Study Design Recommendations

Caroline A. Lee, Meeghan A. O’Connor, Tasha K. Ritchie, Aleksandra Galetin, Jack A. Cook, Isabelle Ragueneau-Majlessi, Harma Ellens, Bo Feng, Mitchell E. Taub, Mary F. Paine, Joseph W. Polli, Joseph A. Ware and Maciej J. Zamek-Gliszczynski
Drug Metabolism and Disposition April 1, 2015, 43 (4) 490-509; DOI: https://doi.org/10.1124/dmd.114.062174
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  • Article
    • Abstract
    • Introduction
    • Clinical Relevance of BCRP Polymorphisms
    • Potential Clinical BCRP Probe Substrates
    • Clinical Evidence-Based Recommendations for BCRP Substrate Selection
    • Potential Clinical BCRP Inhibitors
    • Clinical Evidence–Based Recommendations for BCRP Inhibitor Selection
    • Recommendations for Clinical BCRP Drug Interaction Study Design
    • Conclusions
    • Authorship Contributions
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