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Updated: Aug 7, 2026

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
08:46

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms

Published on: December 9, 2015

Breast cancer resistance protein in pharmacokinetics and drug-drug interactions

Cindy Q Xia1, Johnny J Yang, Liang-Shang Gan

  • 1Millennium Pharmaceutics, Inc., DMPK, 45 Sidney St., Cambridge, MA 02139, USA. cindy.xia@mpi.com

Expert Opinion on Drug Metabolism & Toxicology
|July 26, 2006
PubMed

Insights

Breast cancer resistance protein (BCRP) is a key transporter affecting drug absorption and chemotherapy. This review details strategies for evaluating BCRP

Area of Science:

  • Pharmacology
  • Biochemistry
  • Drug Metabolism

Background:

  • Breast cancer resistance protein (BCRP), also known as ABCG2, is an ATP-binding cassette transporter.
  • BCRP acts as a cellular barrier, effluxing xenobiotics and impacting drug disposition.
  • It is a significant efflux transporter in chemotherapy due to its substrate specificity and tissue distribution.

Purpose of the Study:

  • To review the role of BCRP in pharmacokinetics.
  • To discuss in vitro and in vivo strategies for evaluating BCRP-mediated drug transport.
  • To explore BCRP's impact on drug-drug interactions, polymorphism, and gender differences.

Main Methods:

  • Review of recent scientific literature on BCRP.
  • Analysis of in vitro and in vivo experimental strategies.
  • Discussion of pharmacokinetic data related to BCRP.

Main Results:

  • BCRP significantly influences drug absorption and disposition.
  • Various methods exist to assess BCRP-mediated transport in hepatic and intestinal systems.
  • BCRP activity is affected by genetic polymorphisms and gender.

Conclusions:

  • Understanding BCRP's role is crucial for optimizing drug therapy and predicting drug-drug interactions.
  • In vitro and in vivo models are essential for characterizing BCRP-mediated drug transport.
  • Further research into BCRP polymorphism and gender effects is warranted.

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