Relevance of ABC Transporters in Drug Development

Curr Drug Metab. 2022;23(6):434-446. doi: 10.2174/1389200223666220621113524.

Abstract

ATP-binding cassette (ABC) transporters play a critical role in protecting vital organs such as the brain and placenta against xenobiotics, as well as in modulating the pharmacological and toxicological profile of several drug candidates by restricting their penetration through cellular and tissue barriers. This review paper describes the structure and function of ABC transporters as well as the role of P-glycoprotein, multidrug resistance-associated protein 2 and breast cancer resistance protein in the disposition of drugs. Furthermore, a review of the in vitro and in vivo techniques for evaluating the interaction between drugs and ABC transporters is provided.

Keywords: P-glycoprotein; breast cancer resistance protein; drug development; multidrug resistance-associated protein 2; pharmacodynamics; pharmacokinetics.

Publication types

  • Review

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
  • ATP Binding Cassette Transporter, Subfamily G, Member 2 / metabolism
  • ATP-Binding Cassette Transporters* / metabolism
  • Drug Development
  • Female
  • Humans
  • Multidrug Resistance-Associated Proteins / metabolism
  • Neoplasm Proteins* / metabolism
  • Pregnancy

Substances

  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • ATP Binding Cassette Transporter, Subfamily G, Member 2
  • ATP-Binding Cassette Transporters
  • Multidrug Resistance-Associated Proteins
  • Neoplasm Proteins