Title:Relevance of ABC Transporters in Drug Development
Volume: 23
Issue: 6
Author(s): Chukwunonso K. Nwabufo*
Affiliation:
- Drug Discovery and Development Research Group, College of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, Canada
- Department of Pharmaceutical Sciences, Leslie Dan Faculty of Pharmacy, University of Toronto, Toronto, ON, Canada
Keywords:
P-glycoprotein, multidrug resistance-associated protein 2, breast cancer resistance protein, drug development, pharmacokinetics, pharmacodynamics.
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.