title: Breast cancer resistance protein in pharmacokinetics and drug-drug interactions.
abstract: Breast cancer resistance protein (BCRP), also known as ABCG2, ABCP and MXR, is a member of the ATP-binding cassette transporter G family. BCRP functions as a biological barrier that extrudes xenobiotics out of cells. The broad substrate specificity and tissue distributions of BCRP in the body make this transporter one of the major efflux transporters in chemotherapy. Recent studies have demonstrated that BCRP exerts a great impact on drug absorption and disposition. This review focuses on the role of BCRP in pharmacokinetics as well as in vitro and in vivo strategies to evaluate hepatic/intestinal BCRP-mediated drug transports and drug-drug interactions. The impacts of polymorphism and gender difference of BCRP are also discussed.
authors.affiliation: Millennium Pharmaceutics, Inc., DMPK, 45 Sidney St., Cambridge, MA 02139, USA. cindy.xia@mpi.com
authors.forename: Cindy Q
authors.initials: CQ
authors.lastname: Xia
authors.forename: Johnny J
authors.initials: JJ
authors.lastname: Yang
authors.forename: Liang-Shang
authors.initials: LS
authors.lastname: Gan
mesh_terms: D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters / Q000032:analysis / Q000037:antagonists & inhibitors / Q000235:genetics / Q000502:physiology*; D000042:Absorption; D019540:Area Under Curve; D001812:Blood-Brain Barrier; D004347:Drug Interactions; D018565:Food-Drug Interactions; D006801:Humans; D009363:Neoplasm Proteins / Q000032:analysis / Q000037:antagonists & inhibitors / Q000235:genetics / Q000502:physiology*; D010599:Pharmacokinetics; D011110:Polymorphism, Genetic
chemical_list: C116614:ABCG2 protein, human; D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters; D009363:Neoplasm Proteins