BCRP (BCRP)

Breast Cancer Resistance Protein (gene: ABCG2), an ATP-dependent efflux transporter expressed at the intestinal brush border, hepatic canalicular membrane, blood-brain barrier, and placental syncytiotrophoblast. Limits oral absorption and promotes biliary and intestinal excretion of substrates. Named for its role in multidrug resistance in breast cancer cell lines. The ABCG2 c.421C>A polymorphism increases rosuvastatin exposure 2-fold.

أمثلة

• Rosuvastatin bioavailability increased by BCRP inhibitors
• Sulfasalazine as clinical BCRP probe substrate
• Topotecan oral bioavailability limited by intestinal BCRP efflux