P-glycoprotein (P-gp)
P-gpAn ATP-dependent efflux transporter encoded by the ABCB1 (MDR1) gene, expressed at pharmacological barriers including the intestinal epithelium, blood-brain barrier, renal tubules, and hepatic canaliculi. Limits oral bioavailability by pumping substrates back into the intestinal lumen and protects the CNS by restricting brain penetration. A major determinant of multidrug resistance in cancer.
أمثلة
- Digoxin efflux reduced by P-gp inhibitor quinidine
- Loperamide excluded from brain by P-gp (no CNS opioid effects)
- Cyclosporine as potent P-gp inhibitor increasing statin exposure
هل تعلم؟
An ATP-dependent efflux transporter encoded by the ABCB1 (MDR1) gene, expressed at pharmacological barriers including the intestinal epithelium, blood-brain barrier, renal tubules, and hepatic canaliculi. Limits oral bioavailability by pumping …