Effects of P-glycoprotein on the pharmacokinetics and interaction mediated by P-glycoprotein

P-glycoprotein is an ATP-driven efflux pump which transport a wide variety of structurally diverse compounds from the cell interior into the extracellular space. Apart from in tumor causing multidrug resistance, it is also localized in healthy tissues such as liver, kidney, intestinal, blood-brain barrier, muscles and adrenal gland etc, and can modulate the pharmacokinetics of a lot of compounds. The role of P-glycoprotein in absorption, distribution, metabolism, excretion and the drug-drug interaction mediated by induction and inhibition of P-glycoprotein are reviewed in this paper.