Pharmacogenetics in Drug Development and Therapy

Oral presentation

Polymorphisms in human drug transporters and drug metabolizing enzymes: The blood- and tissue concentrations and hence the activity of many drugs are influenced by factors that are subject to interindividual variation. Variables that influence blood levels are metabolizing enzymes and transporters. The latter control drug uptake, distribution and elimination. Transport by ATP-driven efflux pumps such as MDR1 encoded P-glycoprotein (PGP) or by MRPs can influence the bioavailability of drugs. Knowing the transporter 'status' may allow compensation of differences in drug uptake, e.g. by dose adjustment, which is important for drugs with narrow therapeutic windows. Intestinal as well as renal and lymphocytic expression and function of P-glycoprotein correlate with defined polymorphisms in drug transporters. This influences the uptake as well as tissue distribution and excretion of drugs, and thereby directly affects the therapeutic efficacy of drugs.

Have something to say? Post a comment on this article!