Pharmacogenomics of drug transporters: the next drug delivery challenge.

Scientifically, the third millennium begins with a major triumph--the publishing of the human genomic map, which is destined to have a momentous impact on the quality of life in our time. Disease prevention, individualized medicine, and genotyped-based medicine will soon become a reality. Pharmacogenetics, the forerunner of pharmacogenomics, began in the 1950s with a series of observations relating drug response to various genetic factors. It took almost two more decades for scientists to discover that cytochrome p450 2D6 was responsible for the metabolism of many drugs. This landmark discovery helped focus attention on how gene expression could impact the response to drugs. The stage was set for a revolution in therapeutics some 30 years later as the Human Genome Project crossed the finishing line triumphantly. A parallel development in drug delivery that may also benefit from the fruits of the Human Genome Project is the growing acceptance/awareness of drug transporters as a gateway to epithelial drug transport. This presentation addresses an area in need of attention: the possible impact of genetic polymorphism of drug transporters in pharmacokinetics and the challenge it poses in drug delivery.