Genetic variations and gene expression of transporters in drug disposition and response

Background: The importance of transporters in drug disposition and response has led to increasing interest in genetic variations and expression differences of their genes. Objective: This review summarizes: i) genetic variations in transporters and associated drug response; and ii) a pharmacogenomic approach to correlate transporter expression and drug response. Methods: Several transporters in ATP-binding cassette family and solute carrier family are discussed. Conclusion: The field of transporter pharmacogenomics is in its early stage. Transporter expression at mRNA levels could be more directly related to their functions and more practical to be assayed in high throughput. Correlating microarray expression of transporters with anticancer drug activity in the NCI-60 panel has provided an approach for identifying drug-transporter relationships and predicting drug response.