Membrane transporters are major determinants of the absorption, distribution and elimination of many of the most commonly used drugs. In the past decade, the field of membrane transporter pharmacogenomics has undergone enormous growth. In particular, functional genomic and clinical studies have provided new information regarding the contribution of coding variants in transporters to drug disposition and response. With continuing advances in sequencing technologies and large-scale human variation studies, over the next decade, knowledge in the field will be transformed. In particular, functional variants in noncoding regions of transporters will be discovered, and large clinical studies will result in the identification of variants in multiple genes, including transporter genes, which contribute to variation in clinical drug response.