More than 400 membrane transporters in two major superfamilies-ATP-binding cassette (ABC) and solute carrier (SLC)-are annotated in the human genome. Preclinical and clinical studies indicate that transport is an important determinant of drug disposition, as well as therapeutic and adverse drug effects. Importantly, transporters may represent the rate-determining step of drug absorption, distribution, and elimination in the intestine, liver, kidney, and blood-brain barrier (BBB), and they are often the sites of drug-drug interactions.