There is a great need to develop experimental approaches to define the roles of enteric drug metabolism, uptake and efflux in the fate and biological effects of the orally-administered drugs. This proposed symposium will a review of the current scientific concepts and experimental approaches in the assessment of intestinal drug uptake, metabolism, drug-drug interactions and enterotoxicity. The presentations will include a review of the current understanding of enteric drug metabolizing enzymes and transporters, in vitro and in vivo experimental approaches, as well as PBPK and IVIVE approaches for the translation of preclinical data to clinical outcome.