In this Science at Sunrise session, members of the ITC from industry, academia and FDA will present new information about transporter-mediated drug-drug interactions (DDIs) in drug development. First an industry perspective will be presented describing how drug metabolites are potent substrates and inhibitors of transporters, and as a result may be subject to DDIs. Second, a regulatory perspective will be given that updates current decision trees focused on transporter-mediated DDIs as well as to discuss potential inhibition of transporter by drug leading to modulation of endogenous biomarkers, such as creatinine. Finally, an academic scientist will illustrate the use of genomic and metabolomic approaches in the discovery of endogenous biomarkers of transporters that may be used to inform clinical DDIs. This comprehensive session led by a multidisciplinary team will expand the knowledge of ASCPT members in the study of transporters in drug development.