Overview. Overview / Albert P Li -- Transporter, Drug Metabolism, and Drug-Induced Liver Injury in Marketed Drugs / Minjun Chen, Kristin Ashby, Yue Wu -- Drug-Metabolism Enzymes and Transporter Activities as Risk Factors of Selected Marketed Drugs Associated with Drug-Induced Fatalities / Albert P Li -- Drug Metabolizing Enzymes and Drug Toxicity. Drug-Metabolizing Enzymes and Drug Toxicity / Albert P Li -- Genetic Polymorphism of Drug-Metabolizing Enzymes and Drug Transporters in Drug Toxicity / Ann K Daly -- Acyl Glucuronidation and Acyl-CoA Formation Mechanisms Mediating the Bioactivation and Potential Toxicity of Carboxylic Acid-containing Drugs / Mark P Grillo -- Liquid Chromatography-Mass Spectrometry (LC-MS) Quantification of Reactive Metabolites / Qingping Wang, Chuang Lu -- Human-Based In Vitro Experimental Approaches for the Evaluation of Metabolism-Dependent Drug Toxicity / Albert P Li -- Drug Transporters and Drug Toxicity. Mechanism-Based Experimental Models for the Evaluation of BSEP Inhibition and DILI / William A Murphy, Chitra Saran, Paavo Honkakoski, Kim LR Brouwer -- Hepatic Bile Acid Transporters in Drug-Induced Cholestasis / Tao Hu, Hongbing Wang -- Role of Renal Transporters in Drug-Drug Interactions and Nephrotoxicity / Yan Zhang, Donald Miller -- Blood-Brain Barrier Transporters and Central Nervous System Drug Response and Toxicity / Donald W Miller, Stacey Line, Nur A Safa, Yan Zhang -- Ototoxicity and Drug Transport in the Cochlea / Stefanie Kennon-McGill, Mitchell R McGill -- Modeling Drug Metabolizing Enzymes-Transporters Interplay for The Prediction of Drug Toxicity. Application of a PBPK Model Incorporating the Interplay Between Transporters and Drug-Metabolizing Enzymes for the Precise Prediction of Drug Toxicity / Kazuya Maeda -- The Extended Clearance Model / Birk Poller, Felix Huth, Vlasia Kastrinou-Lampou, Gerd A Kullak-Ublick, Michael Arand, Gian Camenisch.