Front Matter -- Introduction. Historical Perspective / ROBERTA S KING -- Factors Affecting Metabolism / ROBERTA S KING -- Biotransformations in Drug Metabolism / ROBERTA S KING -- A Comprehensive Picture of Biotransformation in Drug Discovery / JOE R CANNON, PRAKASH VACHASPATI, YANG YUAN -- In Vivo Drug Metabolite Kinetics / ZHENG YANG -- LC-MS / MS -Based Proteomics Methods for Quantifying Drug-Metabolizing Enzymes and Transporters / Logan S Smith, SUN MIN JUNG, JIAPENG LI, HAO-JIE ZHU -- Technologies for In vitro and In vivo Studies. Mass Spectrometry / THOMAS R SHARP -- Accelerating Metabolite Identification Mass Spectrometry Technology Drives Metabolite Identification Studies Forward / ALA F NASSAR -- Role of Structural Modifications of Drug Candidates to Enhance Metabolic Stability / ALA F Nassar -- Drug Design Strategies: Role of Structural Modifications of Drug Candidates to Improve PK Parameters of New Drugs / ALA F NASSAR -- Chemical Structural Alert and Reactive Metabolite Concept as Applied in Medicinal Chemistry to Minimize the Toxicity of Drug Candidates / ALA F NASSAR -- Studies of Reactive Metabolites using Genotoxicity Arrays and Enzyme/ DNA Biocolloids - 2021 / JAMES F RUSLING, ELI G HVASTKOVS -- Drug Interactions. Enzyme Inhibition / PAUL F HOLLENBERG -- Xenobiotic Receptor-Mediated Gene Regulation in Drug Metabolism and Disposition / HONGBING WANG, WEN XIE -- Characterization of Cytochrome P450 Mechanism Based Inhibition / DAN A ROCK, LARRY C WIENKERS -- An Introduction to Metabolic Reaction-Phenotyping / CARL DAVIS -- Epigenetic Regulation of Drug-Metabolizing Enzymes in Cancer / JIAQI WANG, XIAOLI ZHENG, SU ZENG -- Epigenetic Regulation of Drug Transporters in Cancer / YINGYING WANG, YING ZHOU, YU WANG, LUSHAN YU, SU ZENG -- Toxicity. The Role of Drug Metabolism in Toxicity / UMESH M HANUMEGOWDA, CARL DAVIS -- Allergic Reactions to Drugs / MARK P GRILLO -- Chemical Mechanisms in Toxicology / MARK P GRILLO -- Role of Bioactivation Reactions in Chemically Induced Nephrotoxicity / LAWRENCE H LASH -- Applications. Mapping the Heterogeneous Distribution of Cancer Drugs by Imaging Mass Spectrometry / PURVA S DAMALE, SHIBDAS BANERJEE -- Systemic Metabolomic Changes Associated with Chemotherapy: Role in Personalized Therapy / BHARGAB KALITA, GANESH K BARIK, TANISHA SHARMA, KHUSHMAN TAUNK, PRANEETA P BHAVSAR, MANAS K SANTRA, SRIKANTH RAPOLE -- Metabolic Reprogramming in Cancer / DEBASISH PRUSTY, Soumen Kanti Manna -- Case Study: Metabolism and Reactions of Alkylating Agents in Cancer Therapy / ALA F NASSAR, ADAM V WISNEWSKI, IVAN KING -- Rewiring of Drug Metabolism and Its Cross-talk with Metabolic Reprogramming in Cancer / SUBHABRATA MAJUMDER, Soumen Kanti Manna -- Principles of Drug Metabolism and Interactions in Cardio-Oncology / SHERRY-ANN BROWN, CRAIG BEAVERS, SAILAJA KAMARAJU, MEERA MOHAN, OLUBADEWA FATUNDE, GIFT ECHEFU, SVETLANA ZAHAROVA, BRIANNA WALLACE, CAROLYN OXENCIS -- Index