"Drug Metabolism and Transport" is a comprehensive textbook that addresses experimental approaches and strategies for studying the bioactivation, detoxification, tissue distribution, and elimination of xenobiotics. The authors highlight the essential systems of drug metabolism, particularly the cytochrome P450 family, flavin-containing monooxygenases, glutathione S-transferases, glucuronidation, N-acetylation, and sulfotransferases. Additionally, innovative methods for investigating signaling pathways that influence the regulation of drug metabolism enzymes, as well as the role of low-molecular-weight cofactors in modulating drug metabolism, are discussed. This book provides valuable insights into the complex mechanisms that can affect drug therapy and is an indispensable resource for professionals and students in the life sciences.