Membranes bind all cells together, and the lipid bilayer of cell membranes is extremely impervious for most water-soluble compounds. Membrane transport processes that have been identified in many biological events occur during the formation of electrochemical potentials, uptake of nutrients, removal of wastes, endocytotic internalization of macromolecules, and oxygen transport in respiration. Specific transport proteins catalyze the flow of ions, nutrients, and metabolites across cellular membranes. These transport proteins are studied within pharmaceutical science in order to understand their impact on drug absorption, distribution, metabolism, and elimination (ADME), as well as drug safety. Several neurological diseases have been linked to altered CNS transporter expression. As a result, many transport proteins have emerged as pharmacological targets. In this book, various advancements related to the use of membrane transporters as drug targets have been discussed in detail. It aims to equip students and experts with the advanced topics and upcoming concepts in this area of study.