This book is useful to readers who are just beginning in the field of drug design and development. It starts with an introduction and some basic information about drugs. Pharmacokinetic and pharmacodynamic aspects are covered in the initial chapters. Systemic descriptions of pharmacokinetic parameters such as absorption, distribution, metabolism, and excretion are explained in simple and easy language. This book demonstrates detailed concepts of lead molecules and their sources. In addition, drug target classification, identification and validation strategies, as well as the design and development of combinatorial libraries for new lead generation are also covered. This book contains various methodologies, such as structure-based drug designing, quantitative structure activity relationship, pharmacophore modelling, and docking studies for screening and designing the drug candidates. This book will help in the identification and design of drugs that could be potentially useful in deriving the candidate drugs, which may have efficacy in animal models or cell cultures. Thus, the most effective compounds could be employed based on the above results, and will then be moved from preclinical studies to clinical trials. The last couple of chapters describe dosage drug regulatory affairs and recent advancements in healthcare. The aim of this book is to provide comprehensive ideas about overall drug design and development.