This book covers foundational topics in the emerging field of radiopharmaceutical therapy. It is divided into three sections: fundamentals, deeper dives, and special topics. In the first section, the authors examine the field from a bird’s-eye view, covering topics including the history of radiopharmaceutical therapy, the radiobiology of radiopharmaceutical therapy, and the radiopharmaceutical chemistry of both metallic and non-metallic radionuclides. The second section provides a more in-depth look at specific radiotherapeutics. Chapters include broader discussions of the different platforms for radiopharmaceutical therapy as well as more focused case studies covering individual radiotherapeutics. The third and final section explores a number of areas for further study, including medical physics, artificial intelligence, in vivo pretargeting, theranostic imaging, and the regulatory review process for radiotherapeutics. This book is the first of its kind andis useful for a broad audience of scientists, researchers, physicians, and students across a range of fields, including biochemistry, cancer biology, nuclear medicine, radiology, and radiation oncology.