Currently, there is great interest in the field of biomedical research for developing target‐specific radiopharmaceuticals using metallic radionuclides for noninvasive diagnosis of disease and radiotherapy of cancers. It is a multidisciplinary field of science, involving radiometal production, chelate design, bioconjugation, specific targeting, imaging, and therapeutic applications. This article briefly reviews the chemical aspects and clinical applications of inorganic radiopharmaceuticals from a historical perspective to future directions.