Targeted alpha therapy (TAT) has emerged as a viable therapeutic option for cancer management, due to its high target specificity and superlative ability to effectively disrupt the genetic make-up of the cancerous cells, thereby impeding their aggressive growth. TAT belongs to the category of radioligand therapies in oncology wherein alpha-emitting radionuclides are delivered directly to tumours and the tumour microenvironment with little impact on surrounding healthy cells. This approach is facilitated by chelating the radionuclides with ligands or conjugating them to targeting vehicles which facilitate their biodistribution, localization, and accumulation in the target sites. Currently, TAT continues to exhibit promising therapeutic outcomes in both preclinical and clinical evaluations, with more exciting prospects for the future. Accordingly, this timely review focuses on the pertinent, appealing merits of TAT, elaborating on the favourable chemical properties of potent alpha-emitting radionuclides and their enhancement. The current review also delves into the radiobiology and dosimetry of alpha-particles, and their application to TAT. Recent preclinical and clinical reports have further supported the viability of TAT as a promising therapeutic intervention. More so, this review sheds light on the promising therapeutic possibilities that nuclear medicine, particularly TAT, can offer in oncology.