Radioligand therapy is a form of targeted treatment using radioisotopes that emit ionising radiation coupled with a ligand to selectively deliver cytotoxic radiation dose to the intended target cells. There has been an expansion of radioligand therapy in the last two decades, driven by improvements in peptide and antibody technologies, identification of new targets and delivery mechanisms. Various molecular targets, ligands and different forms of ionising radiation are utilised. Prostate-specific membrane antigen is a transmembrane protein upregulated in prostate cancer cells and over expressed in castration-resistant prostate cancer. PSMA radioligand therapy uses a radioisotope attached to a molecule that targets PSMA protein on cancer cells. There is growing evidence for the use of PSMA radioligand therapy in the treatment of prostate cancer with promising efficacy and minimal toxicity when compared to other conventional forms of treatment.