Over the last few years diagnostic and therapeutic advances have contributed to the significant relevance of prostate-specific membrane antigen (PSMA) positron emission tomography/computed tomography (PET/CT) and PSMA radioligand therapy in patients with advanced prostate cancer (PCa). The PSMA-PET/CT has a higher accuracy for the detection of PCa metastases than the combination of CT and bone scintigraphy. Based on the theranostic approach, PSMA radioligand therapy can be performed in the castration-resistant stage in patients with sufficient PSMA expression of the tumor lesions in PSMA PET/CT and progression of PCa after chemotherapy and therapy with abiraterone or an androgen receptor signalling pathway inhibitor. Over the next few years, a large number of studies on the effectiveness of PSMA radioligand therapy in earlier stages of PCa and as part of combination therapies with other drugs will be conducted.