Abstract: Pretargeting is a method that utilizes a specific affinity coupling system to self-attach specific antibodies and radionuclides that are sequentially injected into the body through a two-step process for disease imaging and/or treatment. Pretargeted nuclear medicine imaging and treatment is an alternative method to antibody-based conventional radioimmunotherapy, and has many advantages over conventional radioimmunotherapy. In this review, the authors will discuss two pretargeting strategies that have entered the clinical research stage, describe their current research progress in disease imaging and treatment, and compare the advantages and disadvantages of different approaches.