Abstract: PD-1/PD-L1 immune checkpoint therapy has become another important treatment for several refractory and recurrent tumors besides radiotherapy and chemotherapy; however, only some patients can benefit from it. PD-1/PD-L1 targeted radionuclide molecular probe imaging can detect the PD-1/PD-L1 expression in whole body including tumors and other tissues noninvasively, timely and repeatedly, which will be more convenient for screening the patients benefiting from the immune-therapy, the efficacy evaluation and dynamic monitoring of the changes of PD-1/PD-L1 expression during treatment, providing a strong basis for the adjustment of treatment plan. This paper will review the recent progress of PD-1/PD-L1 targeted molecular probes, in order to provide reference for clinical application and further research of tumor immunotherapy.