Radionuclide therapy targeting PSMA for the treatment of metastatic prostate cancer: Current point of view and ways of improvement

Metastatic castration-resistant prostate cancer (mCRPC) still represents a challenge and an unmet clinical need. RadioLigand therapy targeting PSMA (PRLT) has been used for several years with success and low toxicity. The first radionuclide used were radiolabeled antibody with limited dose due to hematologic toxicity. Rapidly, small molecules targeting PSMA were developed and used with lower toxicity, mostly related to mild transient xerostomia and nausea due to physiological PSMA expression in the salivary glands and proximal bowel. Briefly, 2/3 of the patients may first respond to treatments followed by disease recurrence responding to further cycles for half of them. Therefore, there is a need to improve again the PRLT efficacy and the ways of improvement will be discussed in this review. (C) 2019 Elsevier Masson SAS. All rights reserved.