Prostate cancer is the fourth most commonly diagnosed cancer in the world and the second leading cause of cancer death in men. Worldwide, nearly 1,414,000 people were diagnosed with prostate cancer and 375,304 people died from it in 2020.

Prostate-specific membrane antigen (PSMA), a type II transmembrane enzymatic protein, is overexpressed (up to 1000-fold) in ~90-100% of prostate tumors.  PSMA is directly correlated to disease progression. Since PSMA is highly expressed on the surface of metastatic and hormone-refractory PCa cells, and only minimum expressions in healthy tissue besides the kidneys and salivary glands, it provides targeted radiotherapy an excellent opportunity to deliver radiation specifically to cancer cells. This would result in the treatment of the lesions in a specific and tumor-selective manner.

Vitsgen PSMA-VG-01 showed great efficacy in tumor bearing animal model.  Its biodistribution showed a higher (greater than 2 fold) tumor uptake; higher tumor/kidney (T/K) ratio, and a lower normal organ uptake compared with PSMA 617.