PSMA-ADC

PSMA-ADC is an antibody-drug conjugate (ADC) consisting of a fully human IgG1 monoclonal antibody targeting the prostate-specific membrane antigen (PSMA) conjugated to the microtubule-disrupting agent monomethyl auristatin E (MMAE) via a protease-cleavable valine-citrulline linker. Developed by Progenics Pharmaceuticals (now Lantheus), the drug was designed to target PSMA, which is highly expressed on the surface of prostate cancer cells and the neovasculature of various solid tumors, including glioblastoma multiforme (GBM) and gliosarcoma. Upon binding to PSMA, the ADC is internalized, and MMAE is released intracellularly, where it inhibits tubulin polymerization, leading to cell cycle arrest and apoptosis. While primarily investigated for metastatic castration-resistant prostate cancer, it was also evaluated in a Phase II trial led by Heinrich Elinzano (BrUOG 263) for recurrent GBM and gliosarcoma. The trial was terminated after showing no objective responses and significant toxicity, likely due to low or heterogeneous PSMA expression in the brain tumor environment.

Other names

Prostate-specific membrane antigen antibody-drug conjugatePSMA-ADC-001PSMA-ADC001PSMA-ADC 001