Pelgifatamab

Pelgifatamab (BAY-2315497) is a prostate-specific membrane antigen (PSMA) antibody with a human EC50 of 1.2 nM. Pelgifatamab acts as a carrier for therapeutic radionuclides, enabling the precise delivery of these radionuclides to PSMA-expressing prostate cancer cells. Pelgifatamab effectively inhibits tumor growth and tumor-induced abnormal bone growth in prostate cancer bone metastasis models. Pelgifatamab induces double-strand DNA breaks, cell cycle arrest, and apoptosis in PSMA-positive tumor cells, with its activity dependent on the level of PSMA expression in the cells. Pelgifatamab can be used in prostate cancer research.

Methods: PSMA-positive (C4-2, LNCaP, MDA-PCa-2b, 22Rv1) and negative (PC-3, DU-145) prostate cancer cells were treated with gradient concentrations (0.0002–50 kBq/mL) of ²²⁵Ac-Pelgifatamab, incubated for 5 days, and cell viability was assessed using the CellTiter-Glo assay.
Results: ²²⁵Ac-Pelgifatamab exerted potent cytotoxic effects exclusively on PSMA-positive cells, with toxicity positively correlated with PSMA expression levels; however, it had no significant inhibitory effect on PSMA-negative cells. [1]
Methods: C4-2, LNCaP, and 22Rv1 cells were treated with 0.3–3 kBq/mL ²²⁵Ac-Pelgifatamab for 24 h. Cell cycle analysis was performed by flow cytometry, ROS levels were measured by fluorescence, and Western blot analysis was conducted to detect the expression of p-Chk2, p-ATM, p-ATR, γ-H2AX, and PSMA.
Results: ²²⁵Ac-Pelgifatamab induced G2/M phase arrest in tumor cells, promoted ROS production in a dose-dependent manner, and significantly upregulated DNA damage markers.[1]

Human

Monoclonal

Unconjugated