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FG-3246 is a potential first-in-class, fully human antibody-drug conjugate (ADC) being developed for the treatment of metastatic castration-resistant prostate cancer (mCRPC) and other tumor types. The drug consists of an anti-CD46 antibody (YS5) linked to monomethyl auristatin E (MMAE), an anti-mitotic agent commonly used as a payload in ADCs. FG-3246 targets CD46, a cell surface receptor highly expressed in prostate cancer and some other tumors but with limited expression in normal tissues, making it an attractive target for selective therapy. Upon binding to CD46, the ADC is internalized by tumor cells, delivering MMAE intracellularly to inhibit tubulin polymerization and induce apoptosis. Clinical studies have shown encouraging anti-tumor activity and manageable safety profile in patients with mCRPC who have progressed after androgen receptor signaling inhibitors. The most common adverse events are consistent with other MMAE-based ADCs, including infusion reactions, neutropenia, and peripheral neuropathy[1][5][6][7][8].
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