ARX517

ARX517 is an investigational antibody-drug conjugate (ADC) designed to target prostate-specific membrane antigen (PSMA), which is highly expressed in metastatic castration-resistant prostate cancer (mCRPC). The drug consists of a fully humanized IgG1 kappa monoclonal antibody directed against PSMA, site-specifically conjugated to two molecules of AS269, a proprietary and potent microtubule inhibitor. Upon binding to PSMA on the surface of cancer cells, ARX517 is internalized and its cytotoxic payload is released following lysosomal metabolism, leading to apoptosis. The ADC employs a non-cleavable polyethylene glycol linker and stable oxime conjugation chemistry for enhanced stability and minimal off-target toxicity. Preclinical studies have shown selective cytotoxicity toward PSMA-expressing tumor cells with favorable safety profiles in animal models. ARX517 has received FDA Fast Track designation for mCRPC and is currently being evaluated in phase 1/2 clinical trials[1][3][4][6][7].