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ASC61 is an orally bioavailable small molecule inhibitor of Programmed Death-Ligand 1 (PD-L1), developed by Gannex Pharma (a wholly-owned subsidiary of Ascletis Pharma) for the treatment of advanced solid tumors. Unlike traditional monoclonal antibodies that target the PD-1/PD-L1 pathway, ASC61 is a potent and highly selective small molecule that blocks the PD-1/PD-L1 interaction by inducing PD-L1 dimerization and internalization. This mechanism effectively prevents PD-L1 from binding to PD-1 on T-cells, thereby restoring the immune system's ability to recognize and attack tumor cells. ASC61 has demonstrated significant antitumor efficacy in humanized mouse models and entered Phase 1 clinical development following an Investigational New Drug (IND) application filing in the United States in early 2022.
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