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Eparolimab (SG001) is a humanized IgG1 kappa monoclonal antibody that targets the cytotoxic T-lymphocyte-associated protein 4 (CTLA-4), an immune checkpoint molecule expressed on the surface of T cells. By binding to CTLA-4, eparolimab blocks its interaction with the ligands CD80 (B7-1) and CD86 (B7-2) on antigen-presenting cells, thereby preventing the inhibitory signal that normally downregulates T-cell activation. This mechanism enhances the anti-tumor immune response by promoting T-cell proliferation and activity. Developed by Beijing Sumgen Biotech, eparolimab is primarily being investigated in clinical trials for the treatment of various solid tumors, often in combination with PD-1 inhibitors such as toripalimab. A significant area of clinical focus is its use in neoadjuvant therapy for locally advanced rectal cancer, particularly in patients with proficient mismatch repair (pMMR) or microsatellite stable (MSS) status, where it is combined with chemoradiotherapy to improve pathological complete response rates and facilitate organ-sparing outcomes.
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