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huC242, also known as cantuzumab, is a humanized monoclonal antibody that specifically targets the CanAg antigen, a tumor-associated carbohydrate epitope found on a novel glycoform of MUC1 (mucin 1). Developed primarily by ImmunoGen, huC242 serves as the targeting moiety for several antibody-drug conjugates (ADCs), including cantuzumab mertansine (huC242-DM1, SB-408075) and IMGN242 (huC242-DM4). CanAg is highly expressed in various solid tumors, particularly those of the gastrointestinal tract, such as pancreatic, colorectal, and gastric cancers. While the naked antibody was studied, its primary clinical utility was explored as a delivery vehicle for maytansinoid cytotoxic payloads, which induce mitotic arrest by inhibiting tubulin polymerization. Clinical development of huC242-based therapies reached Phase II but was ultimately discontinued.
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