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SAR566658 is an antibody-drug conjugate (ADC) composed of a humanized monoclonal antibody (huDS6) targeting the tumor-associated sialoglycotope CA6—a glycoepitope of Mucin 1 (MUC1)—conjugated via a cleavable linker to the cytotoxic maytansinoid derivative DM4. The ADC binds with high affinity to CA6-expressing tumor cells, leading to internalization and intracellular release of DM4, which inhibits tubulin polymerization and induces apoptosis in cancer cells. It was developed for the treatment of solid tumors overexpressing CA6, including breast, ovarian, lung, bladder, pancreas, cervix cancers. Clinical trials demonstrated antitumor activity but also notable ocular toxicity (keratopathy). Development has been discontinued[1][2][3][5].
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