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FIS103 is a small molecule anti-cancer prodrug belonging to the N-benzyl indole carbinol (N-BIC) class. It is designed to be selectively activated by the sulfotransferase enzyme SULT1A1, which is overexpressed in approximately 5-15% of cancer patients, including those with renal cell carcinoma (RCC), breast, and prostate cancers. Once activated by SULT1A1, FIS103 induces rapid cell death by causing widespread, non-specific covalent alkylation of proteins within the cancer cell. Developed by Fannin Innovation Studio, FIS103 has shown potent antitumor activity in SULT1A1-high RCC cell lines and mouse xenograft models, while exhibiting low toxicity in cells with low SULT1A1 expression. The development program includes a companion diagnostic to identify patients whose tumors overexpress SULT1A1.
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