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TIX100 is a novel, orally available small molecule developed as a potent and specific inhibitor of thioredoxin-interacting protein (TXNIP). It is designed to protect pancreatic beta cell health and improve islet cell function by inhibiting TXNIP transcription via a conserved E-box motif in the TXNIP promoter. Unlike verapamil, which also inhibits TXNIP but acts as an L-type calcium channel blocker, TIX100 does not affect cellular calcium concentrations or pose cardiovascular risks. Preclinical studies have shown that TIX100 protects against models of Type 1 and Type 2 diabetes as well as metabolic dysfunction-associated steatotic liver disease (MASLD/NAFLD), with demonstrated efficacy in both rodent and human islets. The drug has advanced to Phase 1 clinical trials for Type 1 diabetes, showing good tolerability and no significant adverse effects so far. Developed through high-throughput screening and medicinal chemistry optimization, TIX100 represents a new chemical entity within the substituted quinazoline sulfonamide class[1][2][3][4][5][6][7][8].
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