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  • A first-generation sulfonylurea with hypoglycemic activity. Tolbutamide binds to and blocks adenosine triphosphate (ATP)-sensitive potassium channels on the beta cell membrane of the pancreatic islet tissues. This leads to potassium efflux, which results in depolarization, calcium influx, calcium-calmodulin binding, kinase activation, and release of insulin-containing granules by exocytosis. In addition, tolbutamide may increase the number and affinity of cell surface insulin receptors, thereby enhancing the peripheral response to insulin. Tolbutamide is a CYP2C9 substrate. Check for \'https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C66610\' active clinical trials using this agent. (\'http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C66610\' NCI Thesaurus)
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