Tifenazoxide is a thiadiazine derivative patented by Novo Nordisk A/S as the opener of the KATP-regulated potassium channels useful in the treatment of the endocrine system diseases. Tifenazoxide is a selective opener of the beta-cell type (SUR1 / Kir6.2) KATP channel that characterized as competitive inhibitors of glibenclamide binding to membranes of HEK293 cells expressing human SUR1/Kir6.2and as potent inhibitors of insulin release in isolated rat islets. In clinical trials, Tifenazoxide administration leads to a decrease in insulin concentrations 1 h post-dose. This was accompanied by an increase in glucose and growth hormone concentrations (NS), but not of glucagon. During the OGTT a dose-dependent reduction in the 2 h glucose value was observed.