tolimidone

Tolimidone is an orally delivered small molecule that acts as a selective activator of the enzyme Lyn kinase. Originally discovered by Pfizer and developed through Phase II for gastric ulcers (where it was discontinued due to lack of efficacy), it was later repurposed by Melior Pharmaceuticals and others for diabetes. Tolimidone increases phosphorylation of insulin substrate -1, amplifying the insulin signaling cascade and potentiating insulin activity. It has demonstrated glycemic control via insulin sensitization in animal models and clinical studies in type 2 diabetes mellitus (T2D), with ongoing development for type 1 diabetes mellitus (T1D). The drug also shows potential hepatoprotective effects and is being explored preclinically for non-alcoholic steatohepatitis (NASH) and COVID-19 infections[1][3][4][5][6][7].

Other names

CP-26154CP26154CP 26154MLR-1023MLR1023MLR 1023MTX-228MTX228MTX 228