Ertiprotafib

Ertiprotafib is a small molecule drug that was developed as an insulin sensitizer for the treatment of type 2 diabetes. It acts primarily as an inhibitor of protein tyrosine phosphatase 1B (PTP1B), which prevents dephosphorylation of the insulin receptor, thereby improving insulin sensitivity and lowering blood glucose levels. In addition to PTP1B inhibition, ertiprotafib functions as a dual agonist for peroxisome proliferator-activated receptors alpha and gamma (PPARα/γ), contributing to improved glucose homeostasis and reduced triglyceride and free fatty acid levels. The compound also inhibits IκB kinase beta (IKKβ), providing anti-inflammatory effects. Despite promising preclinical results in animal models, clinical development was discontinued after phase II trials due to insufficient efficacy and adverse effects related to its mechanism—specifically, induction of aggregation of PTP1B rather than classic inhibition[1][2][3][4][5][6][7].

Other names

Ertiprotafib [USAN:INN]