danegaptide

Danegaptide is a small, orally bioavailable modified dipeptide that acts as a selective second-generation gap junction modifier. Its primary mechanism of action is the enhancement of gap junction conductance and coupling, particularly through modulation of connexin43 (Cx43) proteins. This leads to increased intercellular communication by allowing more ions, metabolites, and secondary messengers to pass between cells. Danegaptide has been investigated for its antiarrhythmic properties in large animal models and clinical trials for atrial fibrillation and myocardial reperfusion injury but was discontinued for these indications after lack of efficacy in phase 2/3 studies. More recently, it is being developed as an oral therapy targeting early-stage diabetic retinopathy (DR) and wet age-related macular degeneration (AMD), aiming to prevent cell-cell uncoupling, vascular leakage, apoptotic vascular cell death, and capillary breakdown—key pathological events in these eye diseases[1][3][4][5][6][7].

Other names

(2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acidDANEGAPTIDE