Aleniglipron (GSBR-1290) is a fully biased, orally available, potent GLP-1R agonist with binding Ki of <10 nM and cAMP EC50 of <0.1 nM. GSBR-1290 strongly activated GLP-1R Gαs cAMP pathway without inducing measurable β-arrestin recruitment signaling, which indicates it is a fully biased agonist. GSBR-1290 showed dose dependent induction of insulin secretion GSBR-1290 strongly induced insulin secretion and glucose clearance in acute intravenous glucose tolerance test (ivGTT). GSBR-1290 administered orally once daily for 7-day demonstrated robust increase in insulin secretion and glucose clearance in ivGTT and a dose dependent reduction of food intake and body weight.
