Insulin efsitora alfa

Insulin efsitora alfa (LY-3209590) is a selective agonist of insulin receptor (IR). Insulin efsitora alfa is a fusion protein composed of human IR agonists fused with the crystallizable (Fc) domain of human immunoglobulin G2 (IgG2) fragment, with a molecular weight of 64.1 kDa. Insulin efsitora alfa is well tolerated and has potential applications in diabetes patients[1].

Research Areas >> Metabolic Disease

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Insulin Receptor

Insulin efsitora alfa (0.01-100 nM) 在 HEK293 细胞中刺激人胰岛素受体同种型 A (hIR-A) 和人胰岛素受体亚型 B (hIR-B) 磷酸化，EC50 值分别为 4241 nM和 391 nM[2]。 Insulin efsitora alfa (20 µM；30 min) 显著促进 hIR-A 和 hIR-B 去磷酸化[2]。 Insulin efsitora alfa 刺激 3T3-L1 脂肪细胞的脂质生成和 SAOS-2 与 H4IIE 细胞的细胞增殖，EC50 值分别为 19 nM、134 nM 和 20 nM[2]。

Insulin efsitora alfa (3、10 和 30 nmol/kg；皮下注射；单剂量) 在使用链脲佐菌素 (Streptozotocin，HY-13753) 治疗的糖尿病大鼠中显著降低了血糖[2]。

[1]. Heise T, et al. Pharmacokinetic and pharmacodynamic properties of the novel basal insulin Fc (insulin efsitora alfa), an insulin fusion protein in development for once-weekly dosing for the treatment of patients with diabetes. Diabetes Obes Metab. 2023 Apr;25(4):1080-1090.  

[2]. Moyers JS, et al. Preclinical Characterization of LY3209590, a Novel Weekly Basal Insulin Fc-Fusion Protein. J Pharmacol Exp Ther. 2022 Sep;382(3):346-355.