"目录号: HY-14771
EpigeneticsPI3K/Akt/mTOR-
Imeglimin(EMD-387008)是口服的抗糖尿病化合物，可作用于肝，肌肉和胰腺中的β细胞。
AMPK
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生物活性
Description
Imeglimin(EMD-387008) is the first in a new tetrahydrotriazine-containing class of oral antidiabetic agents, the glimins; It has been shown to act on the liver, muscle and pancreatic β-cells to uniquely target the key defects of type 2 diabetes.IC50 Value: Target: AMPK stimulatorin vitro: in vivo: A total of 156 patients were randomized 1:1 to receive imeglimin (1,500 mg twice a day) or placebo added to a stable dose of metformin (1,500-2,000 mg/day). Change in A1C from baseline was the primary efficacy outcome; secondary outcomes included fasting plasma glucose (FPG) and proinsulin/insulin ratio [1]. In a 4-week phase IIa, three-arm parallel group study, patients were randomized to imeglimin 2000 mg once daily (od), imeglimin 1000 mg twice daily (bid) or metformin 850 mg bid and responses to an oral glucose tolerance test (OGTT) were measured. In an 8-week phase IIa, four-arm controlled multi-centre study, patients were randomized to imeglimin 500 mg bid, imeglimin 1500 mg bid, metformin 850 mg bid or placebo [2].
Clinical Trial
NCT02373150
Poxel SA
Type 2 Diabetes Mellitus
February 2015
Phase 1
NCT02924337
Poxel SA
Qt Interval, Variation in
September 2016
Phase 1
NCT01951235
Poxel SA
Type 2 Diabetes Mellitus
January 2013
Phase 2
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References
[1].Fouqueray P, et al. The efficacy and safety of imeglimin as add-on therapy in patients with type 2 diabetes inadequately controlled with metformin monotherapy. Diabetes Care. 2013 Mar;36(3):565-8.
[2].Pirags V, et al. Imeglimin, a novel glimin oral antidiabetic, exhibits a good efficacy and safety profile in type 2 diabetic patients. Diabetes Obes Metab. 2012 Sep;14(9):852-8.
[3].F Wagner, et al. Effects of the anti-diabetic imeglimin in hyperglycemic mice with septic shock. Crit Care. 2012; 16(Suppl 1): P21.