Synonyms: HMS-5552 | HMS5552 | RO-5305552 | RO5305552 | Sinogliatin
dorzagliatin is an approved drug (China (2022))
Compound class:
Synthetic organic
Comment: Dorzagliatin (HMS5552) is an allosteric glucokinase (GCK) activator [3,5], that targets both pancreatic and hepatic GCK, and is a 'full' activator that increases GCK's maximum velocity (Vmax) [7]. GCK activators are being developed as novel drugs for the treatment of type 2 diabetes mellitus (T2DM) [1-2,4].
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References |
1. Bloomgarden Z. (2019)
Glucokinase and the potential of glucokinase activation in type 2 diabetes. J Diabetes, 11 (8): 626-627. [PMID:31013387] |
2. Grimsby J, Sarabu R, Corbett WL, Haynes NE, Bizzarro FT, Coffey JW, Guertin KR, Hilliard DW, Kester RF, Mahaney PE et al.. (2003)
Allosteric activators of glucokinase: potential role in diabetes therapy. Science, 301 (5631): 370-3. [PMID:12869762] |
3. Sharma P, Singh S, Sharma N, Singla D, Guarve K, Grewal AS. (2022)
Targeting human Glucokinase for the treatment of type 2 diabetes: an overview of allosteric Glucokinase activators. J Diabetes Metab Disord, 21 (1): 1129-1137. [PMID:35673438] |
4. Toulis KA, Nirantharakumar K, Pourzitaki C, Barnett AH, Tahrani AA. (2020)
Glucokinase Activators for Type 2 Diabetes: Challenges and Future Developments. Drugs, 80 (5): 467-475. [PMID:32162273] |
5. Wang P, Liu H, Chen L, Duan Y, Chen Q, Xi S. (2017)
Effects of a Novel Glucokinase Activator, HMS5552, on Glucose Metabolism in a Rat Model of Type 2 Diabetes Mellitus. J Diabetes Res, 2017: 5812607. [PMID:28191470] |
6. Yang W, Zhu D, Gan S, Dong X, Su J, Li W, Jiang H, Zhao W, Yao M, Song W et al.. (2022)
Dorzagliatin add-on therapy to metformin in patients with type 2 diabetes: a randomized, double-blind, placebo-controlled phase 3 trial. Nat Med, 28 (5): 974-981. [PMID:35551292] |
7. Zhu XX, Zhu DL, Li XY, Li YL, Jin XW, Hu TX, Zhao Y, Li YG, Zhao GY, Ren S et al.. (2018)
Dorzagliatin (HMS5552), a novel dual-acting glucokinase activator, improves glycaemic control and pancreatic β-cell function in patients with type 2 diabetes: A 28-day treatment study using biomarker-guided patient selection. Diabetes Obes Metab, 20 (9): 2113-2120. [PMID:29707866] |