American Diabetes Association Professional Practice Committee. 2. Classification and diagnosis of diabetes: standards of medical care in diabetes-2022. Diabetes Care. 2022;45(Suppl. 1):S17–38.
American Diabetes Association Professional Practice Committee. 9. Pharmacologic approaches to glycemic treatment: standards of medical care in diabetes-2022. Diabetes Care. 2022;45(Suppl. 1):S125–43.
Ji LN, Lu JM, Guo XH, Yang WY, Weng JP, Jia WP, et al. Glycemic control among patients in China with type 2 diabetes mellitus receiving oral drugs or injectables. BMC Public Health. 2013;21(13):602.
Lin X, Xu Y, Pan X, Xu J, Ding Y, Sun X, et al. Global, regional, and national burden and trend of diabetes in 195 countries and territories: an analysis from 1990 to 2025. Sci Rep. 2020;10(1):14790.
Article CAS PubMed PubMed Central Google Scholar
Matschinsky FM, Wilson DF. The central role of glucokinase in glucose homeostasis: a perspective 50 years after demonstrating the presence of the enzyme in islets of Langerhans. Front Physiol. 2019;10:148.
Article PubMed PubMed Central Google Scholar
Doliba NM, Qin W, Najafi H, Liu C, Buettger CW, Sotiris J, et al. Glucokinase activation repairs defective bioenergetics of islets of Langerhans isolated from type 2 diabetics. Am J Physiol Endocrinol Metab. 2012;302(1):E87-102.
Article CAS PubMed Google Scholar
Matschinsky FM. Glucokinase, glucose homeostasis, and diabetes mellitus. Curr Diab Rep. 2005;5(3):171–6.
Article CAS PubMed Google Scholar
Ren Y, Li L, Wan L, Huang Y, Cao S. Glucokinase as an emerging anti-diabetes target and recent progress in the development of its agonists. J Enzyme Inhib Med Chem. 2022;37(1):606–15.
Article CAS PubMed PubMed Central Google Scholar
Spasov AA, Lobasenko VS, Kosolapov VA, Babkov DA, Kuznetsova VA, Maika OY, et al. Synthesis and pharmacological activity of 3-phenoxybenzoic acid derivatives. Pharm Chem J. 2020;54(3):229–35.
Dzyurkevich MS, Babkov DA, Shtyrlin NV, Mayka OY, Iksanova AG, Vassiliev PM, et al. Pyridoxine dipharmacophore derivatives as potent glucokinase activators for the treatment of type 2 diabetes mellitus. Sci Rep. 2017;7(1):16072.
Article PubMed PubMed Central Google Scholar
Li W, Zhang X, Sun Y, Liu Z. Recent clinical advances of glucokinase activators in the treatment of diabetes mellitus type 2. Pharmazie. 2020;75(6):230–5.
Toulis KA, Nirantharakumar K, Pourzitaki C, Barnett AH, Tahrani AA. Glucokinase activators for type 2 diabetes: challenges and future developments. Drugs. 2020;80(5):467–75.
Article CAS PubMed Google Scholar
Zhi J, Zhai S. Effects of piragliatin, a glucokinase activator, on fasting and postprandial plasma glucose in patients with type 2 diabetes mellitus. J Clin Pharmacol. 2016;56(2):231–8.
Article CAS PubMed Google Scholar
Kiyosue A, Hayashi N, Komori H, Leonsson-Zachrisson M, Johnsson E. Dose-ranging study with the glucokinase activator AZD1656 as monotherapy in Japanese patients with type 2 diabetes mellitus. Diabetes Obes Metab. 2013;15(10):923–30.
Article CAS PubMed Google Scholar
Meininger GE, Scott R, Alba M, Shentu Y, Luo E, Amin H, et al. Effects of MK-0941, a novel glucokinase activator, on glycemic control in insulin-treated patients with type 2 diabetes. Diabetes Care. 2011;34(12):2560–6.
Article CAS PubMed PubMed Central Google Scholar
Yang W, Zhu D, Gan S, Dong X, Su J, Li W, et al. Dorzagliatin add-on therapy to metformin in patients with type 2 diabetes: a randomized, double-blind, placebo-controlled phase 3 trial. Nat Med. 2022;28(5):974–81.
Article CAS PubMed PubMed Central Google Scholar
Pfefferkorn JA, Guzman-Perez A, Oates PJ, Litchfield J, Aspnes G, Basak A, et al. Designing glucokinase activators with reduced hypoglycemia risk: discovery of N, N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm. 2011;2(9):828–39.
Amin NB, Aggarwal N, Pall D, Paragh G, Denney WS, Le V, et al. Two dose-ranging studies with PF-04937319, a systemic partial activator of glucokinase, as add-on therapy to metformin in adults with type 2 diabetes. Diabetes Obes Metab. 2015;17(8):751–9.
Article CAS PubMed Google Scholar
Denney WS, Denham DS, Riggs MR, Amin NB. Glycemic effect and safety of a systemic, partial glucokinase activator, PF-04937319, in patients with type 2 diabetes mellitus inadequately controlled on metformin: a randomized, crossover, active-controlled study. Clin Pharmacol Drug Dev. 2016;5(6):517–27.
Article CAS PubMed Google Scholar
Liu D, Du Y, Yao X, Wei Y, Zhu J, Cui C, et al. Safety, tolerability, pharmacokinetics, and pharmacodynamics of the glucokinase activator PB-201 and its effects on the glucose excursion profile in drug-naïve Chinese patients with type 2 diabetes: a randomised controlled, crossover, single-centre phase 1 trial. EClinicalMedicine. 2021;42: 101185.
Article PubMed PubMed Central Google Scholar
Bergstrand M, Karlsson MO. Handling data below the limit of quantification in mixed effect models. AAPS J. 2009;11(2):371–80.
Article CAS PubMed PubMed Central Google Scholar
Gao W, Jusko WJ. Modeling disease progression and rosiglitazone intervention in type 2 diabetic Goto-Kakizaki rats. J Pharmacol Exp Ther. 2012;341(3):617–25.
Article CAS PubMed PubMed Central Google Scholar
Borzilleri KA, Pfefferkorn JA, Guzman-Perez A, Liu SP, Qiu XY, Chrunyk BA, et al. Optimizing glucokinase activator binding kinetics to lower in vivo hypoglycemia risk. Medchemcomm. 2014;5(6):802–7.
Borg R, Kuenen JC, Carstensen B, Zheng H, Nathan DM, Heine RJ, et al. Associations between features of glucose exposure and A1C: the A1C-Derived Average Glucose (ADAG) study. Diabetes. 2010;59(7):1585–90.
Article CAS PubMed PubMed Central Google Scholar
Gaitonde P, Garhyan P, Link C, Chien JY, Trame MN, Schmidt S. A comprehensive review of novel drug-disease models in diabetes drug development. Clin Pharmacokinet. 2016;55(7):769–88.
Article CAS PubMed Google Scholar
Savic RM, Karlsson MO. Importance of shrinkage in empirical bayes estimates for diagnostics: problems and solutions. AAPS J. 2009;11(3):558–69.
Article PubMed PubMed Central Google Scholar
Sharma R, Litchfield J, Atkinson K, Eng H, Amin NB, Denney WS, et al. Metabolites in safety testing assessment in early clinical development: a case study with a glucokinase activator. Drug Metab Dispos. 2014;42(11):1926–39.
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