Pharmacokinetic and pharmacodynamic properties of the glucokinase activator MK-0941 in rodent models of type 2 diabetes and healthy dogs

Molecular Pharmacology

Volumn 80, Issue 6, 2011, Pages 1156-1165

  Eiki, Jun Ichi ^a   Nagata, Yasufumi ^a   Futamura, Mayumi ^a   Sasaki Yamamoto, Kaori ^a   Iino, Tomoharu ^a   Nishimura, Teruyuki ^a   Chiba, Masato ^a   Ohyama, Sumika ^a   Yoshida Yoshimioto, Riki ^a   Fujii, Kenji ^a   Hosaka, Hideka ^a   Goto Shimazaki, Hiroko ^a   Kadotani, Akito ^a   Ohe, Tomoyuki ^a   Lin, Songnian ^b   Langdon, Ronald B ^b   Berger, Joel P ^b  

^a BANYU PHARMACEUTICAL CO LTD   (Japan)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 [[ 6 (ETHYLSULFONYL) 3 PYRIDINYL]OXY] 5 (2 HYDROXY 1 METHYLETHOXY) N ( 1 METHYL 1H PYRAZOL 3 YL)BENZAMIDE; ANTIDIABETIC AGENT; BENZAMIDE DERIVATIVE; ENZYME; GLUCOKINASE; GLUCOSE; INSULIN; MK 0941; RECOMBINANT ENZYME; RECOMBINANT GLUCOKINASE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DOG; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; ENZYME ACTIVITY; GLUCOSE METABOLISM; GLUCOSE TRANSPORT; IN VITRO STUDY; INCUBATION TEMPERATURE; INSULIN RELEASE; LIPID DIET; LIVER CELL; MALE; MAXIMUM PLASMA CONCENTRATION; MOUSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; ORAL GLUCOSE TOLERANCE TEST; PANCREAS ISLET; PHARMACODYNAMICS; PHARMACOLOGICAL PARAMETERS; PRIORITY JOURNAL; PROTEIN PHOSPHORYLATION; RODENT; SINGLE DRUG DOSE; TREATMENT DURATION;

ANIMALS; BENZAMIDES; BLOOD GLUCOSE; CELLS, CULTURED; DIABETES MELLITUS, TYPE 2; DISEASE MODELS, ANIMAL; DOGS; ENZYME ACTIVATION; GLUCOKINASE; HUMANS; HYPOGLYCEMIC AGENTS; MALE; MICE; MICE, INBRED C57BL; MICE, INBRED ICR; RATS; RATS, SPRAGUE-DAWLEY; RATS, WISTAR; SULFONES;

EID: 81555204236     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.111.074401     Document Type: Article

References (36)

1. Agius L (1997) Involvement of glucokinase translocation in the mechanism by which resorcinol inhibits glycolysis in hepatocytes. Biochem J 325:667-673.
2. Akgül B, Lin KW, Ou Yang HM, Chen YH, Lu TH, Chen CH, Kikuchi T, Chen YT, and Tu CP (2010) Garlic accelerates red blood cell turnover and splenic erythropoietic gene expression in mice: evidence for erythropoietin-independent erythropoiesis. PLoS One 5:e15358.
3. Bebernitz GR, Beaulieu V, Dale BA, Deacon R, Duttaroy A, Gao J, Grondine MS, Gupta RC, Kakmak M, Kavana M, et al. (2009) Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J Med Chem 52:6142-6152.
4. Bilicki KL, Schermerhorn T, Klocke EE, McMurphy RM, and Roush JK (2010) Evaluation of a real-time, continuous monitor of glucose concentration in healthy dogs during anesthesia. Am J Vet Res 71:11-16.
5. Bonadonna RC, Kapitza C, Heise T, Avogaro A, Boldrin M, Grimsby J, Mulligan ME, Arbet-Engels C, and Balena R (2008) Glucokinase activator RO4389620 improves beta cell function and plasma glucose fluxes in patients with type 2 diabetes. Diabetologia 51 (Suppl 1):S372.
6. Bonadonna RC, Heise T, Arbet-Engels C, Kapitza C, Avogaro A, Grimsby J, Zhi J, Grippo JF, and Balena R (2010) Piragliatin (RO4389620), a novel glucokinase activator, lowers plasma glucose both in the postabsorptive state and after a glucose challenge in patients with type 2 diabetes mellitus: a mechanistic study. J Clin Endocrinol Metab 95:5028-5036.
7. Cryer PE (2008) The barrier of hypoglycemia in diabetes. Diabetes 57:3169-3176.
8. Davis EA, Cuesta-Muñoz A, Raoul M, Buettger C, Sweet I, Moates M, Magnuson MA, and Matschinsky FM (1999) Mutants of glucokinase cause hypoglycaemia- and hyperglycaemia syndromes and their analysis illuminates fundamental quantitative concepts of glucose homeostasis. Diabetologia 42:1175-1186. (Pubitemid 29459813)
9. Fahrbach J, Jacober S, Jiang H, and Martin S (2008) The DURABLE trial study design: comparing the safety, efficacy, and durability of insulin glargine to insulin lispro mix 75/25 added to oral antihyperglycemic agents in patients with type 2 diabetes. J Diabetes Sci Technol 2:831-838.
10. Folch J, Lees M, and Sloane Stanley GH (1957) A simple method for the isolation and purification of total lipides from animal tissues. J Biol Chem 226:497-509.
11. Futamura M, Hosaka H, Kadotani A, Shimazaki H, Sasaki K, Ohyama S, Nishimura T, Eiki J, and Nagata Y (2006) An allosteric activator of glucokinase impairs the interaction of glucokinase and glucokinase regulatory protein and regulates glucose metabolism. J Biol Chem 281:37668-37674. (Pubitemid 46042070)
12. Fyfe MC, White JR, Taylor A, Chatfield R, Wargent E, Printz RL, Sulpice T, McCormack JG, Procter MJ, Reynet C, et al. (2007) Glucokinase activator PSN-GK1 displays enhanced antihyperglycaemic and insulinotropic actions. Diabetologia 50:1277-1287. (Pubitemid 46701554)
13. Gotoh M, Maki T, Kiyoizumi T, Satomi S, and Monaco AP (1985) An improved method for isolation of mouse pancreatic islets. Transplantation 40:437-438. (Pubitemid 16215266)
14. 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 301:370-373. (Pubitemid 36877072)
15. Grimsby J, Berthel SJ, and Sarabu R (2008) Glucokinase activators for the potential treatment of type 2 diabetes. Curr Top Med Chem 8:1524-1532.
16. Kahn SE, Haffner SM, Heise MA, Herman WH, Holman RR, Jones NP, Kravitz BG, Lachin JM, O'Neill MC, Zinman B, et al. (2006) Glycemic durability of rosiglitazone, metformin, or glyburide monotherapy. N Engl J Med 355:2427-2443. (Pubitemid 44903747)
17. Kamata K, Mitsuya M, Nishimura T, Eiki J, and Nagata Y (2004) Structural basis for allosteric regulation of the monomeric allosteric enzyme human glucokinase. Structure 12:429-438. (Pubitemid 38353064)
18. Klueh U, Liu Z, Cho B, Ouyang T, Feldman B, Henning TP, Kaur M, and Kreutzer D (2006) Continuous glucose monitoring in normal mice and mice with prediabetes and diabetes. Diabetes Technol Ther 8:402-412. (Pubitemid 46100534)
19. Levin BE, Becker TC, Eiki J, Zhang BB, and Dunn-Meynell AA (2008) Ventromedial hypothalamic glucokinase is an important mediator of the counterregulatory response to insulin-induced hypoglycemia. Diabetes 57:1371-1379.
20. Matschinsky FM, Magnuson MA, Zelent D, Jetton TL, Doliba N, Han Y, Taub R, and Grimsby J (2006) The network of glucokinase-expressing cells in glucose homeostasis and the potential of glucokinase activators for diabetes therapy. Diabetes 55:1-12. (Pubitemid 43343293)
21. Matschinsky FM (2009) Assessing the potential of glucokinase activators in diabetes therapy. Nat Rev Drug Discov 8:399-416.
22. Matschinsky FM and Porte D (2010) Glucokinase activators (GKAs) promise a new pharmacotherapy for diabetics. F1000 Med Rep 2. pii:43.
23. Meininger GE, Scott R, Alba M, Shentu Y, Luo E, Amin H, Davies MJ, Kaufman KD, and Goldstein BJ (2011) Effects of MK-0941, a novel glucokinase activator, on glycemic control in insulin-treated patients with type 2 diabetes. Diabetes Care doi:10.2337/dc11-1200.
24. Migoya EM, Miller J, Laetham T, Maganti L, Gottesdeiner K, and Wagner JA (2009) The glucokinase (GK) activator MK-0599 lowers plasma glucose concentrations in healthy non-diabetic subjects. Diabetologia 52 (Suppl 1):S344.
25. Mu J, Woods J, Zhou YP, Roy RS, Li Z, Zycband E, Feng Y, Zhu L, Li C, Howard AD, et al. (2006) Chronic inhibition of dipeptidyl peptidase-4 with a sitagliptin analog preserves pancreatic beta-cell mass and function in a rodent model of type 2 diabetes. Diabetes 55:1695-1704. (Pubitemid 44324122)
26. Ohyama S, Takano H, Iino T, Nishimura T, Zhou YP, Langdon RB, Zhang BB, and Eiki J (2010) A small-molecule glucokinase activator lowers blood glucose in the sulfonylurea-desensitized rat. Eur J Pharmacol 640:250-256.
27. 2+ in impaired sensitivity to glucose of rat pancreatic islets exposed to high glucose in vitro. Diabetes 41:1555-1561.
28. Okeda T, Ono J, Takaki R, and Todo S (1979) Simple method for the collection of pancreatic islets by the use of Ficoll-Conray gradient. Endocrinol Jpn 26:495-499. (Pubitemid 10196972)
29. Rustenbeck I (2002) Desensitization of insulin secretion. Biochem Pharmacol 63:1921-1935.
30. Sarabu R, Berthel SJ, Kester RF, and Tilley JW (2008) Glucokinase activators as new type 2 diabetic therapeutic agents. Expert Opin Ther Pat 18:759-768.
31. Sarabu R, Berthel SJ, Kester RF, and Tilley JW (2011) Novel glucokinase activators: a patent review (2008-2010). Expert Opin Ther Pat 21:13-33.
32. Seglen PO (1976) Preparation of isolated rat liver cells. Methods Cell Biol 13:29-83.
33. Tabata H, Kitamura T, and Nagamatsu N (1998) Comparison of effects of restraint, cage transportation, anaesthesia and repeated bleeding on plasma glucose levels between mice and rats. Lab Anim 32:143-148. (Pubitemid 28185296)
34. Wåhlin-Boll E, Sartor G, Melander A, and Scherstén B (1982) Impaired effect of sulfonylurea following increased dosage. Eur J Clin Pharmacol 22:21-25.
35. Zhai S, Mulligan ME, Grimsby J, Arbet-Engels C, Boldrin M, Balena R, and Zhi J. (2008) Phase I assessments of a novel glucokinase activator RO4389620 in healthy male volunteers. Diabetologia 51 (Suppl 1):S372.
36. Zhi J, Zhai S, Mulligan M, Grimsby J, Arbet-Engels C, Boldrin M, and Balena R (2008) A novel glucokinase activator RO4389620 improved fasting and postprandial plasma glucose in type 2 diabetic patients. Diabetologia 51:S23.