TAK-875: Free fatty acid receptor FFA1 agonist insulin secretagogue treatment of type 2 diabetes

Drugs of the Future

Volumn 36, Issue 11, 2011, Pages 813-818

  De Lartigue, J ^a  

^a NONE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

2 [6 [2',6' DIMETHYL 4' [3 (METHYLSULFONYL)PROPOXY]BIPHENYL 3 YLMETHOXY] 2,3 DIHYDRO 1 BENZOFURAN 3 YL]ACETIC ACID; ANTIDIABETIC AGENT; BENZOFURAN DERIVATIVE; G PROTEIN COUPLED RECEPTOR 40; GLIMEPIRIDE; GLYCOSYLATED HEMOGLOBIN; INCRETIN; MEGLITINIDE; SULFONYLUREA DERIVATIVE; TAK 875; UNCLASSIFIED DRUG;

ARTICLE; CLINICAL TRIAL (TOPIC); DIET RESTRICTION; DRUG ACTIVITY; DRUG MECHANISM; DRUG METABOLISM; DRUG TOLERABILITY; EUROPE; HUMAN; HYPERGLYCEMIA; HYPOGLYCEMIA; INSULIN RELEASE; JAPAN; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; POSTPRANDIAL STATE; SINGLE DRUG DOSE; UNITED STATES;

EID: 84952985213     PISSN: 03778282     EISSN: None     Source Type: Journal    
DOI: 10.1358/dof.2011.036.11.1722071     Document Type: Article

References (23)

1. Negoro, N., Sasaki, S., Mikami, S. et al. Discovery of TAK-875: A potent, selective, and orally bioavailable GPR40 agonist. ACS Med Chem Lett 2010, 1: 290-4.
2. Yasuma, T., Negoro, N., Yamashita, M., Itou, M. (Takeda Pharmaeutical Co., Ltd.). Fused cyclic compounds. CA 2656003, EP 2041123, EP 2248812, JP 2009280585, JP 2009542580, US 2010004312, US 7732626, WO 2008001931.
3. Maedler, K., Carr, R., Bosco, D., Zuellig, R., Berney, T., Donath, M. Sulfonylurea induced beta-cell apoptosis in cultured human islets. J Clin Endocrinol Metab 2005, 90(1): 501-6. (Pubitemid 40116700)
4. Cryer, P. Hypoglycemia: The limiting factor in the glycaemic management of type I and type II diabetes. Diabetologia 2002, 45(7): 937-48. (Pubitemid 34762188)
5. Burge, M., Sood, V., Sobhy, T., Rassam, A., Schade, D. Sulfonylurea-induced hypoglycemia in type 2 diabetes mellitus: A review. Diabetes Obes Metab 1999, 1(4): 199-206.
6. Tzoulaki, I., Molokhia, M., Curcin, V. et al. Risk of cardiovascular disease and all cause mortality among patients with type 2 diabetes prescribed oral antidiabetes drugs: Retrospective cohort study using UK general practice research database. BMJ 2009, 339: b4731.
7. Drucker, D., Nauck, M. The incretin system: Glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. Lancet 2006, 368(9548): 1696-705. (Pubitemid 46048557)
8. Prentki, M., Tonkheim, K., Corkey, B. Signal transduction mechanisms in nutrient-induced insulin secretion. Diabetologia 1997, 40(Suppl. 2): S32-41. (Pubitemid 27306920)
9. Haber, E., Ximenes, H., J, P., Carvahlo, C., Curi, R., Carpinelli, A. Pleiotropic effects of fatty acids on pancreatic beta-cells. J Cell Physiol 2003, 194(1): 1-12. (Pubitemid 35424222)
10. Schyler, S., Horuk, R. I want a new drug: G-protein-coupled receptors in drug development. Drug Discov Today 2006, 11(11-12): 481-93.
11. Milligan, G. G-protein-coupled receptor heterodimers: Pharmacology, function and relevance to drug discovery. Drug Discov Today 2006, 11(11-12): 541-9.
12. Itoh, Y., Kawamata, Y., Harada, M. et al. Free fatty acids regulated insulin secretion from pancreatic beta cells through GPR40. Nature 2003, 422(6928): 173-6. (Pubitemid 36362750)
13. Shapiro, H., Shachar, S., Sekler, I., Hershfinkel, M., Walker, M. Role of GPR40 in fatty acid action on the beta cell line INS-1E. Biochem Biophys Res Commun 2005, 335(1): 97-104. (Pubitemid 41350767)
14. 2+ channel and link to insulin secretion. Am J Physiol Endocrinol Metab 2005, 289(4): E670-E7.
15. Bharate, S., Nemmani, K., Vishwakarma, R. Progress in the discovery and development of small-molecule modulators of G-protein-coupled receptor 40 (GPR40/FFA1/FFA1R): An emerging target for type 2 diabetes. Expert Opin Ther Pat 2009, 19(2): 237-64.
16. Takeuchi, K., Tsujihata, Y., Ito, R., Suzuki, M., Harada, A. A selective GPR40 agonist, TAK-875, stimulates glucose-dependent insulin secretion without beta cell toxicity and decreases blood glycosylated haemoglobin levels in diabetic rats. Diabetologia 2010, 53(Suppl 1): Abst 882.
17. Tsujihata, Y., Ito, R., Suzuki, M. et al. TAK-875, an orally available GPR40/FFA1 agonist enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats. J Pharmacol Exp Ther 2011, 339(1): 228-37.
18. th Annu Meet Eur Assoc Study Diabetes (EASD) (Sept 12-16, Lisbon) 2011, Abst 187:
19. Naik, H., Vakilynejad, M., Wu, J., Viswanathan, P., Dote, N., Higuchi, T., Leifke, E. Safety, tolerability, pharmacokinetics, and pharmacodynamic properties of the GPR40 agonist TAK-875: Results from a double-blind, placebo-controlled single oral dose rising study in healthy volunteers. J Clin Pharmacol 2011, Epub ahead of print.
20. Vakily, M., Wu, J., Viswanathan, P., Leifke, E. A safety, tolerability, pharmacokinetics, and pharmacodynamics and preliminary food-effect study of TAK-875 GPR40 agonist, following oral administration of sequential ascending single doses to healthy subjects. Diabetes 2010, 59(Suppl. 1): Abst 630-P.
21. Matsuno, K., Hirayama, M., Araki, T., Dote, N., Kondo, T. Pharmacokinetics, safety and tolerability of single and multiple doses of TAK-875, a novel GPR40 agonist, in Japanese healthy male subjects. Diabetes 2010, 59(Suppl. 1): Abst 707-P.
22. th Annu Meet Eur Assoc Study Diabetes (EASD) (Sept 12-16, Lisbon) 2011, Abst 187.
23. st Annu Meet Sci Sess Am Diabetes Assoc (ADA) (June 24-28, San Diego) 2011, Abst 0312-OR.