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Volumn 92, Issue 1, 2012, Pages 29-39

A multiple-ascending-dose study to evaluate safety, pharmacokinetics, and pharmacodynamics of a novel GPR40 agonist, TAK-875, in subjects with type 2 diabetes

Author keywords

[No Author keywords available]

Indexed keywords

ANTIDIABETIC AGENT; G PROTEIN COUPLED RECEPTOR 40; PLACEBO; TAK 875; UNCLASSIFIED DRUG;

EID: 84862589520     PISSN: 00099236     EISSN: 15326535     Source Type: Journal    
DOI: 10.1038/clpt.2012.43     Document Type: Article
Times cited : (82)

References (21)
  • 1
    • 0037434991 scopus 로고    scopus 로고
    • Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40
    • Itoh, Y. et al. Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40. Nature 422, 173-176 (2003).
    • (2003) Nature , vol.422 , pp. 173-176
    • Itoh, Y.1
  • 2
    • 0037838892 scopus 로고    scopus 로고
    • The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids
    • Briscoe, C.P. et al. The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids. J. Biol. Chem. 278, 11303-11311 (2003).
    • (2003) J. Biol. Chem. , vol.278 , pp. 11303-11311
    • Briscoe, C.P.1
  • 3
    • 0037423719 scopus 로고    scopus 로고
    • A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs
    • Kotarsky, K., Nilsson, N.E., Flodgren, E., Owman, C. & Olde, B. A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs. Biochem. Biophys. Res. Commun. 301, 406-410 (2003).
    • (2003) Biochem. Biophys. Res. Commun. , vol.301 , pp. 406-410
    • Kotarsky, K.1    Nilsson, N.E.2    Flodgren, E.3    Owman, C.4    Olde, B.5
  • 4
    • 65549114432 scopus 로고    scopus 로고
    • Overexpression of GPR40 in pancreatic beta-cells augments glucose-stimulated insulin secretion and improves glucose tolerance in normal and diabetic mice
    • Nagasumi, K. et al. Overexpression of GPR40 in pancreatic beta-cells augments glucose-stimulated insulin secretion and improves glucose tolerance in normal and diabetic mice. Diabetes 58, 1067-1076 (2009).
    • (2009) Diabetes , vol.58 , pp. 1067-1076
    • Nagasumi, K.1
  • 5
    • 29144463108 scopus 로고    scopus 로고
    • GPR40, a free fatty acid receptor on pancreatic beta cells, regulates insulin secretion
    • Itoh, Y. & Hinuma, S. GPR40, a free fatty acid receptor on pancreatic beta cells, regulates insulin secretion. Hepatol. Res. 33, 171-173 (2005).
    • (2005) Hepatol. Res. , vol.33 , pp. 171-173
    • Itoh, Y.1    Hinuma, S.2
  • 6
    • 79952261037 scopus 로고    scopus 로고
    • Design, synthesis, and biological activity of potent and orally available G protein-coupled receptor 40 agonists
    • Sasaki, S. et al. Design, synthesis, and biological activity of potent and orally available G protein-coupled receptor 40 agonists. J. Med. Chem. 54, 1365-1378 (2011).
    • (2011) J. Med. Chem. , vol.54 , pp. 1365-1378
    • Sasaki, S.1
  • 7
    • 84858229848 scopus 로고    scopus 로고
    • A selective GPR40 agonist, TAK-875, stimulates glucose-dependent insulin secretion without beta cell toxicity and decreases glycosylated hemoglobin levels in diabetic rats
    • Abstract
    • Takeuchi, K., Tsujihata, Y., Ito, R., Suzuki, M., Harada, A. & Hazama, M. A selective GPR40 agonist, TAK-875, stimulates glucose-dependent insulin secretion without beta cell toxicity and decreases glycosylated hemoglobin levels in diabetic rats. Diabetologia. 53, S353 (Abstract) (2010).
    • (2010) Diabetologia , vol.53
    • Takeuchi, K.1    Tsujihata, Y.2    Ito, R.3    Suzuki, M.4    Harada, A.5    Hazama, M.6
  • 8
    • 80053168996 scopus 로고    scopus 로고
    • 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
    • e-pub ahead of print 24 May 2011
    • Naik, H.et al. 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); e-pub ahead of print 24 May 2011.
    • (2011) J. Clin. Pharmacol.
    • Naik, H.1
  • 9
    • 80053185708 scopus 로고    scopus 로고
    • Pharmacokinetics, safety and tolerability of single and multiple doses of TAK-875, a novel GPR40 agonist, in Japanese healthy male subjects
    • Abstract
    • Matsuno, K., Hirayama, M., Araki, T., Dote, N., Kondo, T. & Nakamura, K. Pharmacokinetics, safety and tolerability of single and multiple doses of TAK-875, a novel GPR40 agonist, in Japanese healthy male subjects. Diabetes. 59, A193 (Abstract) (2010).
    • (2010) Diabetes , vol.59
    • Matsuno, K.1    Hirayama, M.2    Araki, T.3    Dote, N.4    Kondo, T.5    Nakamura, K.6
  • 10
    • 84859625938 scopus 로고    scopus 로고
    • TAK-875, a G protein-coupled receptor 40 agonist, for the treatment of type 2 diabetes mellitus: A phase ii, randomized, double-blind, placebo- And active-controlled study
    • Burant, C. et al. TAK-875, a G protein-coupled receptor 40 agonist, for the treatment of type 2 diabetes mellitus: a phase ii, randomized, double-blind, placebo- and active-controlled study. Lancet 379, 1403-1411 (2012).
    • (2012) Lancet , vol.379 , pp. 1403-1411
    • Burant, C.1
  • 11
    • 55249114365 scopus 로고    scopus 로고
    • Diabetic nephropathy: Important pathophysiologic mechanisms
    • Soldatos, G. & Cooper, M.E. Diabetic nephropathy: important pathophysiologic mechanisms. Diabetes Res. Clin. Pract. 82 (suppl. 1), S75-S79 (2008).
    • (2008) Diabetes Res. Clin. Pract. , vol.82 , Issue.SUPPL. 1
    • Soldatos, G.1    Cooper, M.E.2
  • 12
    • 60449089649 scopus 로고    scopus 로고
    • Medical management of hyperglycemia in type 2 diabetes: A consensus algorithm for the initiation and adjustment of therapy: A consensus statement of the American Diabetes Association and the European Association for the Study of Diabetes
    • American Diabetes Association; European Association for the Study of Diabetes
    • Nathan, D.M. et al.; American Diabetes Association; European Association for the Study of Diabetes. Medical management of hyperglycemia in type 2 diabetes: a consensus algorithm for the initiation and adjustment of therapy: a consensus statement of the American Diabetes Association and the European Association for the Study of Diabetes. Diabetes Care 32, 193-203 (2009).
    • (2009) Diabetes Care , vol.32 , pp. 193-203
    • Nathan, D.M.1
  • 13
    • 59149102061 scopus 로고    scopus 로고
    • Management of blood glucose in type 2 diabetes mellitus
    • Ripsin, C.M., Kang, H. & Urban, R.J. Management of blood glucose in type 2 diabetes mellitus. Am. Fam. Physician 79, 29-36 (2009).
    • (2009) Am. Fam. Physician , vol.79 , pp. 29-36
    • Ripsin, C.M.1    Kang, H.2    Urban, R.J.3
  • 14
    • 84856019616 scopus 로고    scopus 로고
    • The effects of TAK-875, a selective G protein-coupled receptor 40/free fatty acid 1 agonist, on insulin and glucagon secretion in isolated rat and human islets
    • Yashiro, H., Tsujihata, Y., Takeuchi, K., Hazama, M., Johnson, P.R. & Rorsman, P. The effects of TAK-875, a selective G protein-coupled receptor 40/free fatty acid 1 agonist, on insulin and glucagon secretion in isolated rat and human islets. J. Pharmacol. Exp. Ther. 340, 483-489 (2012).
    • (2012) J. Pharmacol. Exp. Ther. , vol.340 , pp. 483-489
    • Yashiro, H.1    Tsujihata, Y.2    Takeuchi, K.3    Hazama, M.4    Johnson, P.R.5    Rorsman, P.6
  • 15
    • 52749098923 scopus 로고    scopus 로고
    • Gpr40 is expressed in enteroendocrine cells and mediates free fatty acid stimulation of incretin secretion
    • Edfalk, S., Steneberg, P. & Edlund, H. Gpr40 is expressed in enteroendocrine cells and mediates free fatty acid stimulation of incretin secretion. Diabetes 57, 2280-2287 (2008).
    • (2008) Diabetes , vol.57 , pp. 2280-2287
    • Edfalk, S.1    Steneberg, P.2    Edlund, H.3
  • 16
    • 0036797157 scopus 로고    scopus 로고
    • Treating hyperglycemia in type 2 diabetes: New goals and strategies
    • Lebovitz, H.E. Treating hyperglycemia in type 2 diabetes: new goals and strategies. Cleve. Clin. J. Med. 69, 809-820 (2002).
    • (2002) Cleve. Clin. J. Med. , vol.69 , pp. 809-820
    • Lebovitz, H.E.1
  • 17
    • 33644817974 scopus 로고    scopus 로고
    • Hypoglycemia in type 2 diabetes: Pathophysiology, frequency, and effects of different treatment modalities
    • Zammitt, N.N. & Frier, B.M. Hypoglycemia in type 2 diabetes: pathophysiology, frequency, and effects of different treatment modalities. Diabetes Care 28, 2948-2961 (2005).
    • (2005) Diabetes Care , vol.28 , pp. 2948-2961
    • Zammitt, N.N.1    Frier, B.M.2
  • 18
    • 45149131667 scopus 로고    scopus 로고
    • Effects of intensive glucose lowering in type 2 diabetes
    • Action to Control Cardiovascular Risk in Diabetes Study Group
    • Action to Control Cardiovascular Risk in Diabetes Study Group. Effects of intensive glucose lowering in type 2 diabetes. N. Engl. J. Med. 358, 2545-2559 (2008).
    • (2008) N. Engl. J. Med. , vol.358 , pp. 2545-2559
  • 20
    • 77957742069 scopus 로고    scopus 로고
    • Severe hypoglycemia and risks of vascular events and death
    • ADVANCE Collaborative Group
    • Zoungas, S. et al.; ADVANCE Collaborative Group. Severe hypoglycemia and risks of vascular events and death. N. Engl. J. Med. 363, 1410-1418 (2010).
    • (2010) N. Engl. J. Med. , vol.363 , pp. 1410-1418
    • Zoungas, S.1
  • 21
    • 80053138180 scopus 로고    scopus 로고
    • TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats
    • Tsujihata, Y. et al. TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats. J. Pharmacol. Exp. Ther. 339, 228-237 (2011).
    • (2011) J. Pharmacol. Exp. Ther. , vol.339 , pp. 228-237
    • Tsujihata, Y.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.