MK-767 Kyorin/Banyu/Merck

Current Opinion in Investigational Drugs

Volumn 4, Issue 4, 2003, Pages 444-448

  Calkin, Anna C ^a   Thomas, Merlin C ^a   Cooper, Mark E ^a  

^a BAKER IDI HEART AND DIABETES INSTITUTE   (Australia)

Author keywords

[No Author keywords available]

Indexed keywords

2,4 THIAZOLIDINEDIONE DERIVATIVE; 5 (2,4 DIOXO 5 THIAZOLIDINYLMETHYL) 2 METHOXY N [4 (TRIFLUOROMETHYL)BENZYL]BENZAMIDE; BEZAFIBRATE; FARGLITAZAR; GLUCOSE; LIPID; NETOGLITAZONE; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR AGONIST; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA; PIOGLITAZONE; RAGAGLITAZAR; REGLITAZAR; ROSIGLITAZONE; TESAGLITAZAR; TROGLITAZONE; UNCLASSIFIED DRUG;

CLINICAL TRIAL; DOSE RESPONSE; DRUG ACTIVITY; DRUG EFFICACY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; FLUID RETENTION; GLUCOSE TRANSPORT; HUMAN; HYPERGLYCEMIA; LIPID METABOLISM; METABOLIC PARAMETERS; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; REVIEW; SIDE EFFECT; STRUCTURE ACTIVITY RELATION; WEIGHT GAIN;

ANIMALS; CLINICAL TRIALS, PHASE I; CLINICAL TRIALS, PHASE II; CLINICAL TRIALS, PHASE III; DIABETES MELLITUS, TYPE 2; HUMANS; HYPOGLYCEMIC AGENTS; THIAZOLES; THIAZOLIDINES;

EID: 0037531293     PISSN: 14724472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (33)

1. 226454 Thiazolidinediones produce a conformational change in peroxisomal proliferator-activated receptor-γ: Binding and activation correlate with antidiabetic actions in db/db mice. Berger J, Bailey P, Biswas C, Cullinan CA, Doebber TW, Hayes NS, Saperstein R, Smith RG, Leibowitz MD Endocrinology 1996 137 10 4189-4195
2. 309730 N-(2-Benzoylphenyl)-L-tyrosine PPARγ agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents. Henke BR, Blanchard SG, Brackeen MF, Brown KK, Cobb JE, Collins JL, Harrington WW, Hashim MA, Hull Ryde EA, Kaldor I, Kliewer SA et al J Med Chem 1998 41 25 5020-5036
3. 311944 A novel insulin sensitizer acts as a coligand for peroxisome proliferator-activated receptor-α (PPAR-α) and PPAR-γ. Effects of PPAR-α activation on abnormal lipid metabolism in liver of Zucker fatty rats. Murakami K, Tobe K, Ide T, Mochizuki T, Ohashi M, Akanuma Y, Yazaki Y, Kadowaki T Diabetes 1998 47 12 1841-1847
4. 315791 (3-Substituted benzyl)thiazolidine-2,4-diones as structurally new antihyperglycemic agents. Nomura M, Kinoshita S, Satoh H, Maeda T, Murakami K, Tsunoda M, Miyachi H, Awano K Bioorg Med Chem Lett 1999 9 4 533-538 Outlines the discovery of MK-767 from a series of 3-[(2,4-dioxothiazolidin-5-yl)methyl]benzamide derivatives, and demonstrates its potency as an antihyperglycemic agent.
5. 347848 Kyorin licenses diabetes treatment KRP-297 to Merck. Pharma Jpn 1999 1671 9
6. 348301 KRP-297 improves impaired fatty acid oxidation in skeletal muscles and livers of Zucker diabetic fatty rats. Ide T, Murakami K, Tsunoda M, Mochizuki T, Kadowaki T Diabetologia 1999 42 Suppl 1 Abs 50
7. 355614 Amelioration by KRP-297, a new thiazolidinedione, of impaired glucose uptake in skeletal muscle from obese insulin-resistant animals. Murakami K, Tsunoda M, Ide T, Ohashi M, Mochizuki T Metab Clin Exp 1999 48 11 1450-1454
8. 365321 Thiazolidinediones: An update. Schoonjans K, Auwerx J Lancet 2000 355 9208 1008-1010
9. 389646 Drug development update (Merck) - KRP-297. Merck Research Laboratories Company Communication 2000 November 14
10. 394354 Central role of peroxisome proliferator-activated receptors in the actions of peroxisome proliferators. Corton JC, Anderson SP, Stauber A Annu Rev Pharmacol Toxicol 2000 40 491-518
11. 395849 Tissue-specific actions of antidiabetic thiazolidinediones on the reduced fatty acid oxidation in skeletal muscle and liver of Zucker diabetic fatty rats. Ide T, Nakazawa T, Mochizuki T, Murakami K Metabolism 2000 49 4 521-525
12. 395851 Fenofibrate and rosiglitazone lower serum triglycerides with opposing effects on body weight. Chaput E, Saladin R, Silvestre M, Edgar AD Biochem Biophys Res Commun 2000 271 2 445-450 Demonstrates that co-administration of rosiglitazone and fenofibrate has no additional effect on glucose or triglyceride levels compared with either agent alone.
13. 400514 Drugs under development in Japanese companies. Pharma Jpn 2001 1735 9-13
14. 412881 Characterisation of a future generation insulin sensitizers in vitro and in vivo. Wulff EM, Jeppesen L, Bury PS, Mogensen JP, Fleckner J, Andersen A-ST, Wassermanm K, Sauerberg P Diabetes 2001 50 Suppl 2 Abs 2210-PO Compares the activity and antidiabetic effects of a number of new PPAR agonists currently under investigation.
15. 412933 Effects of pioglitazone and KRP-297 on insulin secretion in normal and db/db mice using in situ pancreatic perfusion. Yajima K, Hirose H, Fujita H, Seto Y, Fujita Y, Uketa K, Kawai T, Yamamoto Y, Saruta T Diabetes 2001 50 Suppl 2 Abs 2237-PO
16. 415122 American Diabetes Association - 61st Scientific Sessions (Part VI), Philadelphia, PA, USA. Hopfner R IDDB Meeting Report 2001 June 22-26
17. 420809 Pharmaceutical desk reference: Global equities research US - Our models of the major US pharma companies. Lehman Brothers Inc 2001 August
18. 420816 2Q01 preview and model book - The poor prognosis for drugs. Deutsche Banc Alex Brown - US 2001 June 25
19. 427414 GSK ends PPAR-γ diabetes development, studying new indications. FDC Reports Pink Sheet 2001 63 44 23
20. 434065 Design, synthesis, and evaluation of substituted phenylpropanoic acid derivaties as peroxisome proliferator-activated receptor (PPAR) activators: Novel human PPARα-selective activators. Miyachi H, Nomura M, Tanase T, Takahashi Y, Ide T, Tsunoda M, Murakami K, Awano K Bioorg Med Chem Lett 2002 12 1 77-80
21. 441434 Enantio-dependent binding and transactivation of optically active phenylpropanoic acid derivatives at human peroxisome proliferator-activated receptor α. Miyachi H, Nomura M, Tanase T, Suzuki M, Murakami K, Awano K Bioorg Med Chem Lett 2002 12 3 333-335
22. 442497 KRP-297, MCC-555. Nippon Rinsho 2001 59 11 2200-2206
23. 451260 Financial News & Investor Relations: Presentations - Deutsche Bank Health Care 2002 Conference. Merck & Co Inc Company Presentation 2002 May 15
24. 472321 Thiazolidinediones: Metabolic actions in vitro. Furnsinn C, Waldhausl W Diabetologia 2002 45 9 1211-1223 Discusses the mechanisms that underlie the antidiabetic effects of thiazolidinediones.
25. 472329 Thiazolidinediones: A pharmacological overview. Owens DR Clin Drug Invest 2002 22 8 485-505
26. 472330 The mechanisms of action of PPARs. Berger J, Moller DE Annu Rev Med 2002 53 409-435
27. 473730 Broadened portfolio of breakthrough medicines will drive Merck's growth. Merck & Co Inc Press Release 2002 December 10
28. 473816 Broadening the portfolio with new products in new categories: Merck's late stage pipeline. Merck & Co Inc Company Presentation 2002 December 10
29. 480936 Mechanism of free fatty acid-induced insulin resistance in humans. Roden M, Price TB, Perseghin G, Petersen KF, Rothman DL, Cline GW, Shulman GI J Clin Invest 1996 97 12 2859-2865
30. 480937 Regulation of lipoprotein metabolism by thiazolidinediones occurs through a distinct but complementary mechanism relative to fibrates. Lefebvre AM, Peinado-Onsurbe J, Leitersdort I, Briggs MR, Paterniti JR, Fruchart JC, Fievet C, Auwerx J, Staels B Arterioscler Thromb Vasc Biol 1997 17 9 1756-1764
31. 480939 Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors. Xu HE, Lambert MH, Montana VG, Plunket KD, Moore LB, Collins JL, Oplinger JA, Kliewer SA, Gampe RT Jr, McKee DD, Moore JT, Willson TM Proc Natl Acad Sci USA 2001 98 24 13919-13924 Discusses ligand binding selectivity between the PPAR isoforms based on crystal structure.
32. 480941 Differential activity of rosiglitazone enantiomers at PPAR γ. Parks DJ, Tomkinson NC, Villeneuve MS, Blanchard SG, Willson TM Bioorg Med Chem Lett 1998 8 24 3657-3658
33. 480942 Anti-atherogenic effects of fibrates in type 2 diabetes. Barter P Curr Controlled Trials Cardiovasc Med (Online) 2001 2 5 218-220