ASP8497 is a novel selective and competitive dipeptidyl peptidase-IV inhibitor with antihyperglycemic activity

Biochemical Pharmacology

Volumn 76, Issue 1, 2008, Pages 98-107

  Matsuyama Yokono, Akiko ^a   Tahara, Atsuo ^a   Nakano, Ryosuke ^a   Someya, Yuka ^a   Nagase, Itsuro ^a   Hayakawa, Masahiko ^a   Shibasaki, Masayuki ^a  

^a ASTELLAS PHARMA INC   (Japan)

Author keywords

Diabetes; Dipeptidyl peptidase IV; Glucagon like peptide 1; Insulin

Indexed keywords

1 (1,3 DIHYDRO 2H ISOINDOL 2 YL) 3 METHYL 1 OXO 2 PENTANAMINE 2 BUTENEDIOATE; 4 FLUORO A [[[4 METHYL 1 (METHYLSULFONYL)PIPERIDIN 4 YL]AMINO]ACETYL]PYRROLIDINE 2 CARBONITRILE MONOFUMARATE; ASP 8497; BMS 477178; DIPEPTIDYL PEPTIDASE IV INHIBITOR; GLICLAZIDE; GLUCAGON LIKE PEPTIDE 1; INSULIN; NICOTINAMIDE; PEPTIDE HYDROLASE INHIBITOR; SAXAGLIPTIN; SITAGLIPTIN; STREPTOZOCIN; VILDAGLIPTIN;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; COMPETITIVE INHIBITION; CONTROLLED STUDY; DOG; DRUG ACTIVITY; DRUG STRUCTURE; ENZYME INHIBITION; GLUCOSE BLOOD LEVEL; HYPOGLYCEMIA; IC 50; INSULIN BLOOD LEVEL; INTESTINE TRANSIT TIME; MALE; MOUSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; ORAL GLUCOSE TOLERANCE TEST; PRIORITY JOURNAL; STOMACH EMPTYING;

ANIMALS; ANTIGENS, CD26; BLOOD GLUCOSE; DIABETES MELLITUS, EXPERIMENTAL; GLUCOSE TOLERANCE TEST; HYPOGLYCEMIC AGENTS; INSULIN; MICE; PIPERIDINES; PROTEASE INHIBITORS; PYRROLIDINES; STREPTOZOCIN;

EID: 45049086968     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bcp.2008.03.021     Document Type: Article

References (39)

1. Polonsky K.S., Given B.D., Hirsch L.J., Tillil H., Shapiro E.T., Beebe C., et al. Abnormal patterns of insulin secretion in non-insulin-dependent diabetes mellitus. N Engl J Med 318 (1998) 1231-1239
2. Stahl M., and Berger W. Higher incidence of severe hypoglycemia leading to hospital admission in Type 2 diabetic patients treated with long-acting versus short-acting sulphonylureas. Diabet Med 16 (1999) 586-590
3. Holst J.J. Enteroglucagon. Annu Rev Physiol 59 (1997) 257-271
4. MacDonald P.E., El-Kholy W., Riedel M.J., Salapatek A.M., Light P.E., and Wheeler M.B. The multiple actions of GLP-1 on the process of glucose-stimulated insulin secretion. Diabetes 51 Suppl. 3 (2002) S434-S442
5. Ahren B., Larsson H., and Holst J.J. Effects of glucagon-like peptide-1 on islet function and insulin sensitivity in noninsulin-dependent diabetes mellitus. J Clin Endocrinol Metab 82 (1997) 473-478
6. Nauck M.A., Wollschlager D., Werner J., Holst J.J., Orskov C., Creutzfeldt W., et al. Effects of subcutaneous glucagon-like peptide 1 (GLP-1 [7-36 amide]) in patients with NIDDM. Diabetologia 39 (1996) 1546-1553
7. Drucker D.J. Biological actions and therapeutic potential of the glucagon-like peptides. Gastroenterology 122 (2002) 531-544
8. Nauck M.A., Niedereichholz U., Ettler R., Holst J.J., Orskov C., Ritzel R., et al. Glucagon-like peptide 1 inhibition of gastric emptying outweighs its insulinotropic effects in healthy humans. Am J Physiol 273 (1997) E981-E988
9. Kieffer T.J., McIntosh C.H., and Pederson R.A. Degradation of glucose-dependent insulinotropic polypeptide and truncated glucagon-like peptide 1 in vitro and in vivo by dipeptidyl peptidase IV. Endocrinology 136 (1995) 3585-3596
10. 2-terminus in type II diabetic patients and in healthy subjects. Diabetes 44 (1995) 1126-1131
11. Pederson R.A., White H.A., Schlenzig D., Pauly R.P., McIntoch C.H., and Demuth H.U. Improved glucose tolerance in Zucker fatty rats by oral administration of the dipeptidyl peptidase IV inhibitor isoleucine thiazolidide. Diabetes 47 (1998) 1253-1258
12. Reimer M.K., Holst J.J., and Ahren B. Long-term inhibition of dipeptidyl peptidase IV improves glucose tolerance and preserves islet function in mice. Eur J Endocrinol 146 (2002) 717-727
13. Burkey B.F., Li X., Bolognese L., Balkan B., Mone M., Russell M., et al. Acute and chronic effects of the incretin enhancer vildagliptin in insulin-resistant rats. J Pharmacol Exp Ther 315 (2005) 688-695
14. Raz I., et al. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy in patients with type 2 diabetes mellitus. Diabetologia 49 (2006) 2564-2571
15. Rosenstock J., Baron M.A., Dejager S., Mills D., and Schweizer A. Comparison of vildagliptin and rosiglitazone monotherapy in patients with type 2 diabetes: a 24-week, double-blind, randomized trial. Diabetes Care 30 (2007) 217-223
16. Demuth H.U., McIntosh C.H., and Pederson R.A. Type 2 diabetes-therapy with dipeptidyl peptidase IV inhibitors. Biochim Biophys Acta 1751 (2005) 33-44
17. Abbott C.A., Yu D.M., Woollatt E., Sutherland G.R., McCaughan G.W., and Gorrell M.D. Cloning, expression and chromosomal localization of a novel human dipeptidyl peptidase (DPP) IV homolog, DPP8. Eur J Biochem 267 (2000) 6140-6150
18. Ajami K., Abbott C.A., McCaughan G.W., and Gorrell M.D. Dipeptidyl peptidase 9 has two forms, a broad tissue distribution, cytoplasmic localization and DPIV-like peptidase activity. Biochim Biophys Acta 1679 (2004) 18-28
19. Lankas G.R., Leiting B., Roy R.S., Eiermann G.J., Beconi M.G., Biftu T., et al. Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidase 8 and 9. Diabetes 54 (2005) 2988-2994
20. Wettergren A., Schjoldager B., Mortensen P.E., Myhre J., Christiansen J., and Holst J.J. Truncated GLP-1 (proglucagon 78-107-amide) inhibits gastric and pancreatic functions in man. Dig Dis Sci 38 (1993) 665-673
21. Delgado-Aros S., Kim D.Y., Burton D.D., Thomforde G.M., Stephens D., Brinkmann B.H., et al. Effect of GLP-1 on gastric volume, emptying, maximum volume ingested, and postprandial symptoms in humans. Am J Physiol 282 (2002) G424-G431
22. Balkan B., Kwasnik L., Miserendino R., Holst J.J., and Li X. Inhibition of dipeptidyl peptidase IV with NVP-DPP728 increases plasma GLP-1 (7-36 amide) concentrations and improves oral glucose tolerance in obese Zucker rats. Diabetologia 42 (1999) 1324-1331
23. Lee H.J., Chen Y.S., Chou C.Y., Chien C.H., Lin C.H., Chang G.G., et al. Investigation of the dimer interface and substrate specificity of prolyl dipeptidase DPP8. J Biol Chem 281 (2006) 38653-38662
24. Takasaki K., Iwase M., Nakajima T., Ueno K., Nomoto Y., Nakanishi S., et al. K579, a slow-binding inhibitor of dipeptidyl peptidase IV, is a long-acting hypoglycemia agent. Eur J Pharmacol 486 (2004) 335-342
25. Augeri D.J., Robl J.A., Betebenner D.A., Magnin D.R., Khanna A., Robertson J.G., et al. Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. J Med Chem 48 (2005) 5025-5037
26. Ahren B., Simonsson E., Larsson H., Landin-Olsson M., Torgeirsson H., Jansson P.A., et al. Inhibition of dipeptidyl peptidase IV improves metabolic control over a 4-week study period in type 2 diabetes. Diabetes Care 25 (2002) 869-875
27. Ristic S., Byiers S., Foley J., and Holmes D. Improved glycaemic control with dipeptidyl peptidase-4 inhibition in patients with type 2 diabetes: vildagliptin (LAF237) dose response. Diabetes Obes Metab 7 (2005) 692-698
28. Kim D., Wang L., Beconi M., Eiermann G.J., Fisher M.H., He H., et al. (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. J Med Chem 48 (2005) 141-151
29. Masiello P., Broca C., Gross R., Roye M., Manteghetti M., Hillaire-Buys D., et al. Experimental NIDDM: development of a new model in adult rats administered streptozotocin and nicotinamide. Diabetes 47 (1998) 224-229
30. Davis T.M., Daly F., Walsh J.P., Ilett K.F., Beilby J.P., Dusci L.J., et al. Pharmacokinetics and pharmacodynamics of gliclazide in Caucasians and Australian Aborigines with type 2 diabetes. Br J Clin Pharmacol 49 (2000) 223-230
31. Yip R.G., and Wolfe M.M. GIP biology and fat metabolism. Life Sci 66 (2000) 91-103
32. Hansotia T., Baggio L.L., Delmeire D., Hinke S.A., Yamada Y., Tsukiyama K., et al. Double incretin receptor knockout (DIRKO) mice reveal an essential role for the enteroinsular axis in transducing the glucoregulatory actions of DPP-IV inhibitors. Diabetes 53 (2004) 1326-1335
33. Drucker D.J. Therapeutic potential of dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes. Expert Opin Investig Drugs 12 (2003) 87-100
34. Marguet D., Baggio L., Kobayashi T., Bernard A.M., Pierres M., Nielsen P.F., et al. Enhanced insulin secretion and improved glucose tolerance in mice lacking CD26. Proc Natl Acad Sci USA 97 (2000) 6874-6879
35. Nagakura T., Yasuda N., Yamazaki K., Ikuta H., Yoshikawa S., Asano O., et al. Improved glucose tolerance via enhanced glucose-dependent insulin secretion in dipeptidyl peptidase IV-deficient Fischer rats. Biochem Biophys Res Commun 284 (2001) 501-506
36. Ahren B., Landin-Olsson M., Jansson P.A., Svensson M., Holmes D., and Schweizer A. Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels, and reduces glucagon levels in type 2 diabetes. J Clin Endocrinol Metab 89 (2004) 2078-2084
37. Iltz J.L., Baker D.E., Setter S.M., and Keith Campbell R. Exenatide: an incretin mimetic for the treatment of type 2 diabetes mellitus. Clin Ther 28 (2006) 652-665
38. Madsbad S., Schmitz O., Ranstam J., Jakobsen G., and Matthews D.R. Improved glycemic control with no weight increase in patients with type 2 diabetes after once-daily treatment with the long-acting glucagon-like peptide 1 analog liraglutide (NN2211): a 12-week, double-blind, randomized, controlled trial. Diabetes Care 27 (2004) 1335-1342
39. Nauck M.A., Hompesch M., Filipczak R., Le T.D., Zdravkovic M., and Gumprecht J. Five weeks of treatment with the GLP-1 analogue liraglutide improves glycaemic control and lowers body weight in subjects with type 2 diabetes. Exp Clin Endocrinol Diabetes 114 (2006) 417-423