Therapeutic assessment of glucagon-like peptide-1 agonists compared with dipeptidyl peptidase IV inhibitors as potential antidiabetic drugs

Expert Opinion on Investigational Drugs

Volumn 14, Issue 1, 2005, Pages 57-64

  Mentlein, Rolf ^a  

^a UNIVERSITY OF KIEL   (Germany)

Author keywords

Dipeptidyl peptidase IV; Dipeptidyl peptidase IV inhibitors; Glucagon like peptide 1; Glucagon like peptide 1 analogues; Incretin hormones; PACAP; Type 2 diabetes

Indexed keywords

ALBUMIN; ANTIDIABETIC AGENT; CJC 1131; DIPEPTIDYL PEPTIDASE IV; DIPEPTIDYL PEPTIDASE IV INHIBITOR; EXENDIN 4; FATTY ACID; GASTROINTESTINAL HORMONE; GLUCAGON LIKE PEPTIDE 1 DERIVATIVE; INCRETIN; INSULIN; LIRAGLUTIDE; METFORMIN; UNCLASSIFIED DRUG; VILDAGLIPTIN;

AMINO TERMINAL SEQUENCE; CENTRAL NERVOUS SYSTEM DISEASE; CLINICAL TRIAL; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DEGRADATION; DRUG EFFICACY; DRUG ELIMINATION; DRUG FORMULATION; DRUG HALF LIFE; DRUG MECHANISM; DRUG POTENCY; DRUG POTENTIATION; DRUG PURIFICATION; DRUG SCREENING; DRUG STABILITY; EDEMA; FIRST PASS EFFECT; GLUCOSE TOLERANCE; HORMONAL REGULATION; HORMONE ACTION; HUMAN; HYPOGLYCEMIA; INSULIN LIKE ACTIVITY; INSULIN RELEASE; NAUSEA; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PANCREAS ISLET CELL; PATIENT COMPLIANCE; PREVALENCE; PROTEIN DEGRADATION; REVIEW; VOMITING;

ANIMALS; ANTIGENS, CD26; DIABETES MELLITUS, TYPE 2; GLUCAGON-LIKE PEPTIDE 1; HUMANS; HYPOGLYCEMIC AGENTS; PROTEASE INHIBITORS;

EID: 12744269699     PISSN: 13543784     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543784.14.1.57     Document Type: Review

References (65)

1. KIEFFER TJ, HABENER JF: The glucagon-like peptides. Endocr. Rev. (1999) 20:876-913.
2. HOLST JJ: Gut hormones as pharmaceuticals. Regul. Peptides (2000) 93:45-51.
3. DRUCKER DJ: Glucagon-like peptides: regulators of cell proliferation, differentiation, and apoptosis. Mol. Endocrinol. (2003) 17:161-171.
4. DRUCKER DJ: Enhancing incretin action for the treatment of Type 2 diabetes. Diabetes Care (2003) 26:2929-2940.
5. VAHL TP, D'ALESSIO DA. Gut peptides in the treatment of diabetes mellitus. Expert Opin. Investig. Drugs (2004) 13 177-188
6. VILSBØLL T, HOLST JJ: Incretins, insulin secretion and Type 2 diabetes mellitus. Diabetologia (2004) 47:357-366.
7. SHERWOOD NM, KRUECKL SL, MCRORY JE: The origin and function of the pituitary adenylate cyclase-activating polypeptide (PACAP)/glucagon superfamily. Endocr. Rev. (2000) 21:619-670.
8. FILIPSSON K, KVIST-REIMER M, AHRÉN B: The neuropeptide pituitary adenylate cyclase-activating polypeptide and islet function. Diabetes (2001) 50:1959-1969.
9. NAUCK MA, STOCKMANN F, EBERT R, CREUTZFELD W: Reduced incretin effect in Type 2 (non-insulin-dependent) diabetes. Diabetologica (1986) 29:46-52.
10. RACHMANN J, BARROW BA, LEVY JC, TUNER RC: Near normalization of diurnal glucose concentrations by continuous administration of glucagon-like peptide 1 (GLP-1) in subjects with NIDDM. Diabetelogica (1997) 40:205-211.
11. MENTLEIN R, GALLWITZ B, SCHMIDT WE: Dipeptidyl-peptidase IV hydrolyses gastric inhibitory polypeptide, glucagon-like peptide-1(7-36)amide, peptide histidine methionine and is responsible for their degradation in human serum. Eur. J. Biochem. (1993) 214 829-835.
12. HOLST JJ: Implementation of GLP-1 based therapy of Type 2 diabetes mellitus using DPP-IV inhibitors. Adv. Exp. Med. Biol. (2003) 524:263-279.
13. MEIER JJ, GALLWITZ B, NAUCK MA: Glucagon-like peptide 1 and gastric inhibitory polypeptide: potential applications in Type 2 diabetes mellitus. BioDrugs (2003) 17:93-102.
14. NAUCK MA, MEIER JJ, CREUTZFELDT W: Incretins and their analogues as new antidiabetic drugs. Drug News Perspect. (2003) 16:413-422.
15. SIEGEL EG, GALLWITZ B, SCHARF G et al.: Biological activity of GLP-1-analogues with N-terminal modifications. Regul. Pept. (1999) 79:93-102.
16. HOLZ GG, CHEPURNY OG: Glucagon-like peptide-1 synthetic analogs: new therapeutic agents for use in the treatment of diabetes mellitus. Curr. Med. Chem. (2003) 10:2471-2483.
17. RITZEL R, ORSKOV C, HOLST JJ, NAUCK MA. Pharmacokinetic, insulinotropic, and glucagonostatic properties of GLP-1 [7-36 amide] after subcutaneous injection in healthy volunteers. Dose-response-relationships. Diabetologia (1995) 38:720-725.
18. EGAN JM, CLOCQUET AR, ELAHI D: The insulinotropic effect of acute exendin-4 administered to humans: comparison of nondiabetic state to Type 2 diabetes. J. Clin. Endocrinol. Metab. (2002) 87 1282-1290.
19. ELBROND B, JAKOBSEN G, LARSEN S et al.: Pharmacokinetics, pharmacodynamics, safety, and tolerability of a single-dose of NN2211, a long-acting glucagon-like peptide 1 derivative, in healthy male subjects. Diabetes Care 25:1398-1404.
20. KOLTERMAN OG, BUSE JB, FINEMAN MS et al.: Synthetic exendin-4 (exenatide) significantly reduces postprandial and fasting plasma glucose in subjects with Type 2 diabetes. J. Clin. Endocrinol. Metab. (2003) 88:3082-3089.
21. FINEMAN MS, SHEN LZ, TAYLOR K, KIM DD, BARON AD: Effectiveness of progressive dose-escalation of exenatide (exendin-4) in reducing dose-limiting side effects in subjects with Type 2 diabetes. Diabetes. Metab. Res. Rev. (2004) 20:411-417.
22. BUSE JB, HENRY RR, HAN J, KIM DD, FINEMAN MS, BARON AD: Effects of exenatide (exendin-4) on glycemic control over 30 weeks in sulfonylurea-treated patients with Type 2 diabetes. Diabetes Care (2004) 27:2628-2635.
23. DEGN KB, JUHL CB, STURIS J et al.: One week's treatment with the long-acting glucagon-like peptide 1 derivative liraglutide (NN2211) markedly improves 24-h glycemia and α- and β-cell function and reduces endogenous glucose release in patients with Type 2 diabetes. Diabetes (2004) 53:1187-1194.
24. HARDER H, NIELSEN L, TU DT, ASTRUP A: The effect of liraglutide, a long-acting glucagon-like peptide 1 derivative, on glycemic control, body composition, and 24-h energy expenditure in patients with Type 2 diabetes. Diabetes Care (2004) 27 1915-1921.
25. JOY SV, RODGERS PT, SCATES AC: Incretin numetics as emerging treatments for Type 2 Diabetes. Ann. Pharmacother. (2005) (In Press).
26. GROUZMANN E, COMOY E, WALKER P et al.: Production and characterization offour anti-neuropeptide Y monoclonal antibodies. Hybridoma (1992) 11:409-424.
27. FINEMAN MS, BICSAK TA, SHEN LZ et al.: Effect on glycemic control of exenatide (synthetic exendin-4) additive to existing metformin and/or sulfonurea treatment in patients with Type 2 diabetes. Diabetes Care (2003) 26:2370-2377.
28. WEN S, CHATENOUD L, LAWRENCE B, FRANCO P, CASTAIGNE J, BACH J: Lack of immunogenicity of CJC-1131, a long-acting GLP-1 analog for the treatment of Type 2 diabetes. Diabetes (2004) 53(Suppl. 2):A151 (Abstract 634-P).
29. DRUCKER DJ: Therapeutic potential of dipeptidyl peptidase IV inhibitors for the treatment of Type 2 diabetes. Expert. Opin. Investig. Drugs (2003) 12:87-100.
30. AUGUSTYNS K, VAN DER VEKEN P, SENTEN K, HAEMERS A. Dipeptidyl peptidase IV inhibitors as new therapeutic agents for the treatment of Type 2 diabetes. Expert Opin. Therap. Patents. (2003) 13 499-510.
31. WIEDEMAN PE, TREVILLYAN JM: Dipeptidyl peptidase IV inhibitors for the treatment of impaired glucose tolerance and Type 2 diabetes. Curr. Opin. Investig. Drugs (2003) 4:412-420.
32. VILLHAUER EB, COPPOLA GM, HUGHES TE: DPP-IV inhibition and therapeutic potential. Annual Reports Medicinal Chemistry (2001) 36:191-200.
33. RASMUSSEN HB, BRANNER S, WIBERG FC, WAGTMANN N: Crystal structure of human dipeptidyl peptidase IV/CD26 in complex with a substrate analog. Nat. Struct. Biol. (2003) 10:19-25
34. ENGEL M, HOFFMANN T, WAGNER L et al.: The crystal structure of dipeptidyl peptidase IV (CD26) reveals its functional regulation and enzymatic mechanism. Proc. Natl. Acad. Sci. USA (2003) 100:5063-5068.
35. MENTLEIN R. Dipeptidyl-peptidase IV (CD26)-role in the inactivation of regulatory peptides. Regul. Peptides (1999) 85 9-24.
36. MENTLEIN R: Cell surface peptidases. Int. Rev. Cytology (2004) 235:165-213.
37. AHRÉN B, SIMONSSON E, LARSSON H et al.: Inhibition of dipeptidyl peptidase IV improves metabolic control over a 4-week study period in Type 2 diabetes. Diabetes Care (2002) 25:869-875.
38. AHRÉN B, LANDIN-OLSSON M, JANSSON PA, SVENSSON M, HOLMES D, SCHWEIZER A. Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels, and reduces glucagon levels in Type 2 diabetes. Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels, and reduces glucagon levels in Type 2 diabetes. J. Clin. Endocrinol. Metab. (2004) 89:2078-2084.
39. AHRÉN B, GOMIS R, MILLS D, SCHWEIZER, A: The DPP-4 inhibitor, LAF 237, improves glycemic control in patients with Type 2 diabetes (T2DM) inadequately treated with metformin. Diabetes (2004) 53(Suppl. 2):A83
40. CONARELLO SL, LI Z, RONAN J et al.: Mice lacking dipeptidyl peptidase IV are protected against obesity and insulin resistance. Proc. Natl. Acad. Sci. USA (2003) 100:6825-6830.
41. SHINGU K, HELFRITZ A, ZIELINSKA-SKOWRONEK M et al.: CD26 expression determines lung metastasis in mutant F344 rats: involvement of NK cell function and soluble CD26. Cancer Immunol. Immunother. (2003) 52:546-554.
42. POSPISILIK JA, STAFFORD SG, DEMUTH HU et al.: Long-term treatment with the dipeptidyl peptidase IV inhibitor P32/98 causes sustained improvements in glucose tolerance, insulin sensitivity, hyperinsulinemia, and α-cell glucose responsiveness in VDF (fa/fa) Zucker rats. Diabetes (2002) 51:943-950.
43. HANSEN L, DEACON CF, ORSKOV C, HOLST JJ: Glucagon-like peptide-1-(7-36)amide is transformed to glucagon-like peptide-1-(9-36)amide by dipeptidyl peptidase IV in the capillaries supplying the L cells of the porcine intestine. Endocrinology (1999) 140:5356-5363.
44. PREITNER F, IBBERSON M, FRANKLIN I et al.: Gluco-incretins control insulin secretion at multiple levels as revealed in mice lacking GLP-1 and GIP receptors. J. Clin. Invest. (2004) 113:635-45.
45. AHRÉN B: Sensory nerves contribute to insulin secretion by glucagon-like peptide-1 in mice. Am J. Physiol. Regul. Integr. Comp. Physiol. (2004) 286:R269-R272.
46. MARGUET D, BAGGIO L, KOBAYASHI T et al.: Enhanced insulin secretion and improved glucose tolerance in mice lacking CD26. Proc. Natl. Acad. Sci. USA (2000) 97:6874-6879.
47. FARILLA I, BULOTTA A, HIRSHBERG B et al.: Glucagon-like peptide 1 inhibits cell apoptosis and improves glucose responsiveness of freshly isolated human islets. Endocrinology (2003) 144 5149-5158.
48. URUSOVA IA, FARILLA L, HUI H, D'AMICO E, PERFETTI R: GLP-1 inhibition of pancreatic islet cell apoptosis. Trends Endocrinol Metab. (2004) 15:27-33.
49. NIELSEN LL, YOUNG AA, PARKES DG: Pharmacology of exenatide (synthetic exendin-4): a potential therapeutic for improved glycemic control of Type 2 diabetes. Regul. Peptides (2004) 117:77-88.
50. VON BONIN A, HUHN J, FLEISCHER B: Dipeptidyl-peptidase IV/CD26 on T cells: analysis of an alternative T-cell activation pathway. Immunol. Rev. (1998) 161:43-53.
51. GORRELL MD, GYSBERS V, McCAUGHAN GW: CD26: a multifunctional integral membrane and secreted protein of activated lymphocytes. Scand. J. Immunol. (2001) 54:249-264.
52. HEYMANN E, MENTLEIN R: Complementary action of dipeptidyl peptidase IV and aminopeptidase M in the digestion of beta-casein. J. Dairy Res. (1986) 53:229-236.
53. +) exchanger isoform NHE3 and dipeptidyl peptidase IV in the renal proximal tubule. J. Biol. Chem. (2001) 276:46671-46677.
54. LAMBEIR AM, PROOST P, DURINX C et al.: Kinetic investigation of chemokine truncation by CD26/dipeptidyl peptidase IV reveals a striking selectivity within the chemokine family. J. Biol. Chem. (2001) 276:29839-29845.
55. TANAKA S, MURAKAMI T, HORIKAWA H, SUGIURA M, KAWASHIMA K, SUGITA T. Suppression of arthritis by the inhibitors of dipeptidyl peptidase IV. Int. J. Immunopharmacol. (1997) 19:15-24.
56. + T cell clones. J. Neuroimmunol. (1998) 87:203-209.
57. ZHU L, TAMVAKOPOULOS C, XIE D et al.: The role of dipeptidyl peptidase IV in the cleavage of glucagon family peptides: in vivo metabolism of pituitary adenylate cyclase activating polypeptide-(1-38). J. Biol. Chem. (2003) 278:22418-22423.
58. HANSOTIA T, BAGGIO LL, DELMEIRE D 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 (2004) 53:1326-1335.
59. MENTLEIN R, DAHMS P, GRANDT D, KRÜGER R: Proteolytic processing of neuropeptide Y and peptide YY by dipeptidyl peptidase IV. Regul. Peptides (1993) 49:133-144.
60. GROUZMANN E, MONOD M, LANDIS B et al.: Loss of dipeptidylpeptidase IV activity in chronic rhinosinusitis contributes to the neurogenic inflammation induced by substance P in the nasal mucosa. FASEB J. (2002) 16:1132-1134.
61. DIMITRIJEVIC M, STANOJEVIC S, VUJIC V et al.: Effect of neuropeptide Y on inflammatory paw edema in the rat: involvement of peripheral NPY Y1 and Y5 receptors and interaction with dipeptidyl-peptidase IV (CD26). J. Neuroimmunol. (2002) 129 35-42.
62. ROSENBLUM JS, KOZARICH JW: Prolyl peptidases: a serine protease subfamily with high potential for drug discovery. Curr. Opionion Chem. Biol. (2003) 7:496-504.
63. ABBOTT CA, YU DM, WOOLLATT E, SUTHERLAND GR, McCAUGHAN GW, GORRELL MD: Cloning, expression and chromosomal localization of a novel human dipeptidyl peptidase (DPP) IV homolog, DPP8. Eur. J. Biochem. (2000) 267:6140-6150.
64. OLSEN C, WAGTMANN N: Identification and characterization of human DPP9, a novel homologue of dipeptidyl peptidase IV. Gene (2002) 299:185-193.
65. LANKAS G, LEITING B, ROY RS et al.: Inhibition of DPP8/9 results in toxicity in preclinical species: Potential importance of selective dipeptidyl peptidase IV inhibition for the treatment of Type 2 DM. Diabetes (2004) 53(Suppl. 2):A2