Prospects of the first human glucagon-like peptide 1 analog liraglutid use in the treatment of patients with type 2 diabetes mellitus


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Abstract

Liraglutid is the first representative of human glucagon-like peptide-1 (GLP-1) analogs. The article presents data for the mechanisms of liraglutid action and review of studies on the efficacy and safety of its use in patients with type 2 diabetes mellitus (type 2 diabetes). Based on the research results, liraglutid administration in doses of 1.2/1.8 mg once daily resulted in significant and sustained glycemic control improvement, and also was accompanied by a number of additional effects, such as a persistent decrease in body weight, clinically significant decrease of systolic blood pressure level and improvement of of beta-cells function. Thus, new class of human GLP-1 analogs provides a unique opportunity in the treatment of type 2 diabetes mellitus, providing pathogenetic influence on progressive reduction of beta-cell function, and factors of cardiovascular risk.

References

  1. Moore B. On the treatment of diabetes mellitus by acid extract of duodenal mucous membrane. Biochem J 1906;1:28-38.
  2. Drucker DJ. Enhancing incretin action for the treatment of type 2 diabetes. Diabetes Care 2003;26:2929-40.
  3. Nauck MA, Homberger E, Siegel EG, et al. Incretin effects of increasing glucose loads in man calculated from venous insulin and C-peptide responses. J Clin Endocrinol Metab 1986;63:492-98.
  4. Nauck MA, Kleine N, Orskov C, et al. Normalization of fasting hyperglycaemia by exogenous glucagon-like peptide 1 (7-36 amide) in type 2 (non-insulin-dependent) diabetic patients. Diabetologia 1993;36:741-44.
  5. Vilsboll T, Agerso H, Krarup T, et al. Similar elimination rates of glucagon-like peptide-1 in obese type 2 diabetic patients and healthy subjects. J Clin Endocrinol Metab 2003;88:220-24.
  6. Vilsboll T. Liraglutide: a once-daily GLP-1 analogue for the treatment of type 2 diabetes mellitus.Expert Opin Investig Drugs 2007;16:231-37.
  7. Drucker D, Nauck M. The incretin system: glucagonlike peptide-1 receptor agonists and dipeptidyl peptidase- 4 inhibitors in type 2 diabetes. Lancet 2006;368:1696-701.
  8. 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 2002;25:1398-404.
  9. Agerso H, Jensen LB, Elbrond B, et al. The pharmacokinetics, pharmacodynamics, safety and tolerability of NN2211, a new long-acting GLP-1 derivative, in healthy men. Diabetologia 2002;45:195-202.
  10. Knop FK, Vilsboll T, Hojberg PV, et al. Reduced incretin effect in type 2 diabetes: cause or consequence of the diabetic state? Diabetes 2007;56:1951-59.
  11. Zander M, Madsbad S, Madsen JL, et al. Effect of 6-week course of glucagon-like peptide 1 on glycaemic control, insulin sensitivity, and beta-cell function in type 2 diabetes: a parallel-group study. Lancet 2002;359:824-80.
  12. Zdravkovic M, Hale P, Le Thi TD, et al. Overview of the design of the phase 3 studies for the longacting human GLP-1 analogue liraglutide: Liraglutide Effect and Action in Diabetes (LEAD). Diabetes 2007;56(Suppl. 1):abstr. 2251-PO.
  13. Holst JJ, Orskov C, Nielsen OV, et al. Truncated glucagon-like peptide I, an insulin-releasing hormone from the distal gut. FEBS Lett 1987;211:169-74.
  14. Orskov C, Holst JJ, Nielsen OV. Effect of truncated glucagon-like peptide-1 [proglucagon-(78-107) amide] on endocrine secretion from pig pancreas, antrum, and nonantral stomach. Endocrinology 1988;123:2009-13.
  15. Doyle ME, Egan JM. Mechanisms of action of glucagon-like peptide 1 in the pancreas. Pharmacol Ther 2007;113:546-93.
  16. Drucker DJ. The biology of the incretins. Cell Metab 2006;3:153-65.
  17. Holz GG IV, Kuhtreiber WM, Habener JF. Pancreatic beta-cells are rendered glucose-competent by the insulinotropic hormone glucagon-like peptide-1 (7-37). Nature 1993;361:362-65.
  18. Madsbad S, Schmitz O, Ranstam J, et al. 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 2004;27:1335-42.
  19. Feinglos MN, Saad MF, Pi-Sunyer FX, et al. Effects of liraglutide (NN2211), a long-acting GLP-1 analogue, on glycaemic control and bodyweight in subjects with type 2 diabetes. Diabet Med 2005;22:1016-23.
  20. Harder H, Nielsen L, Tu DT, et al. 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;27:1915-21.
  21. Vilsboll T, Zdravkovic M, Le-Thi T, et al. Liraglutide, a long-acting human GLP-1 analog, given as monotherapy significantly improves glycemic control and lowers body weight without risk of hypoglycemia in patients with type 2 diabetes mellitus. Diabetes Care 2007;30:1608-10.
  22. 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 a- and b-cell function and reduces endogenous glucose release in patients with type 2 diabetes. Diabetes 2004;53:1187-94.
  23. Mari A, Degn K, Brock B, et al. Characterisation of beta-cell function improvement by liraglutide: modelling analysis of 24-h tests. Diabetes 2006;55(Suppl. 1):A124, abstr. 522-P.
  24. Nauck MA, Homspesch M, Filipczak R, et al. 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 2006;114:417-23.
  25. Seino Y, Kaku K, Nishijima K, et al. Once daily dosing of the long acting GLP-1 analog liraglutide significantly improves glycaemic control by reducing both fasting and post-prandial glucose levels in Japanese subjects with type 2 diabetes. Diabetes 2007;56(Suppl. 1):abstr. 0520-P.
  26. Blonde L, et al. Liraglutide: superior glycemic control versus exenatide when added to metformin and-or SU in type 2 diabetes. Can J Diab 2008;32(Suppl.):abstr. 107.
  27. Garber A, et al. Lancet 2008:doi: 10.1016/S0140-6736(08)61246-5.
  28. Marre M, et al. Diabetes 2008;57(Suppl. 1):13-OR.
  29. Nauck M, et al. Diabetes Care 2008;in press.
  30. Russell-Jones D, et al. Diabetes 2008a;57(Suppl. 1):A159, abstr. P536.
  31. Zinman B, et al. Diabetologia 2008;51(Suppl.1):359, abstr. 898.
  32. Vilsboll T, Brock B, Perrild H, et al. Liraglutide, a oncedaily human GLP-1 analogue improves beta-cell function and arginine stimulated insulin secretion at hyperglycaemia in patients with type 2 diabetes mellitus. Diabet Med 2008;25:152-56.
  33. Holst JJ. The physiology of glucagon-like peptide 1. Physiol Rev 2007;87:1409-39.
  34. Mentlein R, Gallwitz B, Schmidt WE, et al. Dipeptidylpeptidase 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;214:829-35.
  35. Fehmann HC, Hering BJ, Wolf MJ, et al. Effects of glucagon-like peptide-I (GLP-I) on hormone secretion from isolated human pancreatic islets. Pancreas 1995;11:196-200.
  36. Gros R, You X, Baggio CC, et al. Cardiac function in mice lacking the glucagon-like peptide-1 receptor. Endocrinology 2003;144:2242-52.
  37. Nikolaidis LA, Elahi D, Hentosz T, et al. Recombinant glucagon-like peptide-1 increases myocardial glucose uptake and improves left ventricular performance in conscious dogs with pacing-induced dilated cardiomyopathy. Circulation 2004;110:955-61.
  38. Bose AK, Mocanu MM, Carr RD, et al. Glucagon-like peptide 1 can directly protect the heart against ischemia/reperfusion injury. Diabetes 2005;54:146-51.
  39. Vilsboll T, Zdravkovic M, Le-Thi T, et al. Liraglutide treatment, blood pressure and biomarkers of cardiovascular risk in patients with type 2 diabetes: 14 weeks monotherapy study. Diabetes 2006;55(Suppl. 1):abstr. 2007-PO.
  40. Colagiuri S, et al. Diabetologia 2008;51(Suppl. 1):S360, abstr. 899.
  41. Turton MD, O'Shea D, Gunn I, et al. A role for glucagonlike peptide-1 in the central regulation of feeding. Nature 1996;379:69-72.
  42. Tang-Christensen M, Larsen PH, Goke R, et al. Central administration of GLP-1-(7-36) amide inhibits food and water intake in rats. Am J Physiol 1996;271:R848-R856.
  43. Meeran K, O'Shea D, Edwards CM, et al. Repeated intracerebroventricular administration of glucagon-like peptide-1-(7-36) amide or exendin-(9-39) alters body weight in the rat. Endocrinology 1999;140:244-50.
  44. Bose A, Mocanu MM, Carr RD, et al. Glucagon-like peptide 1 can directly protect the heart against ischemia/reperfusion injury. Diabetes 2005;54:146-51.
  45. Mari A, Sallas WM, He YL. Vildagliptin, a dipeptidyl peptidase-IV inhibitor, improves model-assessed beta cell function in patients with type 2 diabetes. J Clin Endocrinol Metab 2005;90:4888-94.
  46. Jonker D, Toft AD, Kristensen P, et al. Pharmacokinetic modelling of the once-daily human GLP-1 analogue liraglutide in healthy volunteers and comparison to exenatide. Diabetes 2007;56(Suppl. 1):abstr. 0605-P.
  47. Jendle J, et al. Diabetes 2008;57(Suppl. 1):P106.
  48. Nauck MA, Niedereichholz U, Etter R, et al. Glucagon-like peptide 1 inhibition of gastric emptying outweighs its insulinotropic effects in healthy volunteers. Am J Physiol 1997;273:E981-E988.
  49. Irie S, Matsumura Y, Zdravkovic M, et al. Safety, tolerability, pharmacokinetics, and pharmacodynamics of once-daily GLP-1 analogue liraglutide in healthy Japanese subjects. Diabetes 2007;56(Suppl. 1):abstr. 2131-PO.
  50. LEAD1,2,3,4,5 meta-analysis of antibody formation; Novo Nordisk, Data on file.
  51. http://www.pharmateca.ru/cgi-bin/statyi.pl?sid=2211&mid=1085056570&magid=166

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