Liraglutide: The therapeutic promise from animal models

International Journal of Clinical Practice

Volumn 64, Issue SUPPL. 167, 2010, Pages 4-11

  Knudsen, L B ^a  

^a NOVO NORDISK A S   (Denmark)

Author keywords

[No Author keywords available]

Indexed keywords

EXENDIN 4; GLUCAGON LIKE PEPTIDE 1 RECEPTOR; LIRAGLUTIDE; PIOGLITAZONE; SAXAGLIPTIN; SERUM ALBUMIN; SITAGLIPTIN; VILDAGLIPTIN;

AMINO ACID SEQUENCE; AREA UNDER THE CURVE; BODY WEIGHT; CLINICAL RESEARCH; DIABETES MELLITUS; DOSE RESPONSE; DRUG BINDING; DRUG HALF LIFE; DRUG MECHANISM; DRUG POTENTIATION; EXPERIMENTAL ANIMAL; EXPERIMENTAL MOUSE; EXPERIMENTAL RAT; GLUCAGON RELEASE; GLYCEMIC CONTROL; HEART FUNCTION; HEART PROTECTION; HUMAN; HYPOGLYCEMIA; INSULIN BLOOD LEVEL; MINIPIG; NONHUMAN; PANCREAS ISLET BETA CELL; PRIORITY JOURNAL; REVIEW; STOMACH EMPTYING; WEIGHT REDUCTION;

ANIMALS; BODY WEIGHT; DIABETES MELLITUS, TYPE 2; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; GLUCAGON; GLUCAGON-LIKE PEPTIDE 1; HEMOGLOBIN A, GLYCOSYLATED; HUMANS; HYPOGLYCEMIC AGENTS; INSULIN; INSULIN-SECRETING CELLS; MICE; MICE, OBESE; PEPTIDES; RATS; RATS, ZUCKER; RECEPTORS, GLUCAGON; SWINE; SWINE, MINIATURE; VENOMS;

EID: 77956893157     PISSN: 13685031     EISSN: 17421241     Source Type: Journal    
DOI: 10.1111/j.1742-1241.2010.02499.x     Document Type: Review

References (33)

1. Knudsen LB, Nielsen PF, Huusfeldt PO et al. Potent derivatives of glucagon-like peptide-1 with pharmacokinetic properties suitable for once daily administration. J Med Chem 2000 43 : 1664 9.
2. Vilsbøll T, Agersø H, Krarup T, Holst JJ. Similar elimination rates of glucagon-like peptide-1 in obese type 2 diabetic patients and healthy subjects. J Clin Endocrinol Metab 2003 88 : 220 4.
3. Agersø H, Jensen LB, Elbrønd B, Rolan P, Zdravkovic M. The pharmacokinetics, pharmacodynamics, safety and tolerability of NN2211, a new long-acting GLP-1 derivative, in healthy men. Diabetologia 2002 45 : 195 202.
4. Steensgaard DB, Thomsen JK, Olsen HB, Knudsen LB. The molecular basis for the delayed absorption of the once-daily human GLP-1 analogue, liraglutide. Diabetes 2008 57 (Suppl 1 A164.
5. Nauck MA, Heimesaat MM, Behle K et al. Effects of glucagon-like peptide 1 on counterregulatory hormone responses, cognitive functions, and insulin secretion during hyperinsulinemic, stepped hypoglycemic clamp experiments in healthy volunteers. J Clin Endocrinol Metab 2002 87 : 1239 46.
6. Nauck MA, Niederereichholz U, Ettler R et al. Glucagon-like peptide-1 inhibition of gastric-emptying outweighs its insulinotropic effects in healthy humans. Am J Physiol 1997 273 : E981 8.
7. Nielsen LL, Young AA, Parkes DG. Pharmacology of exenatide (synthetic exendin-4): a potential therapeutic for improved glycemic control of type 2 diabetes. Regul Pept 2004 117 : 77 88.
8. Mu J, Woods J, Zhou YP et al. Chronic inhibition of dipeptidyl peptidase-4 with a sitagliptin analog preserves pancreatic beta-cell mass and function in a rodent model of type 2 diabetes. Diabetes 2006 55 : 1695 704.
9. Winzell MS, Ahrén B. The high-fat diet-fed mouse. A model for studying mechanisms and treatment of impaired glucose tolerance and type 2 diabetes. Diabetes 2004 53 (Suppl 3 S215 9.
10. Rolin B, Larsen MO, Gotfredsen CF et al. The long-acting GLP-1 derivative NN2211 ameliorates glycemia and increases beta-cell mass in diabetic mice. Am J Physiol Endocrinol Metab 2002 283 : E745 52.
11. Sturis J, Gotfredsen CF, Rømer J et al. GLP-1 derivative liraglutide in rats with beta-cell deficiencies: influence of metabolic state on beta-cell mass dynamics. Br J Pharmacol 2003 140 : 123 32.
12. Larsen PJ, Wulff EM, Gotfredsen CF et al. Combination of the insulin sensitizer, pioglitazone, and the long-acting GLP-1 human analog, liraglutide, exerts potent synergistic glucose-lowering efficacy in severely diabetic ZDF rats. Diabetes Obes Metab 2008 10 : 301 11.
13. Brand CL, Galsgaard ED, Tornehave D et al. Synergistic effect of the human GLP-1 analogue liraglutide and a dual PPAR agonist on glycaemic control in Zucker diabetic fatty rats. Diabetes Obes Metab 2009 11 : 795 803.
14. Ribel U, Larsen MO, Rolin B et al. NN2211: a long-acting glucagon-like peptide-1 derivative with anti-diabetic effects in glucose-intolerant pigs. Eur J Pharmacol 2002 451 : 217 25.
15. Anderson JW, Konz EC. Obesity and disease management: effects of weight loss on comorbid conditions. Obes Res 2001 9 (Suppl 4 326 34S.
16. Flint A, Raben A, Astrup A, Holst JJ. Glucagon-like peptide 1 promotes satiety and suppresses energy intake in humans. J Clin Invest 1998 101 : 515 20.
17. Zander M, Madsbad S, Madsen JL, Holst JJ. 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 30.
18. Raun K, von Voss P, Gotfredsen CF, Golozoubova V, Rolin B, Knudsen LB. Liraglutide, a long-acting glucagon-like peptide-1 analog, reduces body weight and food intake in obese candy-fed rats, whereas a dipeptidyl peptidase-IV inhibitor, vildagliptin, does not. Diabetes 2007 56 : 8 15.
19. Larsen PJ, Fledelius C, Knudsen LB, Tang-Christensen M. Systemic administration of the long-acting GLP-1 derivative NN2211 induces lasting and reversible weight loss in both normal and obese rats. Diabetes 2001 50 : 2530 9.
20. Bock T, Pakkenberg B, Buschard K. The endocrine pancreas in non-diabetic rats after short-term and long-term treatment with the long-acting GLP-1 derivative NN2211. APMIS 2003 111 : 1117 24.
21. Lykkegaard K, Larsen PJ, Vrang N, Bock C, Bock T, Knudsen LB. The once-daily human GLP-1 analog, liraglutide, reduces olanzapine-induced weight gain and glucose intolerance. Schizophr Res 2008 103 : 94 103.
22. Raun K, von Voss P, Knudsen LB. Liraglutide, a once-daily human glucagon-like peptide-1 analog, minimizes food intake in severely obese minipigs. Obesity (Silver Spring) 2007 15 : 1710 6.
23. Baggio LL, Drucker DJ. Biology of incretins: GLP-1 and GIP. Gastroenterology 2007 132 : 2131 57.
24. Merani S, Truong W, Emamaullee JA, Toso C, Knudsen LB, Shapiro AMJ. Liraglutide, a long-acting human glucagon-like peptide 1 analog, improves glucose homeostasis in marginal mass islet transplantation in mice. Endocrinology 2008 149 : 4322 8.
25. Friedrichsen BN, Neubauer N, Lee YC et al. Stimulation of pancreatic -cell replication by incretins involves transcriptional induction of cyclin D1 via multiple signalling pathways. J Endocrinol 2006 188 : 481 92.
26. Bregenholt S, Møldrup A, Blume N et al. The long-acting glucagon-like peptide-1 analogue, liraglutide, inhibits beta-cell apoptosis in vitro. Biochem Biophys Res Commun 2005 330 : 577 84.
27. Emamaullee JA, Merani S, Toso C et al. Porcine marginal mass islet autografts resist metabolic failure over time and are enhanced by early treatment with liraglutide. Endocrinology 2009 150 : 2145 52.
28. Mafong DD, Henry RR. The role of incretins in cardiovascular control. Curr Hypertens Rep 2009 11 : 18 22.
29. Sonne DP, Engstrøm T, Treiman M. Protective effects of GLP-1 analogues exendin-4 and GLP-1(9-36) amide against ischemia-reperfusion injury in rat heart. Regul Pept 2008 146 : 243 9.
30. Laugero KD, Stonehouse AH, Guss S, Landry J, Vu C, Parkes DG. Exenatide improves hypertension in a rat model of the metabolic syndrome. Metab Syndr Relat Disord 2009 7 : 327 34.
31. Yu M, Moreno C, Hoagland KM et al. Antihypertensive effect of glucagon-like peptide 1 in Dahl salt-sensitive rats. J Hypertens 2003 21 : 1125 35.
32. Ban K, Noyan-Ashraf MH, Hoefer J, Bolz SS, Drucker DJ, Husain M. Cardioprotective and vasodilatory actions of glucagon-like peptide 1 receptor are mediated through both glucagon-like peptide 1 receptor-dependent and -independent pathways. Circulation 2008 117 : 2340 50.
33. Noyan-Ashraf MH, Momen MA, Ban K et al. GLP-1R agonist liraglutide activates cytoprotective pathways and improves outcomes after experimental myocardial infarction in mice. Diabetes 2009 58 : 975 83.