Glucoregulatory effects and prolonged duration of action of davalintide: A novel amylinomimetic peptide

Diabetes, Obesity and Metabolism

Volumn 13, Issue 12, 2011, Pages 1105-1113

  Mack, C M ^a   Smith, P A ^a   Athanacio, J R ^a   Xu, K ^a   Wilson, J K ^a   Reynolds, J M ^a   Jodka, C M ^a   Lu, M G W ^a   Parkes, D G ^a  

^a AMYLIN PHARMACEUTICALS INC   (United States)

Author keywords

Binding kinetics; Food intake; Gastric emptying; Glucagon secretion; Glucose; OGTT

Indexed keywords

AMYLIN; ARGININE; DAVALINTIDE; GLUCAGON; GLUCOSE;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG EFFECT; DRUG ELIMINATION; FOOD INTAKE; GLUCAGON BLOOD LEVEL; GLUCAGON RELEASE; GLUCOREGULATORY EFFECT; GLUCOSE BLOOD LEVEL; GLUCOSE TOLERANCE TEST; MALE; NONHUMAN; NUCLEUS ACCUMBENS; RAT; STOMACH EMPTYING;

EID: 80055032330     PISSN: 14628902     EISSN: 14631326     Source Type: Journal    
DOI: 10.1111/j.1463-1326.2011.01465.x     Document Type: Article

References (38)

1. Young AA, Gedulin BR, Rink TJ. Dose-responses for the slowing of gastric emptying in a rodent model by glucagon-like peptide (7-36)NH2, amylin, cholecystokinin, and other possible regulators of nutrient uptake. Metabolism 1996; 45: 1-3.
2. Gedulin BR, Young AA. Hypoglycemia overrides amylin-meditated regulation of gastric emptying in rats. Diabetes 1998; 47: 93-97.
3. Young, A. Inhibition of Gastric Emptying. Amylin: Physiology and Pharmacology (Advances in Pharmacology), vol. 52. Academic Press, 99-121.
4. Kong MF, King P, Macdonald IA et al. Infusion of pramlintide, a human amylin analogue, delays gastric emptying in men with IDDM. Diabetologia 1997; 40: 82-88.
5. Kong MF, Stubbs TA, King P et al. The effect of single dose of pramlintide on gastric emptying of two meals in men with IDDM. Diabetologia 1998; 41: 577-583.
6. Vella A, Lee JS, Camilleri M et al. Effects of pramlintide, an amylin analog, on gastric emptying in type 1 and 2 diabetes mellitus. Neurogastroenterol Motil 2002; 14: 123-131.
7. Samsom M, Szarka LA, Camilleri M, Vella A, Zinmeister AR, Rizza RA. Pramlintide, an amylin analog, selectively delays gastric emptying: potential role of vagal inhibition. Am J Physiol Gastrointest Liver Physiol 2000; 278: G946-951.
8. Gedulin BR, Rink TJ, Young AA. Dose-response for glucagonostatic effect of amylin in rats. Metabolism 1997; 46: 67-70.
9. Silvestre RA, Rodríguez-Gallardo J, Jodka C et al. Selective amylin inhibition of the glucagon response to arginine is extrinsic to the pancreas. Am J Physiol Endocrinol Metab 2001; 280: E443-449.
10. Gedulin B, Percy A, Jodka C, Young A. Endogenous amylin inhibits glucagon secretion as demonstrated by studies using neutralizing antibody and the antagonist AC187. Diabet Med 1997; 14: S18.
11. Nyholm B, Orskov L, Hove KY et al. The amylin analog pramlintide improves glycemic control and reduces postprandial glucagon concentrations in patients with type 1 diabetes. Metabolism 1999; 48: 935-941.
12. Fineman M, Weyer C, Maggs DG, Strobe S, Kolterman OG. The human amylin analog, pramlintide, reduces postprandial hyperglucagonemia in patients with type 2 diabetes. Horm Metab Res 2002; 34: 504-508.
13. Fineman M, Weyer C, Maggs DG, Strobe S, Kolterman OG. The human amylin analog, pramlintide, reduces postprandial hyperglucagonemia in patients with type 1 diabetes. Metabolism 2002; 51: 636-641.
14. Chelikani PK, Haver AC, Reidelberger RD. Relative potencies of anorexigenic substances in suppressing food intake in free feeding rats. Appetite 2006; 46: 344.
15. Lutz TA, Tshudy S, Rushing PA, Scharrer E. Amylin receptors mediate the anorectic effects of salmon calcitonin. Peptides 2000; 21: 233-238.
16. Mack CM, Wilson J, Athanacio J et al. Pharmacological actions of the peptide hormone amylin in the long-term regulation of food intake, food preference and body weight. Am J Physiol Regul Integr Comp Physiol 2007; 293: R1855-1863.
17. Morley JE, Suarez MD, Mattamal M, Flood JF. Amylin and food intake in mice: effects on motivation to eat and mechanism of action. Pharmacol Biochem Behav 1997; 56: 123-129.
18. Rushing PA, Seeley RJ, Air EL, Lutz TA, Woods SC. Acute 3rdventricular amylin infusion potently reduces food intake but does not produce aversive consequences. Peptides 2002; 23: 985-988.
19. Lutz TA, Senn M, Althaus J, Del Prete E, Ehrensperger F, Scharrer E. Lesion of the area postrema/nucleus of the solitary tract(AP/NTS) attenuates the anorectic effects of amylin and calcitonin gene-related peptide (CGRP) in rats. Peptides 1998; 19: 309-317.
20. Riediger T, Zuend D, Becskei C, Lutz TA. The anorectic hormoneamylin contributes to feeding-related changes of neuronal activity in key structures of the gut-brain axis. Am J Physiol Regul Integr Comp Physiol 2004; 286: R114-122.
21. Roth JD, Hughes H, Kendall E, Baron AD, Anderson CM. Antiobesity effects of the b-cell hormone amylin in diet-induced obese rats: effects on food intake, body weight, composition, energy expenditure, and gene expression. Endocrinology 2006; 147: 5855-5864.
22. Smith SR, Blundell JE, Burns C et al. Pramlintide treatment reduces 24-h caloric intake and meal sizes and improves control of eating in obese subjects: a 6-wk translational research study. Am J Physiol Endocrinol Metab 2007; 293: E620-627.
23. Chapman I, Parker B, Doran S et al. Effect of pramlintide on satiety and food intake in obese subjects and subjects with type 2 diabetes. Diabetologia 2005; 48: 838-848.
24. Aronne L, Fujioka K, Aroda V et al. Progressive reduction in body weight after treatment with the amylin analogue pramlintide in obese subjects: a phase 2, randomized, placebo-controlled, dose-escalation study. J Clin Endocrinol Metab 2007; 92: 2977-2983.
25. Smith SR, Aronne LJ, Burns CM, Kesty NC, Halseth AE, Weyer C. Sustained weight loss following 12-month pramlintide treatment as an adjunct to lifestyle intervention in obesity. Diabetes Care 2008; 31: 1816-1823.
26. Aronne LJ, Halseth AE, Burns CM, Miller S, Shen LZ. Enhanced weight loss following coadministration of pramlintide with sibutramine or phentermine in a multicenter trial. Obesity 2010; 18: 1739-1746.
27. Roth JD, Roland BL, Cole RL, Trevaskis JL, Weyer C, Koda JE et al. Leptin responsiveness restored by amylin agonism in diet induced obesity: evidence from nonclinical and clinical studies. Proc Natl Acad Sci USA 2008; 105: 7257-7262.
28. Ravussin E, Smith SR, Mitchell JA et al. Enhanced weight loss with pramlintide/metreleptin: an integrated neurohormonal approach to obesity pharmacotherapy. Obesity 2009; 17: 1736-1743.
29. Mack CM, Soares CJ, Wilson JK et al. Davalintide (AC2307), a novel amylin-mimetic peptide: enhanced pharmacological properties over native amylin to reduce food intake and body weight. Inter J Obes 2010; 34: 385-395.
30. Levin, BE, Dunn-Meynell, AA, Balkan B, Keesey RE. Selective breeding for diet-induced obesity and resistance I Sprague-Dawley rats. Am J Physiol 1997; 273: R725-730.
31. Hatanaka S, Kondoh M, Kawarabayashi K, Furuhama K. The measurement of gastric emptying in conscious rats by monitoring serial changes in serum acetaminophen level. J Pharmacol Toxicol Methods 1994; 31: 161-165.
32. Beaumont K, Kenney MA, Young AA, Rink TJ. High affinity amylin binding sites in rat brain. Mol Pharmacol 1993; 44: 493-497.
33. Young, A. Effects on Plasma Glucose and Lactate. Amylin: Physiology and Pharmacology (Advances in Pharmacology), vol. 52. Academic Press, 2005, 193-208.
34. Unger R, Aguilar-Parada E, Muller WA, Eisentraut AM. Studies of pancreatic alpha cell function in normal and diabetic subjects. J Clin Invest 1970; 49: 837-848.
35. Unger RH, Orci L. The role of glucagon in the endogenous hyperglycemia of diabetes mellitus. Ann Rev Med 1977; 28: 119-130.
36. Silvestre RA, Rodriguez-Gallardo J, Jodka C et al. Selective amylin inhibition of the glucagon response to arginine is extrinsic to the pancreas. Am J Physiol 2001; 280: E443-449.
37. Vine W, Smith P, LaChappell R, Blase E, Lumpkin R, Young A. Nephrectomy decreases amylin and pramlintide clearance in rats. Horm Metab Res 1998; 30: 514-517.
38. Muff R, Born W, Fischer JA. Calcitonin, calcitonin gene-related peptide, adrenomedullin and amylin: homologous peptides, separate receptors and overlapping biological actions. Eur J Endocrinol 1995; 133: 17-20.