Exenatide: A novel incretin mimetic agent for treating type 2 diabetes mellitus

Cardiology in Review

Volumn 14, Issue 4, 2006, Pages 205-211

  Lam, Sum ^a,b   See, Sharon ^a,c  

^a ST JOHN'S UNIVERSITY   (United States)

^b WINTHROP UNIVERSITY HOSPITAL   (United States)

^c Beth Israel Residency in Urban Family Practice   (United States)

Author keywords

Exenatide; Glucagon like peptides; Incretin mimetic; Type 2 diabetes mellitus

Indexed keywords

DIGOXIN; EXENDIN 4; GLUCAGON LIKE PEPTIDE 1; INCRETIN; INSULIN GLARGINE; LISINOPRIL; METFORMIN; MEVINOLIN; PARACETAMOL; PLACEBO; SULFONYLUREA; ANTIDIABETIC AGENT; PEPTIDE; VENOM;

AMINO ACID SEQUENCE; CLINICAL TRIAL; DIARRHEA; DIZZINESS; DRUG ANTAGONISM; DRUG BLOOD LEVEL; DRUG COST; DRUG DOSE REGIMEN; DRUG EFFECT; DRUG HALF LIFE; DYSPEPSIA; FOOD INTAKE; GLYCEMIC CONTROL; HEADACHE; HORMONE RELEASE; HUMAN; HYPOGLYCEMIA; NAUSEA; NERVOUSNESS; NON INSULIN DEPENDENT DIABETES MELLITUS; REVIEW; SIDE EFFECT; VOMITING; WEIGHT REDUCTION; CHEMISTRY; DRUG INTERACTION; MOLECULAR GENETICS;

AMINO ACID SEQUENCE; CLINICAL TRIALS; DIABETES MELLITUS, TYPE 2; DRUG INTERACTIONS; GLUCAGON-LIKE PEPTIDE 1; HUMANS; HYPOGLYCEMIC AGENTS; MOLECULAR SEQUENCE DATA; PEPTIDES; VENOMS;

EID: 33746298115     PISSN: 10615377     EISSN: None     Source Type: Journal    
DOI: 10.1097/01.crd.0000223655.16253.e4     Document Type: Review

References (40)

1. American Diabetes Association. All About Diabetes. Available at: http://diabetes.org/diabetes-statistics/national-diabetes-fact-sheet.jsp. Accessed July 15, 2005.
2. World Health Organization. Diabetes Mellitus Fact Sheet 138. Available at: http://www.who.int/mediacentre/factsheets/fs138/en/index.html. Accessed July 15, 2005.
3. King H, Aubert RE, Herman WH. Global burden of diabetes, 1995-2025: prevalence, numerical estimates, and projections. Diabetes Care. 1998;21:1414-1431.
4. UK Prospective Diabetes Study Group. Intensive blood-glucose control with sulphonylureas or insulin compared with conventional treatment and risk of complications in patients with type 2 diabetes (UKPDS 33). Lancet. 1998;352:837-853.
5. Stratton IM, Adler AI, Neil AW, et al. Association of glycaemia with macrovascular and microvascular complications of type 2 diabetes (UKPDS 35): prospective observational study. BMJ. 2000;321:405-412.
6. American Diabetes Association. Summary of revision for the 2006 clinical practice recommendations. Diabetes Care. 2006;29(suppl 1):S3.
7. United Kingdom Prospective Diabetes Study Group. Overview of 6 years' therapy of type 2 diabetes: a progressive disease. Diabetes. 1995;44:1249-1258.
8. Inzucchi SE. Oral antihyperglycemic therapy for type 2 diabetes. JAMA. 2002;287:360-372.
9. Harris MI, Eastman RC, Cowie CC, et al. Racial and ethnic differences in glycemic control of adults with type 2 diabetes. Diabetes Care. 1999;22:403-408.
10. Product information: Byetta, exenatide injection. San Diego: Amylin Pharmaceuticals, Inc.
11. Eng J, Kleinman WA, Singh L, et al. Isolation and characterization of exendin-4, an exendin-3 analogue, from Heloderma suspectum venom. Further evidence for an exendin receptor on dispersed acini from guinea pig pancreas. J Biol Chem. 1992;267:7402-7405.
12. Young A, Blasé E, Petrella E, et al. Exendin-4 is a circulating meal-related peptide in the gila monster (Heloderma suspectum). Diabetes. 1999;48(suppl):Abstract A425.
13. Nielsen LL, Baron AD. Pharmacology of exenatide (synthetic exendin-4) for the treatment of type 2 diabetes. Curr Opin Investig Drugs. 2003;4:401-405.
14. Nielsen LL, Young AA, Parkes DG. Pharmacology of exenatide (synthetic-4): a potential therapeutic for improved glycemic control of type 2 diabetes. Regul Pept. 2004;117:77-88.
15. Kieffer TJ, McIntose CH, Pederson RA. Degradation of glucose-dependent insulinotropic polypeptide and truncated glucagon-like peptide I in vitro and in vivo by dipeptidyl peptidase IV. Endocrinology. 1995;136:3585-3596.
16. Deacon CF, Nauck MA, Toft-Nielsen M, et al. Both subcutaneously and intravenously administered glucagon-like peptide-1 are rapidly degraded from the NH2-terminus in type II diabetic patients and in healthy subjects. Diabetes. 1995;44:1126-1131.
17. Goke R, Fehmann HC, Linn T, et al. Exendin-4 is a high potency agonist and truncated exendin-(9-39)-amide an antagonist at the glucagon-like peptide 1-(7-36)-amide receptor of insulin-secreting beta-cells. J Biol Chem. 1993;26:19650-19655.
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. Poon T, Nelson P, Shen L, et al. Exenatide improves glycemic control and reduces body weight in subjects with type 2 diabetes: a dose-ranging study. Diabetes Technol Ther. 2005;7:467-477.
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. Young AA, Gedulin BR, Bhavsar S, et al. Glucose-lowering ad insulin-sensitizing actions of exenatine-4: studies in obese diabetic (ob/ob, db/db) mice, diabetic fatty Zucker rats and diabetic rhesus monkeys (Macaca mulatoo). Diabetes. 1999;48:1026-1034.
22. Egan JM, Meneilly GS, Habener JF, et al. Glucagon-like peptide-1 augments insulin-mediated glucose uptake in the obese state. J Clin Endocrinol Metab. 2002;87:3768-3773.
23. Egan JM, Meneilly GS, Elahi D. Effects of 1-mo bolus subcutaneous administration of exendin-4 in type 2 diabetes. Am J Physiol Endocrinol Metab. 2003;284:1072-1079.
24. Naslund E, Gutniak M, Skogar S, et al. Glucagon-like peptide 1 increases the period of postprandial satiety and slows gastric emptying in obese men. Am J Clin Nutr. 1998;68:525-530.
25. Szayna M, Doyle ME, Betkey JA, et al. Exendin-4 decelerates food intake, weight gain, and fat deposition in Zucker rats. Endocrinology. 2000;141:1936-1941.
26. Xu G, Stoffers DA, Habener JF, et al. Exendin-4 stimulates both beta-cell replication and neogenesis, resulting in increased beta-cell mass and improved glucose tolerance in diabetic rats. Diabetes. 1999;48:2270-2276.
27. Tourrel C, Bailbe D, Meile MJ, et al. Glucagon-like peptide-1 and exendin-4 stimulate β-cell neogenesis in streptozotocin-treated newborn rats resulting in persistently improved glucose homeostasis at adult age. Diabetes. 2001;50:1562-1570.
28. Tourrel C, Bailbe D, Lacorne M, et al. Persistent improvement of type 2 diabetes in the Goto-Kakizaki rat model by expansion of the β-cell mass during the prediabetic period with glucagon-like peptide-1 or exendin-4. Diabetes. 2002;51:1443-1452.
29. Perfetti R, Merkel P. Glucagon-like peptide-1: a major regulator of pancreatic beta-cell function. Eur J Endocrinol. 2000;143:717-725.
30. Kolterman OG, Kim DD, Shen L, et al. Pharmacokinetics, pharmacodynamics, and safety of exenatide in patients with type 2 diabetes mellitus. Am J Health Syst Pharm. 2005;62:173-181.
31. Edwards CM, Stanley SA, Davis R, et al. Exendin-4 reduces fasting and postprandial glucose and decreases energy intake in healthy volunteers. Am J Physiol Endocriol Metab. 2001;281:E155-E161.
32. Fineman MS, Biscsak TA, Shen LZ, et al. Effect on glycemic control of exenatide (synthetic exendin-4) additive to existing metformin and/or sulfonylurea treatment in patients with type 2 diabetes. Diabetes Care. 2003;26:2370-2377.
33. Calara F, Taylor K, Han J, et al. A randomized, open-label, crossover study examining the effect of injection site on bioavailability of exenatide (synthetic exendin-4). Clin Ther. 2005;27:210-215.
34. DeFronzo RA, Ratner RE, Han J, et al. Effects of exenatide (exendin-4) on glycemic control and weight over 30 weeks in metformin-treated patients with type 2 diabetes. Diabetes Care. 2005;28:1092-1100.
35. Buse JB, Henry RR, Han J, et al. Effect of exenatide (exendin-4) on glycemic control over 30 weeks in sulfonylurea-treated patients with type 2 diabetes. Diabetes Care. 2004;27:2628-2635.
36. Kendall DM, Riddle MC, Rosenstock J, et al. Effects of exenatide (exendin-4) on glycemic control over 30 weeks in patients with type 2 diabetes treated with metformin and a sulfonylurea. Diabetes Care. 2005;28:1083-1091.
37. Heine RJ, Van Gaal LF, Johns D, et al. Exenatide versus insulin glargine in patients with suboptimally controlled type 2 diabetes. Ann Intern Med. 2005;143:559-569.
38. Berenson A. A ray of hope for diabetics. This drug helps shed pounds. New York Times. Thursday, March 2, 2006 (Business Day Section, C1).
39. Fineman MS, Shen LZ, Taylor K, et al. Effectiveness of progressive dose-escalation of exenatide (exenedin-4) in reducing dose-limiting side effects in subjects with type 2 diabetes. Diabetes Metab Res Rev. 2004;20:411-417.
40. CVS Pharmacy Web Site. Available at: http://www.cvs.com. Accessed July 21, 2005.