Nateglinide (Starlix®): Update on a new antidiabetic agent

International Journal of Clinical Practice

Volumn 57, Issue 6, 2003, Pages 535-541

  Phillips, Lawrence S ^a   Dunning, B E ^b  

^a EMORY UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b NOVARTIS PHARMA AG   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

2,4 THIAZOLIDINEDIONE DERIVATIVE; ACARBOSE; GLICLAZIDE; GLIPIZIDE; GLUCOSE; HEMOGLOBIN A1C; INSULIN; METFORMIN; NATEGLINIDE; REPAGLINIDE; SULFONYLUREA; TROGLITAZONE; ANTIDIABETIC AGENT; CYCLOHEXANE DERIVATIVE; DRUG DERIVATIVE; PHENYLALANINE;

CLINICAL TRIAL; DIABETES MELLITUS; DIET RESTRICTION; DOSE RESPONSE; DRUG MECHANISM; DRUG METABOLISM; DRUG POTENTIATION; DRUG SAFETY; DRUG SPECIFICITY; DRUG TARGETING; DRUG TOLERABILITY; GASTROINTESTINAL SYMPTOM; GLUCOSE BLOOD LEVEL; HUMAN; HYPERGLYCEMIA; HYPERINSULINEMIA; HYPOGLYCEMIA; INSULIN LIKE ACTIVITY; INSULIN RELEASE; KIDNEY FAILURE; LIVER DISEASE; NONHUMAN; POSTPRANDIAL STATE; PRIORITY JOURNAL; REVIEW; TREATMENT FAILURE; WEIGHT GAIN; NON INSULIN DEPENDENT DIABETES MELLITUS; PHYSIOLOGY; TREATMENT OUTCOME;

BLOOD GLUCOSE; CYCLOHEXANES; DIABETES MELLITUS, TYPE 2; HUMANS; HYPERGLYCEMIA; HYPOGLYCEMIC AGENTS; PHENYLALANINE; TREATMENT OUTCOME;

EID: 0041562494     PISSN: 13685031     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (63)

1. Zimmet P, Alberti KG, Shaw J. Global and societal implications of the diabetes epidemic. Nature 2001; 414: 782-787.
2. American Association of Clinical Endocrinologists. Medical guidelines for the management of diabetes mellitus: the AACE system of intensive diabetes self-management: 2002 update. Endocrine Pract 2002; 8: 40-82.
3. European Diabetes Policy Group. A desktop guide to type 2 diabetes mellitus. Diab Med 1999; 16: 716-730.
4. World Health Organization. Definition, diagnosis and classification of diabetes mellitus and its complications: report of a WHO consultation, part 1. Geneva: WHO, 1999.
5. Temelkova-Kurktschiev TS, Koehler C, Henkel E et al. Postchallenge plasma glucose and glycemic spikes are more strongly associated with atherosclerosis than fasting glucose or HbA1c level. Diabetes Care 2000; 23: 1830-1834.
6. vanHaeften TW, Pimenta W, Mitrakou A et al. Disturbances in β-cell function in impaired fasting glycemia. Diabetes 2002; 51: S265-S270.
7. Weyer C, Bogardus C, Mott DM, Pratley RE. The natural history of insulin secretory dysfunction and insulin resistance in the pathogenesis of type 2 diabetes mellitus. J Clin Invest 1999; 104: 787-794.
8. Calles-Escandon J, Robbins DC. Loss of early phase of insulin release in humans impairs glucose tolerance and blunts thermic effect of glucose. Diabetes 1987; 36: 1167-1172.
9. Bruce DG, Chisholmn DJ, Storlien LH, Kraegen EW. Physiological importance of deficiency in early prandial insulin secretion in non-insulin-dependent diabetes. Diabetes 1988; 37: 736-744.
10. 1c. Diabetes Care 2000; 23: 1236-1241.
11. Service FJ, O'Brien PC. The relation of glycaemia to the risk of development and progression of retinopathy in the Diabetic Control and Complications Trial. Diabetologia 2001; 44: 1215-1220.
12. The DECODE study group. Glucose tolerance and cardiovasclar mortality: comparison of fasting and 2-hour diagnostic criteria. Arch Intern Med 2001; 161: 397-404.
13. Fujitani S, Yada T. A novel D-phenylalanine-derivative hypoglycemic agent A-4166 increases cytosolic free Ca2+ in rat pancreatic β-cells by stimulating Ca2+ influx. Endocrinology 1994; 134: 1395-1400.
14. Hu S, Wang S, Fanelli B et al. Pancreatic β-cell KATP channel activity and membrane binding studies with nateglinide: a comparison with sulphonylureas and repaglinide. J Pharm Exp Ther 2000; 293: 444-452.
15. Kalbag JB, Walter YH, Nedelman JR, McLeod JF. Mealtime glucose regulation with nateglinide in healthy volunteers: comparison with repaglinide and placebo. Diabetes Care 2001; 24: 73-77.
16. Walter YH, Spratt DI, Garreffa S, McLeod JF. Mealtime glucose regulation by nateglinide in type-2 diabetes mellitus. Eur J Clin Pharmacol 2000; 56: 129-133.
17. Leclercq-Meyer V, Ladriere, L, Fuhlendorff J, Malaisse WJ. Stimulation of insulin and somatostatin release by two meglitinide analogs. Endocrine 1997; 7: 311-317.
18. Kikuchi M. Modulation of insulin secretion in non -insulin-dependent diabetes mellitus by two novel oral hypoglycaemic agents, NN623 and A4166. Diab Med 1996; 13: S151-S155.
19. Hu S, Wang S, Dunning BE. Glucose-dependent and glucose-sensitizing insulinotropic effects of nateglinide: comparison to sulphonylureas and repaglinide. Int J Exp Diabetes Res 2001; 2: 63-72.
20. Walter YH, Brookman L, Ma P et al. Reduced risk of delayed hypeglycemia with nateglinide compared to repaglinide. Abstract. Diabetes 2001; 49(521-P): A128.
21. Levy J, Malaisse WJ. The stimulus-secretion coupling of glucose-induced insulin release. XVII. Effects of sulfonylureas and diazoxide on insular biosynthetic activity. Biochem Pharmacol 1975; 24: 235-239.
22. Vinambres C, Garcia-Martinez JA, Villanueva-Penacarrillo ML et al. Preservation of nutrient-stimulated biosynthetic activity in pancreatic islets exposed to a meglitinide analogue. Med Sci Res 1995; 23: 779-780.
23. Laghmich A, Ladriere L, Malaisse-Lagae F, Malaisse WJ. Long-term effects of glibenclamide and nateglinide upon pancreatic islet function in normal and diabetic rats. Pharmacol Res 1999; 40: 475-482.
24. ATP channels. J Pharm Exp Ther 1999; 291: 1372-1379.
25. Hu S, Wang S, Dunning BE. Effectiveness of nateglinide on in vitro insulin secretion from rat pancreatic islets desensitized to sulphonylureas. Int J Exp Diabetes Res 2001; 2: 73-79
26. Sato Y, Nishikawa M, Shinkai H, Sukegawa E. Possibility of ideal blood glucose control by a new oral hypoglycemic agent, N-[trans-4-isopropylcyclohexyl)-carbonyl]-D-phenylalanine (A-4166), and its stimulatory effect on insulin secretion in animals. Diabetes Res Clin Pract 1991; 12: 53-59.
27. Ikenoue T, Akiyoshi M, Fujitani S et al. Hypoglycaemic and insulinotropic effects of a novel oral antidiabetic agent, (-)-N-(trans-4-isopropylcyclohexane-carbonyl)-D-phenylalanine (A-4166). Br J Pharmacol 1997; 120: 137-145.
28. Ikenoue T, Okazaki K, Fujitani S et al. Effect of a new hypoglycemic agent, A-4166 [(-)-N-(trans-4-isopropyl-cyclohexanecarbonyl)-D-phenylalanine], on postprandial blood glucose excursion: comparison with voglibose and glibenclamide. Biol Pharm Bull 1997; 20: 354-359.
29. Klimes I, Sebokova E, Gaspericova D et al. Search for extrapancreatic effects of new oral hypoglycemic agent A-4166: 1. Oral glucose tolerance tests in normal and hereditary insulin resistant rats. Endocrine Reg 1998; 32: 115-123.
30. de Souza CJ, Russo P, Lozito R, Dunning BE. Differential effects of short and long duration insulinotropic agents on meal related glucose excursions. Diabetes Obes Metab 2001; 3: 73-83.
31. de Souza CJ, Gagen K, Chen W, Dragonas N. Early insulin release effectively improves glucose tolerance: studies in two rodent models of type 2 diabetes mellitus. Diabetes Obes Metab 2001; 3: 85-95.
32. Dunning BE, Paladini S, Gutierrez C et al. Nateglinide improves prandial glucose excursions by restoring early insulin secretion in pre-diabetic monkeys. Diabetologia 1999; 42(7): A4. Abstract.
33. Dunning BE, Gutierrez C. Pharmacodynamics of nateglinide and repaglinide in Cynomolgus monkeys Diabetes 1999; 48(446): A104. Abstract.
34. Kahn SE, Montgomery B, Howell W et al. Importance of early phase insulin secretion to intravenous glucose tolerance in subjects with type 2 diabetes mellitus. J Clin Endocrinol Metab 2001; 86: 5824-5829.
35. Dunning BE, Paladini S. Mimicking cephalic insulin release the the rapid onset/short duration insulinotrophic agent, nateglinide, reduces prandial glucose excursions without increasing total insulin exposure in IGT monkeys. Diabetes 1999; 48(1233): A282. Abstract.
36. Uto Y, Teno S, Iwamoto Y et al. Improvement of glucose tolerance by nateglinide occurs through enhancement of early phase insulin secretion. Metabolism 2002; 51: 20-24.
37. Hollander PA, Schwartz SL, Gatlin MR et al. Importance of early insulin secretion: comparison of nateglinide and glyburide in previously diet-treated patients with type 2 diabetes. Diabetes Care 2001; 24: 983-988.
38. Uchino H, Niwa M, Shimizu T et al. Impairment of early insulin response after glucose load, rather than insulin resistance, is responsible for postprandial hyperglycemia seen in type 2 diabetes: assessment using nateglinide, a new insulin secretagogue. Endocr J 2000; 47: 639-641.
39. Karara AH, Dunning BE, McLeod JF. The effect of food on the oral bioavailability and the pharmacodynamic actions of the insulinotropic agent nateglinide in healthy subjects. J Clin Pharmacol 1999; 39: 172-179.
40. Weaver ML, Orwig BA, Rodriguez LC et al. Pharmacokinetics and metabolism of nateglinide in humans. Drug Metab Dispos 2001; 29: 415-421.
41. Choudhury S, Hirschberg Y, Filipek R et al. Single-dose pharmacokinetics of nateglinide in subjects with hepatic cirrhosis. J Clin Pharmacol 2000; 40: 634-640.
42. Luzio SD, Anderson DM, Owens DR. Effects of timing of administration and meal composition on the pharmacokinetic and pharmacodynamic characteristics of the short-acting oral hypoglycemic agent nateglinide in healthy subjects. J Clin Endocrinol Metab 2001; 86: 4874-4880.
43. Keilson L, Mather S, Walter YH et al. Synergistic effects of nateglinide and meal administration on insulin secretion in patients with type 2 diabetes mellitus. J Clin Endocrinol Metab 2000; 85: 1081-1086.
44. Ishii T, Yamakita T, Yamagami K et al. Nateglinide is safe and efficacious in lowering postprandial blood glucose in type 2 diabetic patients with various degree of renal function. Diabetes 2001; 50: A118. Abstract.
45. Starlix. Package insert. Novartis Pharmaceuticals, East Hanover, NJ, 2001.
46. Hanefeld M, Dickinson S, Bouter KP, Guitard C. Rapid and short-acting mealtime insulin secretion with nateglinide controls both prandial and mean glycemia. Diabetes Care 2000; 23: 202-207.
47. Holmes D, Raccah D, Escobar-Jimenez F, Standl E. Targeting postprandial hyperglycemia in patients with type 2 diabetes: nateglinide vs acarbose. Diabetologia 2001; 44: A215. Abstract.
48. Horton ES, Clinkinbeard C, Gatlin M et al. Nateglinide alone and in combination with metformin improves glycemic control by reducing meal-time glucose levels in type 2 diabetes. Diabetes Care 2000; 23: 1660-1665.
49. Rosenstock J, Gatlin M, Mallows S, Bush C. Nateglinide improves glycemic control alone and in combination with troglitazone in patients with type 2 diabetes. Diabetes 2000; 49(498-P): A123. Abstract.
50. Foley JE, Gatlin M, Dunn FL, Horton ES. Both nateglinide and metformin sustain HbA1c lowering over 52 weeks in drug-naive type 2 diabetes patients. Diabetologia 2001; 44: A215. Abstract.
51. Saloranta C, Holmes D, Ball M et al. Efficacy and safety of nateglinide in patients with mild hyperglycaemia. Diabetologia 2001; 44: A214. Abstract.
52. Saloranta C, Guitard C, Pecher E et al. Nateglinide improves early insulin secretion and controls postprandial glucose excursions in a prediabetic population. Diabetes Care 2002; 25: 2141-2146.
53. Marre M, Whatmough I, Pongowski M, Guitard C. Nateglinide added to metformin offers safe and effective treatment for type 2 diabetes. Diabetes Obes Metab 2000; 4: 177-186.
54. Rosenstock J, Shen SG, Gatlin MR, Foley JE. Combination therapy with nateglinide and a thiazolidinedione improves glycemic control in type 2 diabetes. Diabetes Care 2002; 25: 1529-1533.
55. Katoh S, Yamazaki H, Yokoyama J, Tajima N. Beneficial effect of nateglinide-gliclazide time-sharing therapy: a new basal-bolus therapy of oral hypoglycemic agents Diabetes 2001; 50: A119. Abstract.
56. Fujita T, Kosugi K, Ueda N, Hatano M. Oral nateglinide administration improves glycemic control of type 2 diabetic patients treated with intermediate-acting insulin Diabetes 2001; 50: A435. Abstract.
57. Landgraf R, Frank M, Bauer C, Dieken ML. Prandial glucose regulation with repaglinide: its clinical and lifestyle impact in a large cohort of patients with type 2 diabetes. Int J Obes 2000; 24: S38-S44.
58. Stahl M, Berger W. Higher incidence of severe hypoglycaemia leading to hospital admission in type 2 diabetic patients treated with long-acting versus shot-acting suffonylureas. Diabet Med 1999; 16: 586-590.
59. Kradjan WA, Kobayashi KA, Bauer LA et al. Glipizide pharmacokinetics: effects of age, diabetes, and multiple dosing. J Clin Pharmacol 1989; 29: 1121-1127.
60. Asplund K, Wiholm BE, Lithner F. Glibenclamide-associated hypeglycaemia: a report on 57 cases. Diabetologia 1983; 24: 412-417.
61. Testa MA, Hayes JF, Turner RR, Simonson DC. Improved quality of life is associated with improved glycemic control in type 2 diabetes: an international, multi-cultural, multi-center, placebo-controlled 'clinical trial Diabetes 2000; 49: A73. Abstract.
62. Barrett-Connor E, Ferrara A. Isolated postchallenge hyperglycemia and the risk of fatal cardiovascular disease in older women and men. Diabetes Care 1998; 21: 1236-1239.
63. NAVIGATOR trial steering committee. Nateglinide and valsartan in impaired glucose tolerance outcomes research: rationale and design of the NAVIGATOR trial Diabetes 2002; 51: A116. Abstract.