Nateglinide.

Abstract

Nateglinide is a novel D-phenylalanine derivative that inhibits ATP-sensitive K+ channels in pancreatic beta-cells in the presence of glucose and thereby stimulates the prandial release of insulin. Nateglinide reduces fasting and mealtime blood glucose levels in animals, healthy volunteers, and patients with type 2 (non-insulin-dependent) diabetes mellitus, and produces prompt prandial insulin responses with return to baseline insulin levels between meals. In randomised, double-blind 24-week studies in patients with type 2 diabetes, oral nateglinide 120 mg 3 times daily before meals improved glycaemic control significantly relative to placebo. Nateglinide 120 mg plus metformin 500 mg, both 3 times daily, conferred greater glycaemic improvement than either drug given alone, and nateglinide 60 or 120 mg 3 times daily plus metformin 1 g twice daily was superior to metformin plus placebo. Nateglinide 120 mg 3 times daily significantly reduced hyperglycaemia relative to placebo in a 16-week double-blind study in patients with type 2 diabetes mellitus. Combination therapy with troglitazone 600 mg daily produced significantly better glycaemic control than either drug given as monotherapy. Mild hypoglycaemia was the most frequently reported adverse event (1.3% of patients) after treatment with nateglinide 120 mg 3 times daily in a 16-week clinical study. No clinically significant abnormalities in laboratory results, ECGs, vital signs or physical examination findings have been noted in patients taking the drug.

• Authors: C J Dunn, D Faulds
• Journal: Drugs (Drugs) Vol. 60 Issue 3 Pg. 607-615; discussion 616-7 (Sep 2000) ISSN: 0012-6667 [Print] New Zealand
• PMID: 11030470 (Publication Type: Journal Article, Review)

Chemical References

• Cyclohexanes
• Hypoglycemic Agents
• Insulin
• Nateglinide
• Phenylalanine

Topics

• Administration, Oral
• Clinical Trials as Topic
• Cyclohexanes (administration & dosage, pharmacokinetics, pharmacology)
• Diabetes Mellitus, Type 2 (drug therapy)
• Humans
• Hypercalcemia (drug therapy)
• Hypoglycemic Agents (administration & dosage, pharmacokinetics, pharmacology)
• Insulin (metabolism)
• Insulin Secretion
• Nateglinide
• Pancreas (drug effects, physiology)
• Phenylalanine (administration & dosage, analogs & derivatives, pharmacokinetics, pharmacology)