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Nateglinide

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Abstract

▴ Nateglinide is a novel D-phenylalanine derivative that inhibits ATP-sensitive K+ channels in pancreatic β-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 120mg 3 times daily before meals improved glycaemic control significantly relative to placebo.

▴ Nateglinide 120mg plus metformin 500mg, both 3 times daily, conferred greater glycaemic improvement than either drug given alone, and nateglinide 60 or 120mg 3 times daily plus metformin 1g twice daily was superior to metformin plus placebo.

▴ Nateglinide 120mg 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 600mg 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 120mg 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.

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Authors and Affiliations

  1. Adis International Limited, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, Auckland 10, New Zealand

    Christopher J. Dunn & Diana Faulds

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  1. Christopher J. Dunn
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  2. Diana Faulds
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Correspondence to Christopher J. Dunn.

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Dunn, C.J., Faulds, D. Nateglinide. Drugs 60, 607–615 (2000). https://doi.org/10.2165/00003495-200060030-00007

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  • DOI: https://doi.org/10.2165/00003495-200060030-00007

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