Teneligliptin, characterized by a "J-shaped" structure formed by five consecutive rings, is a novel dipeptidyl peptidase 4 (DPP IV) inhibitor for the treatment of type 2 diabetes. Teneligliptin is eliminated via excretion with a half-life of 24.2 hours in human plasma from the kidney and metabolism involving certain enzymes. Hence, dose adjustment is not required in patients with renal impairment. A pharmacokinetic/pharmacodynamic study revealed that teneligliptin inhibits DPP IV activity over 24 hours, with elevation of activated glucagon-like peptide 1 (GLP-1) levels and the resulting suppression of postprandial hyperglycemia at all three daily meals. Monotherapy for 12 weeks significantly decreased hemoglobin A1c (HbA1c), fasting blood glucose, and 2-hour postprandial blood glucose levels in patients with type 2 diabetes. The therapeutic efficacy of teneligliptin over 52 weeks was confirmed not only as monotherapy but also as add-on therapy in patients with inadequately controlled blood glucose levels with sulfonylureas or thiazolidinediones. The incidence of adverse drug reactions was approximately 10% in all clinical studies of patients with type 2 diabetes conducted in Japan. The incidence of hypoglycemia was comparable in patients receiving teneligliptin or placebo, and no serious hypoglycemia was observed. Thus, teneligliptin is a novel antihyperglycemic agent with a preferable profile in terms of long-term efficacy and safety in patients with type 2 diabetes.
Keywords: Dipeptidyl peptidase 4; Hypoglycemia; Sulfonylureas; Teneligliptin; Thiazolidinediones; Type 2 diabetes.
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