title: Teneligliptin for the treatment of type 2 diabetes.
abstract: 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.
authors.affiliation: Sales & Marketing Division, Mitsubishi Tanabe Pharma Corporation, Osaka, Japan. Gouda.Maki@mm.mt-pharma.co.jp.
authors.forename: M
authors.initials: M
authors.lastname: Goda
authors.forename: T
authors.initials: T
authors.lastname: Kadowaki
mesh_terms: D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy*; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000627:therapeutic use*; D004347:Drug Interactions; D004359:Drug Therapy, Combination; D006801:Humans; D007004:Hypoglycemic Agents / Q000627:therapeutic use*; D011720:Pyrazoles / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D053778:Thiazolidines / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*
chemical_list: C579035:3-(4-(4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl)pyrrolidin-2-ylcarbonyl)thiazolidine; D054873:Dipeptidyl-Peptidase IV Inhibitors; D007004:Hypoglycemic Agents; D011720:Pyrazoles; D053778:Thiazolidines
keywords: Dipeptidyl peptidase 4; Hypoglycemia; Sulfonylureas; Teneligliptin; Thiazolidinediones; Type 2 diabetes