The Indian Practitioner

Open Access Open Access  Restricted Access Subscription Access
Open Access Open Access Open Access  Restricted Access Restricted Access Subscription Access

Teneligliptin – The Newest DPP4 Inhibitor


Affiliations
1 Medical Services, Centaur Pharmaceuticals Pvt. Ltd., India
2 Jaslok Hospital, Mumbai, India
     

   Subscribe/Renew Journal


Teneligliptin is the newest DPP4 inhibitor approved by the regulatory authority for the treatment of Diabetes mellitus. Teneligliptin scores over other 'gliptins' in being more economical and with better efficacy to control blood glucose and HbA1C levels. Teneligliptin additionally offers other pharmacological advantages like longer half-life, lesser IC50 value, tight and extensive binding to the DPP4 enzyme. Teneligliptin has been studies extensively for its safety and efficacy in various clinical trials conducted internationally. This review article comprehensively documents the available clinical and pharmacological data for Teneligliptin in the treatment of Diabetes mellitus.

Keywords

Diabetes Mellitus, Teneligliptin, HbA1C, Fasting Blood Glucose, Post Prandial Blood Glucose.
Subscription Login to verify subscription
User
Notifications
Font Size


  • Joshi SR, Parikh RM. India - diabetes capital of the world: now heading towards hypertension. J Assoc Physicians India. 2007;55:323–4.

  • Kumar A, Goel MK, Jain RB, Khanna P, Chaudhary V. India towards diabetes control: Key issues. Australas Med J. 2013;6(10):524–31. [PMC free article] [PubMed] 3. Wild S, Roglic G, Green A, Sicree R, King H. Global prevalence of diabetes-estimates for the year 2000 and projections for 2030. Diabetes Care. 2004;27(3):1047–53. [PubMed]

  • Whiting Dr, Guariguata L, Weil C, Shawj. IDF Diabetes atlas: Global estimates of the prevalence of diabetes for 2011 and 2030. Diabetes Res ClinPract. 2011;94:311–21.

  • UK Prospective Diabetes Study (UKPDS) Group. Intensive blood-glucose control with sulphonylureas or insulin compared with conventional treatment and risk of complications in patients with type 2 diabetes (UKPDS 33). Lancet. 1998;352:837e853.

  • Lebovitz HE. Oral antidiabetic agents. In: Kahn CR, Weir GC, editors. Joslin’s diabetes mellitus. 13th ed. Philadelphia: Lea &Febiger; 1994. p. 508e529.

  • DeFronzo RA. Pharmacologic therapy for type 2 diabetes mellitus. Ann Intern Med. 1999;131:281e303.

  • Meier JJ, Nauck MA. Glucagon-like peptide 1(GLP1) in biology and pathology. Diabetes Metab Res Rev. 2005;21:91e117.

  • Edwards KL, Stapleton M, Weis J, Irons BK. An update in incretin-based therapy: A focus on glucagon-like peptide-1 receptor agonists. Diabetes TechnolTher 2012; 14: 951-967.

  • Stonehouse AH, Darsow T, Maggs DG. Incretin-based therapies. J Diabetes 2012; 4: 55-67.

  • Baetta R, Corsini A. Pharmacology of dipeptidyl peptidase-4 inhibitors: similarities and differences. Drugs. 2011;71:1441– 1467.

  • Yoshida T, Akahoshi F, Sakashita H, et al. Discovery and preclinical profile of teneligliptin(3-[(2S,4S)-4-[4-(3-methyl1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2ylcarbonyl]thiazolidine): a highly potent, selective, longlasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Bioorg Med Chem. 2012;20(19):5705–5719.

  • RyuichiMorishitaet. al., Teneligliptin: expectations for its pleiotropic action, Expert Opinion on Pharmacotherapy,16:3, 417-426.

  • Nakamaru Y, Hayashi Y, Ikegawa R, et al. Metabolism and disposition of the dipeptidyl peptidase IV inhibitor teneligliptin in humans. Xenobiotica. 2014;44(3):242–53.

  • InvestiFarma SA. Teneglucon (teneligliptin) via oral: Argentina prescribing information. 2015. http://investi.etradeconsult.com/teneglucon/art_234/es/. Accessed 10 Aug 2015.

  • Nakamaru Y, Hayashi Y, Sekine M, et al. Effect of ketoconazole on the pharmacokinetics of the dipeptidyl peptidase-4 inhibitor teneligliptin: an open-label study in healthy white subjects in Germany. ClinTher. 2014;36(5):760–9.

  • Nakamaru Y, Hayashi Y, Davies M, et al. Investigation of potential pharmacokinetic interactions between teneligliptin and metformin in steady-state conditions in healthy adults. ClinTher. 2015. doi:10.1016/j.clinthera.2015.06.012.

  • Kinoshita S, Kondo K. Evaluation of pharmacokinetic and pharmacodynamic interactions of canagliflozin and teneligliptin.

  • Yoshida T, Akahoshi F, Sakashita H, et al. Discovery and preclinicalprofile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-y lcarbonyl]thiazolidine):a highly potent, selective, longlasting and orallyactive dipeptidyl peptidase IV inhibitor for the treatment of type 2diabetes. Bioorg Med Chem. 2012;20(19):5705–19.

  • Kishimoto M. Teneligliptin: a DPP-4 inhibitor for the treatment of type 2 diabetes. Diabetes Metab Syndrome Obes.2013;6:187–95.

  • Fukuda-Tsuru S, Anabuki J, Abe Y, et al. A novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor, teneligliptin improves postprandial hyperglycemia and dyslipidemia aftersingle and repeated administrations. Eur J Pharmacol.2012;696(1–3):194–202.

  • Eto Et al., Effects of once-daily teneligliptin on 24-h blood glucose control and safety in Japanese patients with type 2 diabetes mellitus, Diabetes, Obesity and Metabolism 14: 1040–1046, 2012.

  • Kadowaki et al., Efficacy, safety and dose–response relationship ofteneligliptin, a dipeptidyl peptidase-4 inhibitor, in Japanese patients with type 2 diabetes mellitus, Diabetes, Obesity and Metabolism 15: 810–818, 2013.

  • Kadowaki et al., Efficacy and safety of teneligliptin added to glimepiride in Japanese patients with type 2 diabetes mellitus: arandomized, double-blind, placebo-controlled study with anopen-label, long-term extension, Diabetes, Obesity and Metabolism 16: 418–425, 2014.

  • EijiKutoha et al., Teneligliptin As an Initial Therapy for Newly Diagnosed, Drug Naive Subjects With Type 2 Diabetes, J Clin Med Res. 2014;6(4):287-294.

  • Rika Ito et al., Teneligliptin, a Dipeptidyl Peptidase-4 Inhibitor, Improves Early-Phase Insulin Secretion in DrugNaive Patients with Type 2 Diabetes, Drugs R D (2015) 15:245–251.

  • Takashi Kadowaki, FuyuhikoMarubayashi, Shoko Yokota, Makoto Katoh& Hiroaki Iijima (2015) Safety and efficacy of teneligliptin in Japanese patients with type2 diabetes mellitus: a pooled analysis of two Phase III clinical studies, Expert Opinion on Pharmacotherapy, 16:7, 971-981

  • Bon Yun Cha, Efficacy and safety of teneligliptin, a dipeptidyl peptidase-4inhibitor, combined with metformin in Korean patients with type2 diabetes mellitus: a 16-week, randomized, double-blind, placebo-controlled phase III trial, Diabetes, Obesity and Metabolism 17: 309–312, 2015.

  • Yoshinobu Nakamaru et al., Investigation of Potential Pharmacokinetic Interactions Between Teneligliptin and Metformin in Steady-StateConditions in Healthy Adults, Clinical Therapeutics2015.

  • Kadowaki T et al., Efficacy and safety of teneligliptin added to glimepiride in Japanese patients with type 2 diabetes mellitus: a randomized, double-blind, placebo-controlled study with an open-label, long-term extension, Diabetes ObesMetab. 2014 May;16(5):418-25.

  • Takashi Kadowaki et al., Efficacy and safety of teneligliptin in combination with pioglitazone in Japanese patients with type 2 diabetes mellitus, Journal of Diabetes Investigation Volume 4 Issue 6 November 2013.

  • Tanaka et al., Add-On Treatment with Teneligliptin Ameliorates Glucose Fluctuations and Improves Glycemic Control Index in Japanese Patients with Type 2 Diabetes on Insulin Therapy, Diabetes Technology & Therapeutics, Volume 16, Number 12, 2014.

  • TakehiroHashikata et al., Teneligliptin improves left ventricular diastolic functionand endothelial function in patients with diabetes, Heart Vessels 2015.

  • AtefHalabi et al., Pharmacokinetics and Safety of Teneligliptin in Subjects With Hepatic Impairment, Clinical Pharmacology in Drug Development 3(4) 2014.

  • AtefHalabi et al., Pharmacokinetics of Teneligliptin in Subjects With Renal Impairment, Clinical Pharmacology in Drug Development 2(3), 2013.

  • Hideo Otsuki et al., Safety and efficacy of teneligliptin: a novel DPP-4 inhibitor for hemodialysis patients with type 2 diabetes, IntUrolNephrol (2014) 46:427–432.

  • Wada, N., Mori, K., Nakagawa, C., Sawa, J., Kumeda, Y., Shoji, T., Emoto, M. &Inaba, M., Improved Glycemic Control with Teneligliptin in Patients with Type 2 Diabetes Mellitus on Hemodialysis: Evaluation by Continuous Glucose Monitoring, Journal of Diabetes and Its Complications, 2015.


Abstract Views: 312

PDF Views: 0




  • Teneligliptin – The Newest DPP4 Inhibitor

Abstract Views: 312  |  PDF Views: 0

Authors

M. Kiran
Medical Services, Centaur Pharmaceuticals Pvt. Ltd., India
H. B. Chandalia
Jaslok Hospital, Mumbai, India

Abstract


Teneligliptin is the newest DPP4 inhibitor approved by the regulatory authority for the treatment of Diabetes mellitus. Teneligliptin scores over other 'gliptins' in being more economical and with better efficacy to control blood glucose and HbA1C levels. Teneligliptin additionally offers other pharmacological advantages like longer half-life, lesser IC50 value, tight and extensive binding to the DPP4 enzyme. Teneligliptin has been studies extensively for its safety and efficacy in various clinical trials conducted internationally. This review article comprehensively documents the available clinical and pharmacological data for Teneligliptin in the treatment of Diabetes mellitus.

Keywords


Diabetes Mellitus, Teneligliptin, HbA1C, Fasting Blood Glucose, Post Prandial Blood Glucose.

References