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Fumitaka Okajima, Tomoko Nagamine, Yuko Nakamura, Naomi Hattori, Hitoshi Sugihara, Naoya Emoto
The efficacy of the administration of sodium-glucose co-transporter 2 inhibitor (SGLT2I) or the co-administration of SGLT2I and dipeptidyl peptidase-4 inhibitor (DPP-4I) to insulin therapy is not well known. Fifty-eight patients with type 2 diabetes, admitted for glycemic control, were randomized to basal-bolus insulin therapy (BBT) alone or BBT plus 50 mg ipragliflozin and/or 20 mg teneligliptin. Insulin doses were adjusted to maintain normal blood glucose levels. Plasma glucose profiles were estimated by continuous glucose monitoring (CGM) before discharge...
October 20, 2016: Journal of Diabetes Investigation
Chihiro Moriya, Hiroaki Satoh
We investigated the effects of teneligliptin on uric acid metabolism in male Wistar rats and 3T3-L1 adipocytes. The rats were fed with a normal chow diet (NCD) or a 60% high-fat diet (HFD) with or without teneligliptin for 4 weeks. The plasma uric acid level was not significantly different between the control and teneligliptin groups under the NCD condition. However, the plasma uric acid level was significantly decreased in the HFD-fed teneligliptin treated rats compared to the HFD-fed control rats. The expression levels of xanthine dehydrogenase (Xdh) mRNA in liver and epididymal adipose tissue of NCD-fed rats were not altered by teneligliptin treatment...
2016: Journal of Diabetes Research
Surendra Kumar Sharma, A Panneerselvam, K P Singh, Girish Parmar, Pradeep Gadge, Onkar C Swami
Teneligliptin is a recently developed oral dipeptidyl peptidase 4 inhibitor indicated for the management of type 2 diabetes mellitus (T2DM) in adults along with diet and exercise. Teneligliptin has been recently available in Japan (Teneria(®)), Argentina (Teneglucon(®)), and India (Tenepure; Teneza) at relatively affordable price. This is a positive step toward the management of T2DM in developing countries, where the cost of medicine is out-of-pocket expenditure and is a limiting factor for health care. This review evaluates the efficacy and safety of teneligliptin in the management of T2DM...
2016: Diabetes, Metabolic Syndrome and Obesity: Targets and Therapy
Gemma Pujadas, Valeria De Nigris, Francesco Prattichizzo, Lucia La Sala, Roberto Testa, Antonio Ceriello
Dipeptidyl peptidase-4 inhibitors are widely used in type 2 diabetes. Endothelium plays a crucial role maintaining vascular integrity and function. Chronic exposure to high glucose drives to endothelial dysfunction generating oxidative stress. Teneligliptin is a novel dipeptidyl peptidase-4 inhibitor with antioxidant properties. This study is aimed to verify a potential protective action of teneligliptin in endothelial cells exposed to high glucose. Human umbilical vein endothelial cells were cultured under normal (5 mmol/L) or high glucose (25 mmol/L) during 21 days, or at high glucose during 14 days followed by 7 days at normal glucose, to reproduce the high-metabolic memory state...
August 16, 2016: Endocrine
Hideo Okonogi, Mikio Harada, Hironobu Sato, Kazuhiko Tokoro, Issei Nakayama, Nobuo Tsuboi, Yoichi Miyazaki, Tetsuya Kawamura, Makoto Ogura, Takashi Yokoo
A 46-year-old diabetic man underwent the removal of a hematoma caused by traumatic brain injury. After surgery, severe hyponatremia occurred. The subsequent administration of NaCl and fludrocortisone improved his laboratory findings. The patient was transferred to our hospital, and his insulin therapy was replaced by teneligliptin. One week later, ipragliflozin treatment was initiated and induced an immediate increase in the serum sodium levels. NaCl and fludrocortisone were therefore discontinued. However, hyponatremia recurred after ipragliflozin withdrawal due to a urinary tract infection...
2016: Internal Medicine
Haruya Kawase, Yasuko K Bando, Kazuyuki Nishimura, Morihiko Aoyama, Akio Monji, Toyoaki Murohara
BACKGROUND: To address the impact of antidiabetic drugs on cardiovascular safety is a matter of clinical concern. Preclinical studies revealed that various protective effects of dipeptidyl peptidase-4 inhibitor (DPP4i) on cardiovascular disease; however, its impact of on hypertension remains controversial. METHODS AND RESULTS: Teneligliptin (TEN; 10mg/kg/day/p.o.) ameliorates hypertension and cardiac remodeling by normalizing a rise of angiotensin-II (AngII) that specifically observed in spontaneously hypertensive rats (SHR)...
September 2016: Journal of Molecular and Cellular Cardiology
Eiji Kutoh, Asuka Wada, Sayaka Terayama
BACKGROUND AND OBJECTIVES: Teneligliptin, a chemotype prolyl-thiazolidine-based novel dipeptidyl peptidase (DPP)-4 inhibitor, was preliminarily shown to reduce insulin resistance in patients with type 2 diabetes mellitus (T2DM). The objective of this study is to further investigate the insulin sensitising properties of teneligliptin in comparison to those of sitagliptin. METHODS: Treatment-naïve subjects with T2DM were administered 20 mg/day teneligliptin monotherapy (n = 45)...
October 2016: Clinical Drug Investigation
Masaaki Sagara, Kunihiro Suzuki, Chie Aoki, Seiichi Tanaka, Isao Taguchi, Teruo Inoue, Yoshimasa Aso
BACKGROUND: The aim of the present study was to elucidate the effect of teneligliptin on oxidative stress and endothelial function in Japanese patients with type 2 diabetes and chronic kidney disease (CKD). METHODS: Forty-five patients with type 2 diabetes and CKD who received sitagliptin for at least 12 months were randomized to either continue sitagliptin (n = 23) or switch to teneligliptin (n = 22) for 24 weeks. The following parameters were evaluated at baseline and after 24 weeks of treatment with continued sitagliptin or teneligliptin: blood pressure, haemoglobin A1c (HbA1c), estimated glomerular filtration rate (eGFR), urinary albumin excretion, endothelial function by reactive hyperaemia index (RHI; EndoPAT(®) system), reactive oxygen metabolites (ROMs) measured by the d-ROMS test, 8-hydroxy-2'-deoxyguanosine, urinary liver-type fatty acid binding protein (L-FABP), and urinary 8-isoprostane...
2016: Cardiovascular Diabetology
Andrew Bryson, Paul E Jennings, Laszlo Deak, Fraga S Paveliu, Matt Lawson
OBJECTIVE: The study investigated the efficacy and tolerability of teneligliptin co-administered to patients with type 2 diabetes mellitus (T2DM) who were inadequately controlled by stable metformin monotherapy ≥ 1000 mg/day. METHODS: A total of 447 patients from 55 European centers who completed a 14-day screening and 14-day run-in phase, received randomized double-blind treatment with 5, 10, 20 or 40 mg teneligliptin or placebo once daily, for 24 weeks. 364 patients continued treatment in a 28-week open label extension during which they received teneligliptin 20 mg once daily...
July 2016: Expert Opinion on Pharmacotherapy
Yoshinori Okuda, Seitaro Omoto, Takehito Taniura, Akira Shouzu, Shosaku Nomura
BACKGROUND: Cardiovascular disease (CVD) is the main cause of death among hemodialysis (HD) patients. The effects of the dipeptidyl peptidase-4 inhibitor teneligliptin on CVD-related biomarkers in patients with type 2 diabetes mellitus (T2DM) receiving HD treatment are poorly understood. To determine whether teneligliptin has anti-CVD properties, we assessed its effects on soluble P-selectin (sP-selectin), platelet-derived microparticles (PDMPs), plasminogen activator inhibitor 1 (PAI-1), soluble E-selectin (sE-selectin), soluble vascular adhesion molecule 1 (sVCAM-1), and adiponectin plasma levels in HD and non-HD patients with T2DM...
2016: International Journal of General Medicine
Takehiro Hashikata, Minako Yamaoka-Tojo, Ryota Kakizaki, Teruyoshi Nemoto, Kazuhiro Fujiyoshi, Sayaka Namba, Lisa Kitasato, Takuya Hashimoto, Ryo Kameda, Emi Maekawa, Takao Shimohama, Taiki Tojo, Junya Ako
No abstract text is available yet for this article.
February 18, 2016: Heart and Vessels
Shinichiro Kimura, Toyoshi Inoguchi, Toshihide Yamasaki, Mayumi Yamato, Makoto Ide, Noriyuki Sonoda, Kenichi Yamada, Ryoichi Takayanagi
AIMS: Recently various dipeptidyl peptidase-4 (DPP-4) inhibitors have emerged because of their high effectiveness and safety. In spite of their common effect of DPP-4 inhibition, the chemical structures are diverse. Here we show that the structure of teneligliptin, a novel DPP-4 inhibitor, has a scavenging activity on hydroxyl radical (·OH). METHODS: ·OH and superoxide (O2(-)) were detected by electron spin resonance (ESR) spectroscopy. ·OH and O2(-) were generated in vitro by the Fenton reaction and a hypoxanthine-xanthine oxidase system, respectively...
March 2016: Metabolism: Clinical and Experimental
Lesley J Scott
Oral teneligliptin [Teneglucon® (Argentina)], a dipeptidyl peptidase-4 inhibitor, is indicated for the treatment of adults with type 2 diabetes (T2DM). This article reviews the pharmacology, therapeutic efficacy and tolerability of teneligliptin in the treatment of adults with T2DM. In 12- or 16-week, placebo-controlled phase 2 and 3 trials, oral teneligliptin 20 or 40 mg once daily, as monotherapy or in combination with metformin, glimepiride or pioglitazone improved glycaemic control, including in patients with end-stage renal disease, and was generally well tolerated...
November 2015: Clinical Drug Investigation
Enrique Z Fisman, Alexander Tenenbaum
The traditional oral pharmacological therapy for type 2 diabetes mellitus (T2DM) has been based on the prescription of metformin, a biguanide, as first line antihyperglycemic agent world over. It has been demonstrated that after 3 years of treatment, approximately 50% of diabetic patients could achieve acceptable glucose levels with monotherapy; but by 9 years this had declined to only 25%. Therefore, the implementation of a combined pharmacological therapy acting via different pathways becomes necessary, and its combination with a compound of the sulfonylurea group was along decades the most frequently employed prescription in routine clinical practice...
2015: Cardiovascular Diabetology
S Shantikumar, N Satheeshkumar, R Srinivas
The aim of the present study is to explore pharmacokinetic and protein binding characteristics of a novel dipeptidylpeptidase-4 (DPP-4) inhibitor, teneligliptin in rats using an ultra high performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UHPLC-QTOF-MS). It is required for demonstrating the high protein binding nature of teneligliptin which can be extended for drug repositioning to brain disorders. Sample preparation was accomplished through a protein precipitation procedure using acetonitrile...
October 1, 2015: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Noritsugu Wada, Katsuhito Mori, Chie Nakagawa, Jun Sawa, Yasuro Kumeda, Tetsuo Shoji, Masanori Emoto, Masaaki Inaba
AIMS: Recent reports suggest that appropriate glycemic control without hypoglycemia could decrease mortality in patients with diabetes mellitus (DM) and end-stage renal disease (ESRD). However, an indication of oral anti-diabetic drugs is limited in this population. The aim of this study was to evaluate efficacy of teneligliptin, a novel DPP-4 inhibitor, by continuous glucose monitoring (CGM) in patients with type 2 DM (T2DM) on hemodialysis (HD). METHODS: This 4-week, open label, single arm, intervention trial included 10 diabetic patients undergoing HD and with glycated albumin (GA) level of ≥18...
November 2015: Journal of Diabetes and its Complications
Takehiro Hashikata, Minako Yamaoka-Tojo, Ryota Kakizaki, Teruyoshi Nemoto, Kazuhiro Fujiyoshi, Sayaka Namba, Lisa Kitasato, Takuya Hashimoto, Ryo Kameda, Emi Maekawa, Takao Shimohama, Taiki Tojo, Junya Ako
Incretin hormones have been reported to have cytoprotective actions in addition to their glucose-lowering effects. We evaluated whether teneligliptin, a novel dipeptidyl peptidase-4 (DPP-4) inhibitor, affects left ventricular (LV) function in patients with type 2 diabetes mellitus (T2DM). Twenty-nine T2DM patients not receiving any incretin-based drugs were enrolled and prescribed with teneligliptin for 3 months. Compared to baseline levels, hemoglobin A1c levels decreased (7.6 ± 1.0 % to 6.9 ± 0.7 %, p < 0...
August 2016: Heart and Vessels
Azusa Sameshima, Tsutomu Wada, Tetsuo Ito, Ayaka Kashimura, Kanae Sawakawa, Rika Yonezawa, Hiroshi Tsuneki, Yoko Ishii, Masakiyo Sasahara, Shigeru Saito, Toshiyasu Sasaoka
A decrease in serum estrogen levels in menopause is closely associated with the development of visceral obesity and the onset of type 2 diabetes in women. In the present study, we demonstrated the therapeutic effects of the novel DPP4 inhibitor, teneligliptin, on the features of postmenopausal obesity in mice. In the control group, female C57BL/6 mice were sham-operated and maintained on a standard diet. In the postmenopausal obese group, ovariectomized (OVX) mice were maintained on a high-fat diet, and were referred to as OVX-HF...
October 2015: Journal of Endocrinology
Rika Ito, Tomoyasu Fukui, Toshiyuki Hayashi, Anna Osamura, Makoto Ohara, Noriko Hara, Akiko Higuchi, Takeshi Yamamoto, Tsutomu Hirano
INTRODUCTION: It remains unknown whether dipeptidyl peptidase-4 (DPP-4) inhibitors improve early-phase insulin secretion in Japanese patients with type 2 diabetes (T2D), a disease characterized by impaired insulin secretion. We investigated the changes in insulin secretion before and after treatment with the DPP-4 inhibitor teneligliptin in patients with T2D with a low insulinogenic index (IGI) determined by the oral glucose tolerance test (OGTT). METHODS: An open-label, prospective clinical study was conducted...
September 2015: Drugs in R&D
Yoshinobu Nakamaru, Yoshiharu Hayashi, Martin Davies, Horst Jürgen Heuer, Noriko Hisanaga, Kei Akimoto
PURPOSE: We assessed the effects of coadministration of metformin and teneligliptin on their pharmacokinetics in steady-state conditions relative to the administration of either drug alone. METHODS: This was a Phase I, single-center, open-label, 2-way parallel-group study in healthy male and female subjects. Subjects in group 1 (n = 20) were administered 40 mg of teneligliptin once daily for 5 days, and 850 mg of metformin BID was added to ongoing teneligliptin for an additional 3 days...
September 2015: Clinical Therapeutics
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