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Friederike Remm, Nicolle Kränkel, Daniela Lener, Daniel J Drucker, Sieghart Sopper, Christoph Brenner
Introduction: DPP4 inhibitors (gliptins) are commonly used antidiabetic drugs for the treatment of type 2 diabetes. Gliptins also act in a glucose-independent manner and show vasoregenerative effects. We have shown that gliptins can remarkably accelerate vascular healing after vascular injury. However, the underlying mechanisms remain unclear. Here, we examined potential signaling pathways linking gliptins to enhanced endothelial regeneration. Methods and Results: We used wild-type and GLP1 receptor knockout ( Glp1r -/- ) mice to investigate the underlying mechanisms of gliptin-induced reendothelialization...
2018: Stem Cells International
Silvano Fasolato, Elisabetta Trevellin, Mariagrazia Ruvoletto, Marnie Granzotto, Giacomo Zanus, Elisa Boscaro, Enrico Babetto, Liliana Terrin, Maria Alberta Battocchio, Francesco Ciscato, Cristian Turato, Santina Quarta, Umberto Cillo, Patrizia Pontisso, Roberto Vettor
AIMS: In hepatocellular carcinoma (HCC), the regulatory protease Dipeptidyl-peptidase IV (DPPIV/CD26), that possesses pro-apoptotic properties, has been found abnormally regulated. The protease inhibitor SerpinB3, exerting anti-apoptotic activity, has also been described to be upregulated, especially in HCCs with poor prognosis. The aim of this study was to investigate the possible relationship between these two molecules in HCC patients and in experimental models. MATERIALS AND METHODS: DPPIV/CD26 and SerpinB3 expression was measured in liver specimens of 67 patients with HCC...
March 7, 2018: Life Sciences
Venu Gopal Jonnalagadda, Harish Prabhanna Char, Praveen Kumar Ankana
No abstract text is available yet for this article.
March 7, 2018: Cardiovascular Drugs and Therapy
Comfort Omoigemete Olurishe, Helen Ochuko Kwanashie, Abdulkadiri Umar Zezi, Nuhu Mohammed Danjuma, Bisalla Mohammed
OBJECTIVE: Sitagliptin (ST) and Moringa oleifera (MO) Lam (Moringaceae) are used concomitantly by diabetic patients, with no study ascertaining for potential favorable or otherwise renal implications. We investigated the effect of coadministration of ST and MO leaf extract on functional and morphological biomarkers of alloxan-induced diabetic nephropathy (DN). MATERIALS AND METHODS: Diabetes was induced with a single dose of 150 mg/kg of alloxan intraperitoneally...
September 2017: Indian Journal of Pharmacology
Ganesh V Sangle, Mohan Patil, Nitin J Deshmukh, Sushant A Shengule, Shantibhushan Kamble, Kiran Kumar Vuppalavanchu, Sushil Kale, Mirza Layeeq Ahmed Baig, Geetchandra Singh, Javed Shaikh, Jitendra Tripathi, P Aravindababu
PURPOSE: Sitagliptin, a dipeptidyl peptidase (DPP)-IV inhibitor approved for the treatment of type 2 diabetes, is reported to be more efficacious in Indian patients than non-Indian patient population. The objective of the study was to evaluate pharmacokinetic and pharmacodynamic (PK/PD) parameters of single-dose sitagliptin 100 mg (Januvia) in healthy Indian male participants. METHOD: In a randomised, single-dose, open-label, three-treatment, three-period, three-sequence, crossover bioavailability study, 18 healthy male participants received single-dose of sitagliptin under fasted and fed conditions...
March 6, 2018: European Journal of Clinical Pharmacology
John F Marcinak, Melvin S Munsaka, Paul B Watkins, Takashi Ohira, Neila Smith
INTRODUCTION: Fasiglifam (TAK-875) is a G protein-coupled receptor 40 agonist that was being investigated for treatment of type 2 diabetes mellitus (T2DM). A development program was terminated late in phase III clinical trials due to liver safety concerns. METHODS: The liver safety of fasiglifam was assessed from data based on six phase II and nine phase III double-blind studies and two open-label studies with emphasis on pooled data from 15 double-blind studies from both global and Japanese development programs...
February 28, 2018: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
Yuichiro Yamada, Yasuo Terauchi, Hirotaka Watada, Yasuhiko Nakatsuka, Kazuhito Shiosakai, Takuo Washio, Takashi Taguchi
INTRODUCTION: G protein-coupled receptor 119 (GPR119) is a promising target for the treatment of type 2 diabetes mellitus (T2DM), as both insulin and glucagon-like peptide-1 secretion can be promoted with a single drug. We compared the efficacy and safety of the GPR119 agonist DS-8500a with placebo and sitagliptin 50 mg in Japanese patients with T2DM. METHODS: This randomized, double-blind, parallel-group comparison study was conducted in Japan (trial registration NCT02628392, JapicCTI-153068)...
February 27, 2018: Advances in Therapy
Dongdong Wang, Guanying Zhang, Xiao Chen, Tong Wei, Chenxu Liu, Chun Chen, Yinhan Gong, Qunli Wei
Diabetic nephropathy (DN) is the leading cause of end-stage failure of the kidney, but the efficacy of current strategies available for the prevention of DN remains unsatisfactory. The purpose of this study was to assess whether sitagliptin (SIT) has therapeutic potential for prevention of DN and to investigate its possible mechanism. The effects of SIT on DN were investigated in rats with type 2 diabetes mellitus (T2DM) and rat mesangial cells (MCs) induced by high glucose. T2DM rats were administered at a dose of 10 mg/kg SIT...
February 16, 2018: International Journal of Molecular Medicine
Jessica R Wilson, Nancy J Brown, Hui Nian, Chang Yu, Martin Bidlingmaier, Jessica K Devin
BACKGROUND: Diminished growth hormone (GH) is associated with impaired endothelial function and fibrinolysis. GH-releasing hormone is the primary stimulus for GH secretion and a substrate of dipeptidyl peptidase-4. We tested the hypothesis that dipeptidyl peptidase-4 inhibition with sitagliptin increases stimulated GH secretion, vasodilation, and tissue plasminogen activator (tPA) activity. METHODS AND RESULTS: Healthy adults participated in a 2-part double-blind, randomized, placebo-controlled, crossover study...
February 25, 2018: Journal of the American Heart Association
Anthony Markham
Ertugliflozin (Steglatro™) is an orally active sodium glucose co-transporter type 2 inhibitor being developed by Merck and Pfizer as a treatment for type 2 diabetes mellitus (T2DM). Ertugliflozin as monotherapy and in combination with various other antidiabetic drugs was associated with improvements in glycaemic control and secondary outcome measures in the VERTIS phase III clinical trial program. Ertugliflozin and fixed-dose combinations of ertugliflozin and metformin (Segluromet™) and ertugliflozin and sitagliptin (Steglujan™) have recently been approved by the US FDA as an adjunct to diet and exercise to improve glycaemic control in adults with T2DM...
February 23, 2018: Drugs
André Jacques Scheen
Dipeptidyl peptidase-4 inhibitors (DPP-4is) are generally considered as glucose-lowering agents with a safe profile in type 2 diabetes. Areas covered: An updated review of recent safety data from randomised controlled trials, observational studies, meta-analyses, pharmacovigilance reports regarding alogliptin, linagliptin, saxagliptin, sitagliptin, and vildagliptin, with a special focus on risks of hypoglycemia, pancreatitis and pancreatic cancer, major cardiovascular events, hospitalisation for heart failure and other new safety issues, such as bone fractures and arthralgia...
April 2018: Expert Opinion on Drug Safety
Elisa J Campos, João Martins, Dan Brudzewsky, Sandra Correia, Ana R Santiago, David Pd Woldbye, António F Ambrósio
BACKGROUND: Neuropeptide Y (NPY) is a neuromodulator that is expressed in the retina. Increasing evidence suggests that NPY has pronounced anti-inflammatory effects, which might depend on the inhibition of dipeptidyl-peptidase-IV (DPP-IV). The aim of this study was to investigate the impact of type 1 diabetes mellitus (DM) and sitagliptin, a DPP-IV inhibitor, on the NPY system in the retina using an animal model. METHODS: Type 1 DM was induced in male Wistar rats by an intraperitoneal injection of streptozotocin (STZ)...
February 14, 2018: Clinical & Experimental Ophthalmology
Chan-Hee Jung, Eun-Jung Rhee, Won-Young Lee, Kyung Wan Min, Vyankatesh K Shivane, Aravind R Sosale, Hak Chul Jang, Choon Hee Chung, Il Seong Nam-Goong
We investigated the long-term efficacy and safety of gemigliptin and the efficacy and safety of gemigliptin treatment after once daily treatment with sitagliptin 100 mg, in patient with type 2 diabetes. This study was a 28-week, extension of a 24-week, randomized, double-blind, parallel study of gemigliptin or sitagliptin, added to ongoing metformin therapy. After randomized to sitagliptin 100 mg qd(S), gemigliptin 25 mg bid (G1), or gemigliptin 50 mg qd(G2) groups and completing treatment of 24 weeks, 118 patients switched from gemigliptin 25 mg bid to 50 mg qd(G1/G2), 111 patients continued gemigliptin 50 mg qd(G2/G2), and 106 patients switched from sitagliptin 100 mg qd to gemigliptin 50 mg qd(S/G2)...
February 13, 2018: Diabetes, Obesity & Metabolism
Shinichiro Ueda, Michio Shimabukuro, Osamu Arasaki, Koichi Node, Takashi Nomiyama, Takeshi Morimoto
BACKGROUND: Reduction of low-density lipoprotein cholesterol (LDL-C) is important for patients with a high risk for atherosclerotic events, such as patients with diabetes and other risk factors. Anagliptin was reported to reduce LDL-C for 12 weeks in phase III trials regardless of the use of statins, but it is uncertain whether this effect is common to other dipeptidylpeptidase-4 (DPP-4) inhibitors. METHODS: A multicenter, randomized, open-label, parallel-group trial was conducted to confirm the superiority of anagliptin to sitagliptin in terms of the primary endpoint of reduction of LDL-C for 52 weeks in patients with type 2 diabetes and atherosclerotic vascular lesions, as well as the non-inferiority of anagliptin to sitagliptin in terms of change in hemoglobin A1c (HbA1c)...
February 12, 2018: Cardiovascular Drugs and Therapy
Mahesh Thondawada, Ashish Devidas Wadhwani, Dhanabal S Palanisamy, Hanumant Singh Rathore, Ramesh C Gupta, Pavan Kumar Chintamaneni, Malay K Samanta, Anil Dubala, Sameer Varma, Praveen T Krishnamurthy, Kuppusamy Gowthamarajan
Nanotechnology based bio-medical approaches and surface modification techniques made it easier for targeting specific site and improving the treatment efficacy. The present study reports on targeted polymeric nanoparticles conjugated with antibody as a site-specific carrier system for effective treatment of Type 1 diabetes. Sitagliptin (SP) loaded Poly (lactic-co-glycolic acid) (PLGA) nanoparticles (NP) were prepared by nanoprecipitation cum solvent evaporation method and were characterized in terms of morphology, size, surface charge and entrapment efficiency...
February 12, 2018: Drug Development and Industrial Pharmacy
Hiroshi Sakura, Naotake Hashimoto, Kazuo Sasamoto, Hiroshi Ohashi, Sumiko Hasumi, Noriko Ujihara, Tadasu Kasahara, Osamu Tomonaga, Hideo Nunome, Masashi Honda, Yasuhiko Iwamoto
AIMS/INTRODUCTION: Hemoglobin A1c (HbA1c) levels in patients with type 2 diabetes mellitus (T2DM) fluctuate throughout the year. However, there are few studies that have evaluated the therapeutic effect of hypoglycemic agents while considering such fluctuations. In a multi-center study (JAMP Study), pre-treatment patients with T2DM were divided into seven groups and administered sitagliptin for 1 year. The aim of this study was to evaluate the differences in the therapeutic effect, and efficacy, of sitagliptin in patients with T2DM based on the month administration of the drug began as sub-analysis of the JAMP Study...
February 10, 2018: Journal of Diabetes Investigation
Timothy M E Davis, Hillary Mulder, Yuliya Lokhnygina, Pablo Aschner, Lee-Ming Chuang, Carlos A Raffo Grado, Eberhard Standl, Eric D Peterson, Rury R Holman
AIM: Pooled efficacy studies suggest that glycaemic responses to dipeptidyl-peptidase 4 inhibitors in type 2 diabetes are greatest in Asians, who may also respond better to alpha-glucosidase inhibitors. We assessed the glycaemic impact of sitagliptin by race in the Trial Evaluating Cardiovascular Outcomes with Sitagliptin (TECOS), and whether this was enhanced in Asians with concomitant acarbose therapy. MATERIALS AND METHODS: TECOS enrolled 14,671 patients with type 2 diabetes, cardiovascular disease and HbA1c of 48-64 mmol/mol (6...
February 6, 2018: Diabetes, Obesity & Metabolism
Yuexin Tang, Xingyue Huang, Jinan Liu, R Ravi Shankar, Michael L Ganz, Swapnil Rajpathak
Background: Health plans have responded to the many treatment options for type 2 diabetes mellitus by implementing formulary restriction policies, including step therapy, to control costs. Little is known about the impact of step therapy programs on antidiabetes medication use. Objective: To assess the impact of a sitagliptin step therapy program on antidiabetes medication use among sitagliptin users. Methods: Using pharmacy claims from the Symphony Health Solutions' Integrated Dataverse, we compared the use of sitagliptin and other antidiabetes medications by patients enrolled in a health plan (Plan A) that implemented a sitagliptin step therapy program on July 1, 2013, with the use by patients who were contemporaneously enrolled in 2 comparison plans-Plans B and C-without step therapy programs...
December 2017: American Health & Drug Benefits
Naoto Katakami, Tomoya Mita, Yoko Irie, Mitsuyoshi Takahara, Taka-Aki Matsuoka, Masahiko Gosho, Hirotaka Watada, Iichiro Shimomura
BACKGROUND: Ultrasonic gray-scale median (GSM) of the carotid wall reflects its composition and low-GSM carotid plaque is considered to be vulnerable. This study aimed to evaluate the effect of sitagliptin, a dipeptidyl peptidase-4 inhibitor, on the longitudinal change in GSM, an index of the tissue characteristics of the carotid wall, in patients with type 2 diabetes mellitus (T2DM). METHODS: This is a post hoc sub-analysis using data obtained from the SPIKE trial, a randomized controlled trial that demonstrated the beneficial effect of sitagliptin on the progression of carotid intima-media thickness in patients with T2DM...
February 5, 2018: Cardiovascular Diabetology
Steven P Marso, Elise Hardy, Jenny Han, Hui Wang, Robert J Chilton
INTRODUCTION: Glucagon-like peptide-1 receptor agonists (GLP-1RAs) improve glycemia in patients with type 2 diabetes, but heart rate increases have been observed. METHODS: A pooled post hoc analysis of 11 randomized clinical trials (N = 4595) of 10-30 weeks' duration from the exenatide once-weekly (QW) development program evaluated heart rate with exenatide QW (intervention group) and exenatide twice daily (BID), liraglutide, and non-GLP-1RAs (insulin, metformin, pioglitazone, and sitagliptin) (comparison groups)...
February 3, 2018: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
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