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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
Osamu Tomonaga, Hiroshi Sakura, Naotake Hashimoto, Kazuo Sasamoto, Hiroshi Ohashi, Sumiko Hasumi, Noriko Ujihara, Tadasu Kasahara, Hideo Nunome, Masashi Honda, Yasuhiko Iwamoto
Background: The aim of the study was to determine the effects of sitagliptin on renal function in a diabetic population including patients with normal renal function. Methods: We analyzed the association between 12-month, 50 mg/day sitagliptin and renal function in outpatients with type 2 diabetes mellitus and poor blood glucose control in a subset of patients in the larger Januvia Multicenter Prospective Trial in Type 2 Diabetes observational study. Stratified analyses of changes in estimated glomerular filtration rate (eGFR) and urinary albumin-to-creatinine ratio (UACR) were performed...
January 2018: Journal of Clinical Medicine Research
Mohammad B Khaled, Roukaya K El Mokadem, Jimmie D Weaver
The photocatalytic C-F functionalization of highly fluorinated arenes is a powerful method for accessing functionalized multifluorinated arenes. The decisive step in the determining regioselectivity in fluorine functionalization is fluoride fragmentation from the radical anion of the multifluorinated arene. To date, the availability of regioisomers has been dictated by the innate electronics of the fluorinated arene, limiting the synthetic utility of the chemistry. This study investigates the remarkable ability of a strategically located hydrogen bond to transcend the normal regioselectivity of the C-F functionalization event...
September 8, 2017: Journal of the American Chemical Society
Xiaozhen Dai, Jun Zeng, Xiaoqing Yan, Qian Lin, Kai Wang, Jing Chen, Feixia Shen, Xuemei Gu, Yuehui Wang, Jun Chen, Kejian Pan, Lu Cai, Kupper A Wintergerst, Yi Tan
Recently, the dipeptidyl peptidase-4 (DPP-4) inhibitor sitagliptin, a major anti-hyperglycaemic agent, has received substantial attention as a therapeutic target for cardiovascular diseases via enhancing the number of circulating endothelial progenitor cells (EPCs). However, the direct effects of sitagliptin on EPC function remain elusive. In this study, we evaluated the proangiogenic effects of sitagliptin on a diabetic hind limb ischaemia (HLI) model in vivo and on EPC culture in vitro. Treatment of db/db mice with sitagliptin (Januvia) after HLI surgery efficiently enhanced ischaemic angiogenesis and blood perfusion, which was accompanied by significant increases in circulating EPC numbers...
January 2018: Journal of Cellular and Molecular Medicine
Rhona Johnston, Olalekan Uthman, Ewen Cummins, Christine Clar, Pamela Royle, Jill Colquitt, Bee Kang Tan, Andrew Clegg, Saran Shantikumar, Rachel Court, J Paul O'Hare, David McGrane, Tim Holt, Norman Waugh
BACKGROUND: Most people with type 2 diabetes are overweight, so initial treatment is aimed at reducing weight and increasing physical activity. Even modest weight loss can improve control of blood glucose. If drug treatment is necessary, the drug of first choice is metformin. However, some people cannot tolerate metformin, which causes diarrhoea in about 10%, and it cannot be used in people with renal impairment. This review appraises three of the newest class of drugs for monotherapy when metformin cannot be used, the sodium-glucose co-transporter 2 (SGLT2) inhibitors...
January 2017: Health Technology Assessment: HTA
Lesley J Scott
The dipeptidyl peptidase-4 inhibitor sitagliptin (Januvia® ; Glactiv® ; Tesavel® ; Xelevia™) is approved in more than 130 countries worldwide as monotherapy and in combination with other antihyperglycaemic drugs for the treatment of adult patients with type 2 diabetes (T2D). Extensive clinical experience has firmly established the glycaemic efficacy of oral sitagliptin (±other antihyperglycaemic drugs) in a broad spectrum of patients with T2D, including obese, elderly and renally impaired patients and those with established cardiovascular (CV) disease (CVD)...
February 2017: Drugs
Maeve Lynch, Tomás B Ahern, Irene Timoney, Cheryl Sweeney, Genevieve Kelly, Rosalind Hughes, Anne-Marie Tobin, Donal O'Shea, Brian Kirby
BACKGROUND: Moderate to severe psoriasis is a systemic inflammatory disease associated with insulin resistance, obesity and type 2 diabetes (T2DM). Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that improves glycaemia and has a marketing authorisation for the treatment of T2DM. Non-immunosuppressive therapies that are effective for psoriasis and its associated comorbidities would be a significant advance in the treatment of this chronic disease. METHODS/DESIGN: This is a single centre, 39-week, prospective, randomised, open label, clinical trial of oral sitagliptin (Januvia(®)) in psoriasis patients who are due to undergo a course of narrow-band ultraviolet-B (NB-UVB) phototherapy...
January 15, 2016: Trials
Yue Ren, Spencer Chiang, Wenpeng Zhang, Xiao Wang, Ziqing Lin, Zheng Ouyang
Paper spray has been developed as an ambient ionization method for direct analysis of biological samples using mass spectrometry. While distinct advantages of paper spray have been demonstrated, especially for quantitative analysis and design of disposable sample cartridges, the need for improvement has also been recognized, especially for the use with miniature mass spectrometers. In this study, we made an improvement to the sampling and ionization by adding a capillary emitter to the paper substrate to produce a paper-capillary spray, which has been shown to have significant, positive impact on the sensitivity and reproducibility for direct mass spectrometry analysis...
February 2016: Analytical and Bioanalytical Chemistry
Altug Akay, Andrei Dragomir, Björn-Erik Erlandsson
A novel data mining method was developed to gauge the experience of the drug Sitagliptin (trade name Januvia) by patients with diabetes mellitus type 2. To this goal, we devised a two-step analysis framework. Initial exploratory analysis using self-organizing maps was performed to determine structures based on user opinions among the forum posts. The results were a compilation of user's clusters and their correlated (positive or negative) opinion of the drug. Subsequent modeling using network analysis methods was used to determine influential users among the forum members...
January 2015: IEEE Journal of Biomedical and Health Informatics
Sahar Kamal Hegazy
Osteoporosis is the most important metabolic bone disease in patients with diabetes mellitus. Several studies have documented that metformin is osteogenic in vitro. In contrast, others showed no effect of metformin on the osteogenic differentiation of bone marrow-derived mesenchymal stem cells. Incretin hormones have received much attention because of their beneficial effects beyond glycemia, including on bone health. The study evaluated the anti-osteoporotic effect of metformin and sitagliptin in postmenopausal diabetic women...
March 2015: Journal of Bone and Mineral Metabolism
Greg L Plosker
Sitagliptin (Januvia(®), Xelevia™, Glactiv(®), Tesavel(®)) is an orally administered, potent and highly selective inhibitor of dipeptidyl peptidase-4 (DPP-4) and was the first agent of its class to be approved for use in the management of adults with type 2 diabetes. Numerous randomized placebo- or active comparator-controlled trials have demonstrated the efficacy of sitagliptin in terms of improving glycaemic control in patients with type 2 diabetes, including its use as monotherapy, initial combination therapy (usually with fixed-dose combinations of sitagliptin/metformin), or add-on therapy to metformin or to other antihyperglycaemic drugs, with or without metformin...
February 2014: Drugs
A J Scheen, L F Van Gaal
Sitagliptin (Januvia) was the first selective inhibitor of dipeptidyl peptidase-4 commercialized for the management of type 2 diabetes. It is also available as a fixed-dose combination with meformin (Janumet). Almost 5 years after its launch in Belgium, the present review summarizes the most recent data regarding the clinical efficacy of this antidiabetic agent, the controversy about its safety profile, its use at lower dosage in case of moderate to severe renal insufficiency, the various indications that have been successively accepted and reimbursed, and, finally, the perspectives offered by a large ongoing cardiovascular outcome trial (TECOS)...
October 2013: Revue Médicale de Liège
A Akay, A Dragomir, Björn-Erik Erlandsson
A novel data-mining method was developed to gauge the experiences of the diabetes mellitus drug Januvia. Self-organizing maps were used to analyze forum posts numerically to infer user opinion of drug Januvia. Graph theory was used to discover influential users. The result is a word list compilation correlating positive and negative word cluster groups and a web of influential users on Januvia. The implications could open new research avenues into rapid data collection, feedback, and analysis that would enable improved solutions for public health...
2013: Conference Proceedings: Annual International Conference of the IEEE Engineering in Medicine and Biology Society
Guillermo E Umpierrez, Roma Gianchandani, Dawn Smiley, Sol Jacobs, David H Wesorick, Christopher Newton, Farnoosh Farrokhi, Limin Peng, David Reyes, Sangeeta Lathkar-Pradhan, Francisco Pasquel
OBJECTIVE: This study investigated the safety and efficacy of sitagliptin (Januvia) for the inpatient management of type 2 diabetes (T2D) in general medicine and surgery patients. RESEARCH DESIGN AND METHODS: In this pilot, multicenter, open-label, randomized study, patients (n = 90) with a known history of T2D treated with diet, oral antidiabetic agents, or low total daily dose of insulin (≤0.4 units/kg/day) were randomized to receive sitagliptin alone or in combination with glargine insulin (glargine) or to a basal bolus insulin regimen (glargine and lispro) plus supplemental (correction) doses of lispro...
November 2013: Diabetes Care
Erin L St Onge, Shannon Miller, Elizabeth Clements
Used together, sitagliptin (Januvia) and metformin (Glucophage) help to improve glycemic levels in diabetic patients, suggesting a synergy between the agents. However, the cost of sitagliptin and the need for more data may restrict its use. More studies are needed to assess the effects of long-term sitagliptin and to determine its role in combination therapy.
December 2012: P & T: a Peer-reviewed Journal for Formulary Management
Sherea M Stricklin, William V Stoecker, Ryan K Rader, Antoinette F Hood, Jerome Z Litt, Thomas P Schuman
Photosensitivity to sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, is reported. No previous reports of photosensitivity to any DPP-4 inhibitors are known. Physical examination of the patient revealed edematous plaques confined to sun-exposed areas of the skin. An unusual finding in this case was the spongy sensation upon palpation of the plaques. Histopathology revealed parakeratosis and abundant eosinophils, supporting the clinical impression of cutaneous drug sensitivity. The eruption finally cleared, approximately two years after onset...
February 2012: Dermatology Online Journal
Quan Shang, Matthew K Liu, Monica Saumoy, Jens Juul Holst, Gerald Salen, Guorong Xu
Bile acid sequestrants have been shown to reduce glucose levels in patients with type 2 diabetes. We previously reported that the bile acid sequestrant colesevelam HCl (Welchol) (COL) induced the release of glucagon-like peptide (GLP)-1 and improved glycemic control in insulin-resistant rats. In the present study, we tested whether adding sitagliptin (Januvia) (SIT), which prolongs bioactive GLP-1 half life, to COL would further enhance glycemic control. Male Zucker diabetic fatty (ZDF) rats were assigned to four groups: diabetic model without treatment (the model), the model treated with 2% COL or 0...
April 15, 2012: American Journal of Physiology. Gastrointestinal and Liver Physiology
Elisabeth Schwaiger, Christoph Klaus, Veerle Matheeussen, Ulrike Baranyi, Nina Pilat, Haley Ramsey, Stephan Korom, Ingrid De Meester, Thomas Wekerle
In order to develop minimally toxic bone marrow transplantation (BMT) protocols suitable for use in a wider range of indications, it is important to identify ways to enhance BM engraftment at a given level of recipient conditioning. CXCL12/stromal cell-derived factor-1α plays a crucial physiological role in homing of hematopoietic stem cells to BM. It is regulated by the ectopeptidase dipeptidyl peptidase IV (DPPIV; DPP4) known as CD26, which cleaves dipeptides from the N-terminus of polypeptide chains. Blocking DPPIV enzymatic activity had a beneficial effect on hematopoietic stem cell engraftment in various but very specific experimental settings...
February 2012: Experimental Hematology
A J Scheen, L F Van Gaal
Sitagliptin (Januvia), the first selective inhibitor of dipeptidylpeptidase-4 with a so-called incretin effect, has been evaluated in SUGAR, a large Belgian prospective observational study carried out in general practice. Sitagliptin, at a dose of 100 mg once daily, was added to previous treatment of not well controlled type 2 diabetic patients (> 95% on metformin monotherapy). Among 605 patients analysed in intention to treat, the worse the glycaemic control at entry, the greatest the reduction in glycated haemoglobin (HbA1c) and fasting plasma glucose levels after the addition of sitagliptin (p < 0...
July 2011: Revue Médicale de Liège
Colin A Leech, Igor Dzhura, Oleg G Chepurny, Guoxin Kang, Frank Schwede, Hans-G Genieser, George G Holz
Insulin secretion from pancreatic β cells is stimulated by glucagon-like peptide-1 (GLP-1), a blood glucose-lowering hormone that is released from enteroendocrine L cells of the distal intestine after the ingestion of a meal. GLP-1 mimetics (e.g., Byetta) and GLP-1 analogs (e.g., Victoza) activate the β cell GLP-1 receptor (GLP-1R), and these compounds stimulate insulin secretion while also lowering levels of blood glucose in patients diagnosed with type 2 diabetes mellitus (T2DM). An additional option for the treatment of T2DM involves the administration of dipeptidyl peptidase-IV (DPP-IV) inhibitors (e...
November 2011: Progress in Biophysics and Molecular Biology
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