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Linagliptin

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https://www.readbyqxmd.com/read/29045658/exendin-4-a-glucagon-like-peptide-1-receptor-agonist-attenuates-breast-cancer-growth-by-inhibiting-nf-%C3%AE%C2%BAb-activation
#1
Chikayo Iwaya, Takashi Nomiyama, Shiho Komatsu, Takako Kawanami, Yoko Tsutsumi, Yuriko Hamaguchi, Tsuyoshi Horikawa, Yasuteru Yoshinaga, Shinichi Yamashita, Tomoko Tanaka, Yuichi Terawaki, Makito Tanabe, Kazuki Nabeshima, Akinori Iwasaki, Toshihiko Yanase
Incretin therapies have received significant attention because of their tissue-protective effects, which extend beyond those associated with glycemic control. Cancer is a primary cause of death in patients with diabetes mellitus. We previously reported anti-prostate cancer effects of the glucagon-like peptide-1 (GLP-1) receptor (GLP-1R) agonist exendin-4 (Ex-4). Breast cancer is one of the most common cancers in female patients with type 2 diabetes mellitus and obesity. Thus, we examined whether GLP-1 action could attenuate breast cancer...
October 13, 2017: Endocrinology
https://www.readbyqxmd.com/read/29037205/vildagliptin-ameliorates-pulmonary-fibrosis-in-lipopolysaccharide-induced-lung-injury-by-inhibiting-endothelial-to-mesenchymal-transition
#2
Toshio Suzuki, Yuji Tada, Santhi Gladson, Rintaro Nishimura, Iwao Shimomura, Satoshi Karasawa, Koichiro Tatsumi, James West
BACKGROUND: Pulmonary fibrosis is a late manifestation of acute respiratory distress syndrome (ARDS). Sepsis is a major cause of ARDS, and its pathogenesis includes endotoxin-induced vascular injury. Recently, endothelial-to-mesenchymal transition (EndMT) was shown to play an important role in pulmonary fibrosis. On the other hand, dipeptidyl peptidase (DPP)-4 was reported to improve vascular dysfunction in an experimental sepsis model, although whether DPP-4 affects EndMT and fibrosis initiation during lipopolysaccharide (LPS)-induced lung injury is unclear...
October 16, 2017: Respiratory Research
https://www.readbyqxmd.com/read/28943546/diabetic-hemichorea-hemiballism-after-prompt-improvement-in-hyperglycemia
#3
Masayuki Kitagawa, Yoshihiro Yamanaka, Toru Adachi, Junitsu Ito, Kazutoshi Fukase, Ikuro Ohta, Tadashi Katagiri
We herein report a case of hemichorea-hemiballism in an 85-year-old man diagnosed with diabetes at 76 years of age. After a one-year interruption in treatment, he was treated with a low-calorie diet, linagliptin, and nateglinide. Over 51 days, his HbA1c level decreased from 15.8% to 7.7%. After a prompt improvement in his hyperglycemia, he began experiencing involuntary movements in the right upper and lower extremities. T1-weighted magnetic resonance imaging showed a high signal intensity in the left lens nucleus...
September 25, 2017: Internal Medicine
https://www.readbyqxmd.com/read/28934557/a-safety-evaluation-of-empagliflozin-plus-linagliptin-for-treating-type-2-diabetes
#4
Baptist Gallwitz
Dipeptidyl-peptidase-IV inhibitors (DPP-4i) and sodium-glucose-transporter-2 inhibitors (SGLT-2i) are oral antidiabetic drugs that improve glycemic parameters and possess a very low intrinsic hypoglycemia risk and favorable cardiovascular data. Areas covered: An overview on the clinical studies investigating the combination therapy with the DPP-4i linagliptin and the SGLT-2i empagliflozin is given. The clinical evidence for the efficacy and safety of free combinations as well as for their fixed dose combinations is presented...
October 11, 2017: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/28932239/computational-analysis-of-gynura-bicolor-bioactive-compounds-as-dipeptidyl-peptidase-iv-inhibitor
#5
Lina Rozano, Muhammad Redha Abdullah Zawawi, Muhamad Aizuddin Ahmad, Indu Bala Jaganath
The inhibition of dipeptidyl peptidase-IV (DPPIV) is a popular route for the treatment of type-2 diabetes. Commercially available gliptin-based drugs such as sitagliptin, anagliptin, linagliptin, saxagliptin, and alogliptin were specifically developed as DPPIV inhibitors for diabetic patients. The use of Gynura bicolor in treating diabetes had been reported in various in vitro experiments. However, an understanding of the inhibitory actions of G. bicolor bioactive compounds on DPPIV is still lacking and this may provide crucial information for the development of more potent and natural sources of DPPIV inhibitors...
2017: Advances in Bioinformatics
https://www.readbyqxmd.com/read/28921919/oral-glucose-lowering-with-linagliptin-and-metformin-compared-with-linagliptin-alone-as-initial-treatment-in-asian-patients-with-newly-diagnosed-type-2-diabetes-and-marked-hyperglycemia-subgroup-analysis-of-a-randomized-clinical-trial
#6
Ronald Cw Ma, Stefano Del Prato, Baptist Gallwitz, Vyankatesh K Shivane, Diane Lewis-D'Agostino, Zelie Bailes, Sanjay Patel, Jisoo Lee, Maximilian von Eynatten, Maximiliano Di Domenico, Stuart A Ross
AIMS/INTRODUCTION: Type 2 diabetes mellitus (T2DM) is an epidemic in Asia, yet clinical trials of glucose-lowering therapies often enrol predominantly Western populations. We explored the initial combination of metformin and linagliptin, a dipeptidyl peptidase-4 inhibitor, in newly diagnosed T2DM patients in Asia with marked hyperglycemia. MATERIALS AND METHODS: This was a post-hoc subgroup analysis of a multinational, parallel-group clinical trial in which 316 newly diagnosed T2DM patients with glycated hemoglobin A1c (HbA1c) 8...
September 16, 2017: Journal of Diabetes Investigation
https://www.readbyqxmd.com/read/28899989/dipeptidyl-peptidase-4-inhibitors-and-risk-of-heart-failure-in-patients-with-type-2-diabetes-mellitus-a-population-based-cohort-study
#7
COMPARATIVE STUDY
Young-Gun Kim, Dukyong Yoon, Sooyoung Park, Seung Jin Han, Dae Jung Kim, Kwan-Woo Lee, Rae Woong Park, Hae Jin Kim
BACKGROUND: The association between dipeptidyl-peptidase IV inhibitors (DPP-4i) and heart failure (HF) remains unclear. In 1 randomized controlled trial and some observational studies, DPP-4i reportedly increased the risk of HF, but 2 other randomized controlled trials and observational studies have shown no such risk. Here, we evaluated the risk of HF and cardiovascular outcomes of DPP-4i compared with sulfonylureas. METHODS AND RESULTS: A population-based retrospective cohort study was conducted using the Korean Health Insurance Review and Assessment Service database from January 1, 2009, to December 31, 2015...
September 2017: Circulation. Heart Failure
https://www.readbyqxmd.com/read/28827024/gastrointestinal-adverse-events-of-dipeptidyl-peptidase-4-inhibitors-in-type-2-diabetes-a-systematic-review-and-network-meta-analysis
#8
Shanshan Wu, Sanbao Chai, Jun Yang, Ting Cai, Yang Xu, Zhirong Yang, Yuan Zhang, Linong Ji, Feng Sun, Siyan Zhan
PURPOSE: The purpose of this study was to systematically evaluate the effect of dipeptidyl peptidase 4 inhibitors on gastrointestinal adverse events in patients with type 2 diabetes. METHODS: MEDLINE, Embase, the Cochrane Library, and ClinicalTrials.gov were searched from inception through April 28, 2016. Randomized controlled trials that compared dipeptidyl peptidase 4 inhibitor-based therapies with placebo and other hypoglycemic agents in type 2 diabetes were included...
August 18, 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/28819835/efficacy-and-safety-of-linagliptin-in-2681-asian-patients-stratified-by-age-obesity-and-renal-function-a-pooled-analysis-of-randomized-clinical-trials
#9
Guang Ning, Tushar Bandgar, Uwe Hehnke, Jisoo Lee, Juliana C N Chan
INTRODUCTION: Asian patients with type 2 diabetes (T2D) are younger, leaner, and more likely to develop renal dysfunction than White populations. In this multiethnic analysis of data from phase 3 trials, we investigated the efficacy and safety of the dipeptidyl peptidase-4 inhibitor linagliptin in Asians stratified by these subphenotypes. METHODS: Data from randomized, double-blind, placebo-controlled trials evaluating linagliptin (as monotherapy, add-on therapy to metformin ± sulfonylurea, combined with pioglitazone or added to insulin) were pooled with efficacy data from 11 randomized trials of at least 24 weeks and safety data from 15 trials of various durations...
August 17, 2017: Advances in Therapy
https://www.readbyqxmd.com/read/28801559/differential-effects-of-linagliptin-on-the-function-of-human-islets-isolated-from-non-diabetic-and-diabetic-donors
#10
Yanqing Zhang, Meifen Wu, Wynn Htun, Emily W Dong, Franck Mauvais-Jarvis, Vivian A Fonseca, Hongju Wu
Linagliptin is a dipeptidyl Peptidase-4 (DPP-4) inhibitor that inhibits the degradation of glucagon-like peptide 1 (GLP-1), and has been approved for the treatment of type 2 diabetes (T2D) in clinic. Previous studies have shown linagliptin improves β cell function using animal models and isolated islets from normal subjects. Since β cell dysfunction occurs during diabetes development, it was not clear how human islets of T2D patients would respond to linagliptin treatment. Therefore, in this study we employed human islets isolated from donors with and without T2D and evaluated how they responded to linagliptin treatment...
August 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28771625/inhibition-of-dipeptidyl-peptidase-4-ameliorates-cardiac-ischemia-and-systolic-dysfunction-by-up-regulating-the-fgf-2-egr-1-pathway
#11
Masayoshi Suda, Ippei Shimizu, Yohko Yoshida, Yuka Hayashi, Ryutaro Ikegami, Goro Katsuumi, Takayuki Wakasugi, Yutaka Yoshida, Shujiro Okuda, Tomoyoshi Soga, Tohru Minamino
Dipeptidyl peptidase 4 inhibitors are used worldwide in the management of diabetes, but their role in the prevention or treatment of cardiovascular disorders has yet to be defined. We found that linagliptin, a DPP-4 inhibitor, suppressed capillary rarefaction in the hearts of mice with dietary obesity. Metabolomic analysis performed with capillary electrophoresis/mass spectrometry (LC-MS/MS) showed that linagliptin promoted favorable metabolic remodeling in cardiac tissue, which was characterized by high levels of citrulline and creatine...
2017: PloS One
https://www.readbyqxmd.com/read/28719008/comparative-efficacy-and-safety-of-gemigliptin-versus-linagliptin-in-type-2-diabetes-patients-with-renal-impairment-a-40-week-extension-of-the-guard-randomized-study
#12
Sang Youb Han, Sun Ae Yoon, Byoung Geun Han, Sung Gyun Kim, Young-Il Jo, Kyung Hwan Jeong, Kook-Hwan Oh, Hyeong Cheon Park, Sun-Hee Park, Shin-Wook Kang, Ki-Ryang Na, Sun Woo Kang, Nam-Ho Kim, Younghwan Jang, Bogyeong Kim, Seonghye Shin, Dae Ryong Cha
AIMS: The present extension study evaluated the long-term safety and efficacy of gemigliptin during a 40-week follow-up period after a 12-week study. METHODS: The main study was a randomized, placebo-controlled, double-blinded, phase IIIb study in which 50 mg of gemigliptin (N = 66) or placebo (N = 66) was administered to patients with type 2 diabetes mellitus (T2DM) with moderate or severe renal impairment over a 12-week period. Patients with a glycated haemoglobin (HbA1c) level of 7-11% and an estimated glomerular filtration rate (eGFR) of 15-59 mL/min/1...
July 18, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28715446/active-subfractions-of-abelmoschus-esculentus-substantially-prevent-free-fatty-acid-induced-%C3%AE-cell-apoptosis-via-inhibiting-dipeptidyl-peptidase-4
#13
Chien-Ning Huang, Chau-Jong Wang, Yi-Ju Lee, Chiung-Huei Peng
Lipotoxicity plays an important role in exacerbating type 2 diabetes mellitus (T2DM) and leads to apoptosis of β cells. Recently dipeptidyl peptidase-4 (DPP-4) inhibitors have emerged as a useful tool in the treatment of T2DM. DPP-4 degrades type 1 glucagon-like peptide (GLP-1), and GLP-1 receptor (GLP-1R) signaling has been shown to protect β cells by modulating AMPK/mTOR, PI3K, and Bax. The anti-hyperglycemic effect of Abelmoschus esculentus (AE) is well known, however its mucilage makes it difficult to further examine this effect...
2017: PloS One
https://www.readbyqxmd.com/read/28701284/cost-effectiveness-analysis-of-different-dipeptidyl-peptidase-4-inhibitor-drugs-for-treatment-of-type-2-diabetes-mellitus
#14
Maurílio de Souza Cazarim, Estael Luzia Coelho da Cruz-Cazarim, André de Oliveira Baldoni, Thais Bueno Enes Dos Santos, Paula Gonçalves de Souza, Ingrid de Almeida Silva, Roberta Niriam Reis Rodrigues, Alda Cristina Franco Correa Maia, Leonardo Régis Leira Pereira, Cristina Sanches
INTRODUCTION: Type 2 diabetes mellitus (T2DM) has burdened health systems in the world to the value of 500 billion dollars/year. Dipeptidyl peptidase 4 inhibitors (DPP-4 Inhibitors) have been strongly associated with spending on the treatment of T2DM by the courts in Brazil. The aim of this study was to estimate the most cost-effective DPP-4 Inhibitor for T2DM treatment. A pharmacoeconomic study of cost-effectiveness was performed in a medium-sized municipality in Minas Gerais state, Brazil...
July 3, 2017: Diabetes & Metabolic Syndrome
https://www.readbyqxmd.com/read/28683709/-linagliptin-induced-liver-toxicity
#15
Emma Bartolomé-García, Sira Sanz-Márquez, Montserrat Pérez-Encinas
No abstract text is available yet for this article.
July 1, 2017: Farmacia Hospitalaria
https://www.readbyqxmd.com/read/28671793/-gliptin-gliflozin-combination-for-treating-type-2-diabetes
#16
André J Scheen, Nicolas Paquot
Type 2 diabetes (T2D) is a complex disease with multiple defects, which generally require a combination of several pharmacological approaches to control hyperglycaemia. Combining a dipeptidyl peptidase-4 inhibitor (DPP-4i) and a sodium-glucose cotransporter type 2 inhibitor (SGT2i) appears to be an attractive approach because the two drugs exert different and potentially complementary glucose-lowering effects. Dual therapy (initial combination or stepwise approach) is more potent than either monotherapy in patients treated with diet and exercise or already treated with metformin...
August 24, 2016: Revue Médicale Suisse
https://www.readbyqxmd.com/read/28659588/the-dual-dpp4-inhibitor-and-gpr119-agonist-hbk001-regulates-glycemic-control-and-beta-cell-function-ex-and-in-vivo
#17
Yi Huan, Qian Jiang, Gang Li, Guoliang Bai, Tian Zhou, Shuainan Liu, Caina Li, Quan Liu, Sujuan Sun, Miaomiao Yang, Nan Guo, Xing Wang, Shusen Wang, Yaojuan Liu, Guanqiao Wang, Haihong Huang, Zhufang Shen
Glucagon like peptide-1 (GLP-1) plays a vital role in glucose homeostasis and sustaining β-cell function. Currently there are two major methods to enhance endogenous GLP-1 activity; inhibiting dipeptidyl peptidase-4 (DPP4) or activating G protein-coupled receptor 119 (GPR119). Here we describe and validate a novel dual-target compound, HBK001, which can both inhibit DPP4 and activate GPR119 ex and in vivo. We show that HBK001 can promote glucose-stimulated insulin secretion in mouse and human primary islets...
June 28, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28653975/development-of-rp-hplc-stability-indicating-method-for-degradation-products-of-linagliptin-in-presence-of-metformin-hcl-by-applying-2-level-factorial-design-and-identification-of-impurity-vii-viii-and-ix-and-synthesis-of-impurity-vii
#18
Sushant B Jadhav, P Sunil Reddy, Kalyanaraman L Narayanan, Popatrao N Bhosale
The novel reverse phase-high performance liquid chromatography (RP-HPLC), stability indicating method was developed for determination of linagliptin (LGP) and its related substances in linagliptin and metformin HCl (MET HCl) tablets by implementing design of experiment to understand the critical method parameters and their relation with critical method attributes; to ensure robustness of the method. The separation of nine specified impurities was achieved with a Zorbax SB-Aq 250 × 4.6 mm, 5 µm column, using gradient elution and a detector wavelength of 225 nm, and validated in accordance with International Conference on Harmonization (ICH) guidelines and found to be accurate, precise, reproducible, robust, and specific...
June 27, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28636754/linagliptin-and-its-effects-on-hyperglycaemia-and-albuminuria-in-patients-with-type-2-diabetes-and-renal-dysfunction-the-randomized-marlina-t2d-trial
#19
Per-Henrik Groop, Mark E Cooper, Vlado Perkovic, Berthold Hocher, Keizo Kanasaki, Masakazu Haneda, Guntram Schernthaner, Kumar Sharma, Robert C Stanton, Robert Toto, Jessica Cescutti, Maud Gordat, Thomas Meinicke, Audrey Koitka-Weber, Sandra Thiemann, Maximilian von Eynatten
AIMS: The MARLINA-T2D study (ClinicalTrials.gov, NCT01792518) was designed to investigate the glycaemic and renal effects of linagliptin added to standard-of-care in individuals with type 2 diabetes and albuminuria. METHODS: A total of 360 individuals with type 2 diabetes, HbA1c 6.5% to 10.0% (48-86 mmol/mol), estimated glomerular filtration rate (eGFR) ≥30 mL/min/1.73 m(2) and urinary albumin-to-creatinine ratio (UACR) 30-3000 mg/g despite single agent renin-angiotensin-system blockade were randomized to double-blind linagliptin (n = 182) or placebo (n = 178) for 24 weeks...
June 21, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28635331/network-meta-analysis-of-liraglutide-versus-dipeptidyl-peptidase-4-inhibitors-for-the-treatment-of-type-2-diabetes-in-japanese-patients
#20
Dieter Ayers, Steve Kanters, Rachel Goldgrub, Monica Hughes, Ryo Kato, Nana Kragh
AIMS: To determine the comparative efficacy and safety of liraglutide and dipeptidyl peptidase-4 (DPP-4) inhibitors as antidiabetics for Japanese patients with uncontrolled type 2 diabetes (T2DM). METHODS AND MATERIALS: We searched for randomized controlled trials (RCTs) evaluating outcomes among Japanese adults with uncontrolled T2DM and including liraglutide or DPP-4 inhibitors up to August 2016. We extracted data on trial and patient characteristics, and the following outcomes: HbA1c, weight, patients meeting HbA1c <7%, patients experiencing hypoglycemic events, microalbuminuria, estimated glomerular filtration rate (eGFR) and creatinine...
September 2017: Current Medical Research and Opinion
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