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Dpp-4 inhibitors

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https://www.readbyqxmd.com/read/29148282/macrocarpal-c-isolated-from-eucalyptus-globulus-inhibits-dipeptidyl-peptidase-4-in-an-aggregated-form
#1
Eisuke Kato, Kazuhiro Kawakami, Jun Kawabata
Dipeptidyl peptidase 4 (DPP-4) inhibitors are used for the treatment of type-2 diabetes mellitus. Various synthetic inhibitors have been developed to date, and plants containing natural DPP-4 inhibitors have also been identified. Here, 13 plant samples were tested for their DPP-4 inhibitory activity. Macrocarpals A-C were isolated from Eucalyptus globulus through activity-guided fractionation and shown to be DPP-4 inhibitors. Of these, macrocarpal C showed the highest inhibitory activity, demonstrating an inhibition curve characterised by a pronounced increase in activity within a narrow concentration range...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29146035/renal-outcomes-with-dipeptidyl-peptidase-4-inhibitors
#2
REVIEW
A J Scheen, P Delanaye
Dipeptidyl peptidase-4 inhibitors (DPP-4is) are increasingly being used in the management of type 2 diabetes (T2D). The present review summarizes the current knowledge of the effects of DPP-4is on renal outcomes by analyzing the experimental preclinical data, the effects of DPP-4is on urinary albumin-creatinine ratios (UACRs) and estimated glomerular filtration rates (eGFRs) from observational studies and clinical trials, and renal events (including kidney failure requiring renal replacement therapy) in recent large prospective cardiovascular outcome trials...
November 13, 2017: Diabetes & Metabolism
https://www.readbyqxmd.com/read/29132091/effect-of-anti-diabetic-drugs-on-bone-metabolism-evidence-from-preclinical-and-clinical-studies
#3
REVIEW
Mohammad Adil, Rashid Ali Khan, Abul Kalam, Shiva Kumar Venkata, Amit Dattatraya Kandhare, Pinaki Ghosh, Manju Sharma
Diabetes mellitus is associated with abnormal bone health and an increased risk of fracture even though patients have normal or higher BMD. The mechanisms behind diabetes mellitus- induced various skeletal disorders remain unclear. Anti-diabetic drugs may have negative or positive impact on bone metabolism. For instance, thiazolidinediones increases the bone loss and risk of fracture possibly through PPARγ activation in bone marrow cells and hamper osteoblastogenesis via decreasing Runx2 transcription factor, IGF-1 and Wnt signalling pathways...
May 25, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29113797/caveolin-1-a-binding-protein-of-cd26-is-essential-for-the-anti-inflammatory-effects-of-dipeptidyl-peptidase-4-inhibitors-on-human-and-mouse-macrophages
#4
Munenori Hiromura, Kyoko Nohtomi, Yusaku Mori, Hideo Kataoka, Marika Sugano, Kei Ohnuma, Hirotaka Kuwata, Tsutomu Hirano
We previously reported that inhibition of dipeptidyl peptidase (DPP)-4, the catalytic site of CD26, prevents atherosclerosis in animal models through suppression of inflammation; however, the underlying molecular mechanisms have not been fully elucidated. Caveolin-1 (Cav-1), a major structural protein of caveolae located on the surface of the cellular membrane, has been reported to modulate inflammatory responses by binding to CD26 in T cells. In this study, we investigated the role of Cav-1 in the suppression of inflammation mediated by the DPP-4 inhibitor, teneligliptin, using mouse and human macrophages...
November 4, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29113790/the-persistent-inhibitory-properties-of-saxagliptin-on-renal-dipeptidyl-peptidase-4-studies-with-hk-2-cells-in%C3%A2-vitro-and-normal-rats-in%C3%A2-vivo
#5
Masako Uchii, Mariko Sakai, Yuhei Hotta, Satoshi Saeki, Naoya Kimoto, Akinori Hamaguchi, Tetsuya Kitayama, Shunji Kunori
Saxagliptin, a potent and selective DPP-4 inhibitor, exhibits a slow dissociation from DPP-4. We investigated the sustained effects of saxagliptin on renal DPP-4 activity in a washout study using renal tubular (HK-2) cells, and in a pharmacodynamic study using normal rats. In HK-2 cells, the inhibitory potency of saxagliptin on DPP-4 activity persisted after washout, while that of sitagliptin was clearly reduced. In normal rats, a single treatment of saxagliptin or sitagliptin inhibited the plasma DPP-4 activity to similar levels...
October 23, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29110647/a-randomized-placebo-controlled-clinical-trial-evaluating-the-safety-and-efficacy-of-the-once-weekly-dpp-4-inhibitor-omarigliptin-in-patients-with-type-2-diabetes-mellitus-inadequately-controlled-by-glimepiride-and-metformin
#6
Seung-Hwan Lee, Ira Gantz, Elizabeth Round, Melanie Latham, Edward A O'Neill, Paulette Ceesay, Shailaja Suryawanshi, Keith D Kaufman, Samuel S Engel, Eseng Lai
BACKGROUND: Type 2 diabetes (T2D) is a progressive disease that often requires a patient to use multiple antihyperglycemic agents to achieve glycemic control with disease progression. Omarigliptin is a once-weekly dipeptidyl peptidase-4 inhibitor. The purpose of this trial was to assess the efficacy and safety of adding omarigliptin to the treatment regimen of patients with T2D inadequately controlled by dual therapy with metformin and glimepiride. METHODS: Patients with T2D and HbA1c ≥7...
November 6, 2017: BMC Endocrine Disorders
https://www.readbyqxmd.com/read/29109662/budget-impact-of-introducing-linagliptin-into-bosnia-and-herzegovina-health-insurance-drug-reimbursement-list-in-2016-2018
#7
Tarik Catic, Lana Lekic, Vlad Zah, Vedad Tabakovic
Introduction: Diabetes is reaching epidemiological scales worldwide. Beside health implications diabetes bears significant financial impact on health systems. Different treatment options aiming to prevent diabetes complications are available. Dipeptidyl-peptidase-IV (DPP-4) inhibitors like linagliptin are usually add-on therapy to metformin in order to achieve glycemic control. Expenditure for oral antidiabetic medicines in Bosnia and Herzegovina (B&H) is low accounting for only 2.53% of the total drug market expenditure...
September 2017: Materia Socio-medica
https://www.readbyqxmd.com/read/29109299/long-term-trends-in-antidiabetes-drug-usage-in-the-u-s-real-world-evidence-in-patients-newly-diagnosed-with-type-2-diabetes
#8
Olga Montvida, Jonathan Shaw, John J Atherton, Frances Stringer, Sanjoy K Paul
OJBECTIVE: To explore temporal trends in antidiabetes drug (ADD) prescribing and intensification patterns, along with glycemic levels and comorbidities, and possible benefits of novel ADDs in delaying the need for insulin initiation in patients diagnosed with type 2 diabetes. RESEARCH DESIGN AND METHODS: Patients with type 2 diabetes aged 18-80 years, who initiated any ADD, were selected (n = 1,023,340) from the U.S. Centricity Electronic Medical Records. Those who initiated second-line ADD after first-line metformin were identified (subcohort 1, n = 357,482); the third-line therapy choices were further explored...
November 6, 2017: Diabetes Care
https://www.readbyqxmd.com/read/29096096/discovery-of-triazole-based-uracil-derivatives-bearing-amide-moieties-as-novel-dipeptidyl-peptidase-iv-inhibitors
#9
Xiaoyan Deng, Li Han, Jinpei Zhou, Huibin Zhang, Qing Li
Dipeptidyl peptidase-IV (DPP-4) is a validated target for T2DM treatment. We previously reported a novel series of triazole-based uracil derivatives bearing aliphatic carboxylic acids with potent DPP-4 inhibitory activities in vitro, but these compounds showed poor hypoglycemic effects in vivo. Herein we further optimized the triazole moiety by amidation of the carboxylic acid to improve in vivo activities. Two series of compounds 3a-f and 4a-g were designed and synthesized. By screening in DPP-4, compound 4c was identified as a potent DPP-4 inhibitor with the IC50 value of 28...
October 23, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29095893/crystal-structure-of-dipeptidyl-peptidase-iii-from-the-human-gut-symbiont-bacteroides-thetaiotaomicron
#10
Igor Sabljić, Nevenka Meštrović, Bojana Vukelić, Peter Macheroux, Karl Gruber, Marija Luić, Marija Abramić
Bacteroides thetaiotaomicron is a dominant member of the human intestinal microbiome. The genome of this anaerobe encodes more than 100 proteolytic enzymes, the majority of which have not been characterized. In the present study, we have produced and purified recombinant dipeptidyl peptidase III (DPP III) from B. thetaiotaomicron for the purposes of biochemical and structural investigations. DPP III is a cytosolic zinc-metallopeptidase of the M49 family, involved in protein metabolism. The biochemical results for B...
2017: PloS One
https://www.readbyqxmd.com/read/29093280/satisfaction-and-efficacy-of-switching-from-daily-dipeptidyl-peptidase-4-inhibitors-to-weekly-trelagliptin-in-patients-with-type-2-diabetes-randomized-controlled-study
#11
Mayuko Oita, Hideaki Miyoshi, Kota Ono, Akinobu Nakamura, Kyu Yong Cho, Hiroshi Nomoto, Kohei Yamamoto, Kazuno Omori, Naoki Manda, Yoshio Kurihara, Shin Aoki, Tatsuya Atsumi
We compared treatment satisfaction between daily dipeptidyl peptidase-4 (DPP-4) inhibitors and a weekly DPP-4 inhibitor in patients with type 2 diabetes. The study was a 12-week, open-label, randomized, multicenter, controlled trial. Participants were Japanese patients with type 2 diabetes who had received daily DPP-4 inhibitors for more than 3 months. Patients were randomly assigned to a treatment cohort: (1) a group that continued taking daily DPP-4 inhibitors (daily group); or (2) a group that switched from daily DPP-4 inhibitors to a weekly DPP-4 inhibitor, trelagliptin (weekly group)...
October 31, 2017: Endocrine Journal
https://www.readbyqxmd.com/read/29078995/rapid-generation-of-a-novel-dpp-4-inhibitor-with-long-acting-properties-sar-study-and-pk-pd-evaluation
#12
Hui Xie, Shaogao Zeng, Yuwen He, Guicheng Zhang, Pengjiu Yu, Guifa Zhong, Hongjiang Xu, Ling Yang, Shanchun Wang, Xin Zhao, Wenhui Hu
Drug compliance is critical for patients with chronic diseases such as diabetes. In our continuous effort to find better glucose-lowering agents, an exploration for long-acting DPP-4 inhibitors had been launched. Based on our previously reported compounds bearing a pyrrolopyrimidine scaffold, the lead compound 4a (IC50 = 2.3 nM, t1/2(rat) = 5.46 h) with pharmacokinetic superiority was rapidly determined. Further SAR study indicated that the pyrrole ring was generally tolerable for variation, in which a β-substitution gave a better DPP-4 affinity...
December 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29076039/effect-of-trelagliptin-on-quality-of-life-in-patients-with-type-2-diabetes-mellitus-study-protocol
#13
Hitoshi Ishii, Yuki Suzaki, Yuko Miyata
INTRODUCTION: Long-term glycemic control in type 2 diabetes is critical to prevent or delay the onset of macrovascular and microvascular complications. Medication adherence is an integral component of type 2 diabetes management. Minimizing the dosing frequency of antidiabetic drugs may reduce treatment burden for patients and improve medication adherence. This study has been proposed to assess the reduction in treatment burden during 12 weeks' administration of trelagliptin, a weekly dosing dipeptidyl peptidase-4 (DPP-4) inhibitor, compared with a daily dosing DPP-4 inhibitor in patients with type 2 diabetes...
October 26, 2017: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
https://www.readbyqxmd.com/read/29074013/newer-classes-of-antidiabetes-drugs-ophthalmological-considerations-for-glp-1r-agonists-dpp-4-inhibitors-and-sglt-2-inhibitors
#14
EDITORIAL
Kylen D McReelis, Julie A Lovshin
No abstract text is available yet for this article.
November 2017: Canadian Journal of Ophthalmology. Journal Canadien D'ophtalmologie
https://www.readbyqxmd.com/read/29068991/the-prescribing-trend-of-oral-antidiabetic-agents-for-type-2-diabetes-in-taiwan-an-8-year-population-based-study
#15
Wei-Min Chu, Hsin-En Ho, Kuang-Hua Huang, Yu-Tse Tsan, Yi-Sheng Liou, Yueh-Hsin Wang, Meng-Chih Lee, Yu-Ching Li
The purpose of this study was to evaluate the prescription trend and pattern of oral antidiabetic (OAD) medications, which are extensively used worldwide for treating type 2 diabetes, in 2 age groups.In this population-based study, data obtained from the National Health Insurance Research Database, Taiwan, were analyzed to investigate the prescription trend of all types of OAD medications during 2005 to 2012. We used descriptive statistics to demonstrate the trend of prescription patterns stratified by age (aged 65 years and above or younger than 65)...
October 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29066384/development-of-a-validated-hplc-method-for-the-quantitative-determination-of-trelagliptin-succinate-and-its-related-substances-in-pharmaceutical-dosage-forms
#16
Zhiqiang Luo, Xinjing Chen, Guopeng Wang, Zhibo Du, Xiaoyun Ma, Hao Wang, Guohua Yu, Aoxue Liu, Mengwei Li, Wei Peng, Yang Liu
Trelagliptin succinate is a dipeptidyl peptidase IV (DPP-4) inhibitor which is used as a new long-acting drug for once-weekly treatment of type 2 diabetes mellitus (DM). In the present study, a rapid, sensitive and accurate high-performance liquid chromatography (HPLC) method was developed and validated for separation and determination of trelagliptin succinate and its eight potential process-related impurities. The chromatographic separation was achieved on a Waters Xselect CSH™ C18 (250mm×4.6mm, 5.0μm) column...
October 21, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29064743/dipeptidyl-peptidase-4-inhibitor-sitagliptin-prevented-weight-regain-in-obese-women-with-polycystic-ovary-syndrome-previously-treated-with-liraglutide-a-pilot-randomized-study
#17
Simona Ferjan, Andrej Janez, Mojca Jensterle
BACKGROUND: Weight loss is often nonsustainable after liraglutide cessation. The present study is the first insight into the potential prevention of weight regain in obese subjects who have been withdrawn from liraglutide. We evaluated whether dipeptidyl peptidase-4 (DPP-4) inhibitor sitagliptin in adjunct to metformin prevents body weight regain more effectively than metformin alone in obese polycystic ovary syndrome (PCOS) previously treated with liraglutide. METHODS: A 12-week prospective randomized open-label study was conducted with 24 obese women with PCOS who had been pretreated with liraglutide 3...
October 24, 2017: Metabolic Syndrome and related Disorders
https://www.readbyqxmd.com/read/29058840/-use-of-oral-glucose-lowering-agents-in-patients-with-renal-impairment
#18
A J Scheen, N Paquot
Patients with type 2 diabetes (T2D) and chronic kidney disease (CKD) are increasingly numerous, especially in the elderly population. Surprisingly, this situation is often under-recognized or even neglected in clinical practice. Yet, most oral antidiabetic (OAD) agents have limitations in case of renal impairment, either because they require a dose reduction, or are contra-indicated mainly for safety reasons. This clinical case gives the opportunity to discuss the modalities of prescription and cautions to be taken when using most commonly prescribed OAD, metformin, insulin secretagogues (sulfonylureas, repaglinide), DPP-4 inhibitors (gliptins) and SGLT2 inhibitors, in a patient with T2D and CKD...
October 2017: Revue Médicale de Liège
https://www.readbyqxmd.com/read/29055144/increased-prevalence-of-diabetes-mellitus-in-bullous-pemphigoid-patients-during-the-last-decade
#19
Luca Fania, Giovanni Di Zenzo, Biagio Didona, Maria Antonietta Pilla, Luciano Sobrino, Annarita Panebianco, Cinzia Mazzanti, Damiano Abeni
Bullous pemphigoid (BP) is a rare autoimmune blistering disease. The association between BP and diabetes mellitus (DM) has been previously reported with inconsistent results(1-4) . Dipeptidyl peptidase (DPP)-IV inhibitors, approved in Europe by EMA in 2007 to treat type-2 DM, are antihyperglycemic drugs that could induce BP disease(5-9) . This article is protected by copyright. All rights reserved.
October 21, 2017: Journal of the European Academy of Dermatology and Venereology: JEADV
https://www.readbyqxmd.com/read/29053207/dpp-4-inhibitors-moderate-the-risk-of-genitourinary-tract-infections-associated-with-sglt2-inhibitors
#20
Gian Paolo Fadini, Benedetta Maria Bonora, Mayur Sarangdhar, Mauro Rigato, Angelo Avogaro
Genito-urinary tract infections (GUTI) are the most common adverse event (AE) during therapy with sodium-glucose cotransporter 2 inhibitors (SGLT2i). We evaluated whether dipeptidyl peptidase 4 inhibitors (DPP4i) moderate the risk of GUTI during therapy with SGLT2i, using two approaches. First, we screened the literature for randomized controlled trials (RCTs) directly comparing the frequency of GUTI in patients receiving a DPP4i/SGLT2i combination therapy versus those receiving a SGLT2i only. In the 5 trials we retrieved, the pooled RR for genital tract infections (GTI) in patients on a DPP4i/SGLT2i combination therapy versus those on SGLT2i alone was 0...
October 20, 2017: Diabetes, Obesity & Metabolism
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