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sitagliptin cancer

M B Rehman, B V Tudrej, J Soustre, M Buisson, P Archambault, D Pouchain, H Vaillant-Roussel, F Gueyffier, J-L Faillie, M-C Perault-Pochat, C Cornu, R Boussageon
BACKGROUND: Guidelines for type 2 diabetes (T2D) recommend reducing HbA1c through lifestyle interventions and glucose-lowering drugs (metformin, then combination with dipeptidyl peptidase-4 inhibitors [DPP-4Is] among other glucose-lowering drugs). However, no double-blind randomized clinical trial (RCT) compared with placebo has so far demonstrated that DDP-4Is reduce micro- and macrovascular complications in T2D. Moreover, the safety of DPP-4Is (with increased heart failure and acute pancreatitis) remains controversial...
October 10, 2016: Diabetes & Metabolism
Chin-Hsiao Tseng
This retrospective cohort study evaluated the risk of prostate cancer associated with sitagliptin use in Taiwanese male patients with type 2 diabetes mellitus by using the reimbursement databases of the National Health Insurance. Male patients with newly diagnosed type 2 diabetes mellitus at an age ≥25 years between 1999 and 2010 were recruited. A total of 37,924 ever users of sitagliptin and 426,276 never users were followed until December 31, 2011. The treatment effect of sitagliptin (for ever versus never users, and for tertiles of cumulative duration of therapy) was estimated by Cox regression incorporated with the inverse probability of treatment weighting using propensity score...
September 20, 2016: Oncotarget
John B Buse, M Angelyn Bethel, Jennifer B Green, Susanna R Stevens, Yuliya Lokhnygina, Pablo Aschner, Carlos Raffo Grado, Tsvetalina Tankova, Julio Wainstein, Robert Josse, John M Lachin, Samuel S Engel, Keyur Patel, Eric D Peterson, Rury R Holman
OBJECTIVE: We evaluated the incidence of acute pancreatitis and pancreatic cancer in patients with type 2 diabetes and cardiovascular disease who were treated with sitagliptin, a dipeptidyl peptidase-4 inhibitor (DPP-4i). RESEARCH DESIGN AND METHODS: In the Trial Evaluating Cardiovascular Outcomes with Sitagliptin (TECOS), a cardiovascular safety study of sitagliptin, all suspected cases of acute pancreatitis and pancreatic cancer were collected prospectively for 14,671 participants during a median follow-up time of 3 years, and were adjudicated blindly...
September 14, 2016: Diabetes Care
Hui Wang, Xiufei Liu, Min Long, Yi Huang, Linlin Zhang, Rui Zhang, Yi Zheng, Xiaoyu Liao, Yuren Wang, Qian Liao, Wenjie Li, Zili Tang, Qiang Tong, Xiaocui Wang, Fang Fang, Montserrat Rojo de la Vega, Qin Ouyang, Donna D Zhang, Shicang Yu, Hongting Zheng
Cancer is a common comorbidity of diabetic patients; however, little is known about the effects that antidiabetic drugs have on tumors. We discovered that common classes of drugs used in type 2 diabetes mellitus, the hypoglycemic dipeptidyl peptidase-4 inhibitors (DPP-4i) saxagliptin and sitagliptin, as well as the antineuropathic α-lipoic acid (ALA), do not increase tumor incidence but increase the risk of metastasis of existing tumors. Specifically, these drugs induce prolonged activation of the nuclear factor E2-related factor 2 (NRF2)-mediated antioxidant response through inhibition of KEAP1-C151-dependent ubiquitination and subsequent degradation of NRF2, resulting in up-regulated expression of metastasis-associated proteins, increased cancer cell migration, and promotion of metastasis in xenograft mouse models...
April 13, 2016: Science Translational Medicine
Aneta Rogalska, Agnieszka Sliwinska, Jacek Kasznicki, Jozef Drzewoski, Agnieszka Marczak
Type 2 diabetes mellitus patients are at increased risk of many forms of malignancies, especially of the pancreas, colon and hepatocellular cancer. Unfortunately, little is known of the possible interaction between antidiabetic drugs and anticancer agents. The present study investigates the influence of metformin (MET) and sitagliptin (SITA) on the in vitro anticancer activity of the microtubule depolymerization inhibitor agent epothilone A (EpoA). Hepatocellular liver carcinoma cell line (HepG2) viability and apoptosis were determined by the MTT test and by double staining with PO-PRO-1 and 7-aminoactinomycin D, respectively, after treatment with EpoA, metformin or sitagliptin...
2016: Asian Pacific Journal of Cancer Prevention: APJCP
Chin-Hsiao Tseng
Whether sitagliptin may increase thyroid cancer risk has not been investigated in the Asian populations. This study evaluated the association in Taiwanese patients with newly diagnosed type 2 diabetes from 1999 to 2008 by using the reimbursement database of the National Health Insurance. They should have been followed for at least 6 months after March 1, 2009, the date when sitagliptin was approved for reimbursement. Patients newly treated with sitagliptin (n=58238, "ever users of sitagliptin") or other antidiabetic drugs (n =312853, "never users of sitagliptin") were followed until December 31, 2011...
April 26, 2016: Oncotarget
Mina Thabet Kelleni, Entesar Farghaly Amin, Aly Mohamed Abdelrahman
Doxorubicin (DOX) is a widely used antineoplastic drug whose efficacy is limited by its cardiotoxicity. The aim of this study was to investigate the possible protective role of the antidiabetic drugs metformin (250 mg/kg dissolved in DW p.o. for seven days) and sitagliptin (10 mg/kg dissolved in DW p.o. for seven days) in a model of DOX-induced (single dose 15 mg/kg i.p. at the fifth day) cardiotoxicity in rats. Results of our study revealed that pretreatment with metformin or sitagliptin produced significant (P < 0...
2015: Journal of Toxicology
C A Amritha, Punnagai Kumaravelu, D Darling Chellathai
INTRODUCTION: Among the oral anti-diabetic drugs, Dipeptidyl peptidase - 4(DPP-4) inhibitor is an emerging class of drugs. Inhibitors of DPP-4 enzyme like Sitagliptin and Vildagliptin have shown Anti-oxidant properties in many studies, both invivo and invitro. It has also been characterized as an apoptotic agent on pancreatic cancer cells. In the following study, Anticancer effect of DPP 4 inhibitors on colon cell lines (HT-29) using MTT assay- {3 -4, 5-dimethyl (thiazol - 2 -yl) -3, 5- dimethyl tetrazolium bromide} assay was elucidated...
December 2015: Journal of Clinical and Diagnostic Research: JCDR
Chin-Hsiao Tseng
BACKGROUND: The risk of pancreatic cancer associated with incretin-based therapies is controversial. METHODS: This study retrospectively analysed the National Health Insurance database including patients with newly diagnosed type 2 diabetes mellitus at an age ≥ 25 years between 1999 and 2010. A total of 71 137 ever users of sitagliptin and 933 046 never users were followed for pancreatic cancer until 31 December 2011. A time-dependent approach was used to calculate incidence and estimate hazard ratios adjusted for propensity score using Cox regression...
January 2016: European Journal of Clinical Investigation
H J Choi, J Y Kim, S-C Lim, G Kim, H J Yun, H S Choi
BACKGROUND AND PURPOSE: Dipeptidyl peptidase 4 (DPP4) is an aminopeptidase that is widely expressed in different cell types. Recent studies suggested that DPP4 plays an important role in tumour progression in several human malignancies. Here we have examined the mechanisms by which up-regulation of DPP4 expression causes epithelial transformation and mammary tumourigenesis. EXPERIMENTAL APPROACH: Expression of DPP4 and the peptidylprolyl cis/trans isomerase, NIMA-interacting 1 (PIN1), and the cytotoxic effects of combined treatment with sitagliptin and juglone were investigated by immunohistochemistry, immunoblotting, real-time PCR, TUNEL and soft agar assays, using MCF7 cells...
November 2015: British Journal of Pharmacology
Aline Beckenkamp, Júlia Biz Willig, Danielle Bertodo Santana, Jéssica Nascimento, Juliano Domiraci Paccez, Luiz Fernando Zerbini, Alessandra Nejar Bruno, Diogo André Pilger, Márcia Rosângela Wink, Andréia Buffon
Dipeptidyl peptidase IV (DPPIV/CD26) is a transmembrane glycoprotein that inactivates or degrades some bioactive peptides and chemokines. For this reason, it regulates cell proliferation, migration and adhesion, showing its role in cancer processes. This enzyme is found mainly anchored onto the cell membrane, although it also has a soluble form, an enzymatically active isoform. In the present study, we investigated DPPIV/CD26 activity and expression in cervical cancer cell lines (SiHa, HeLa and C33A) and non-tumorigenic HaCaT cells...
2015: PloS One
Jennifer B Green, M Angelyn Bethel, Paul W Armstrong, John B Buse, Samuel S Engel, Jyotsna Garg, Robert Josse, Keith D Kaufman, Joerg Koglin, Scott Korn, John M Lachin, Darren K McGuire, Michael J Pencina, Eberhard Standl, Peter P Stein, Shailaja Suryawanshi, Frans Van de Werf, Eric D Peterson, Rury R Holman
BACKGROUND: Data are lacking on the long-term effect on cardiovascular events of adding sitagliptin, a dipeptidyl peptidase 4 inhibitor, to usual care in patients with type 2 diabetes and cardiovascular disease. METHODS: In this randomized, double-blind study, we assigned 14,671 patients to add either sitagliptin or placebo to their existing therapy. Open-label use of antihyperglycemic therapy was encouraged as required, aimed at reaching individually appropriate glycemic targets in all patients...
July 16, 2015: New England Journal of Medicine
Agnieszka Sliwinska, Aneta Rogalska, Agnieszka Marczak, Jacek Kasznicki, Jozef Drzewoski
Metformin and sitagliptin are hypoglycemic drugs with potential use in cancer treatment. Evidence indicates that metformin may inhibit the proliferation and growth of various types of cancer cells. Data regarding the relationship between sitagliptin and cancer cells is limited. Therapy based on anthracycline derivatives, mainly doxorubicin, is commonly used in the treatment of resistant liver cancers. WP 631 is a new structural analogue of doxorubicin that exerts an anticancer action by the induction of apoptosis...
August 2015: Toxicology in Vitro: An International Journal Published in Association with BIBRA
Eva M Vivian
PURPOSE: The pharmacologic properties and clinical efficacy of dapagliflozin, a sodium-glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes, are reviewed. SUMMARY: Dapagliflozin (Farxiga, AstraZeneca) is a selective SGLT2 inhibitor approved as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. Dapagliflozin lowers blood glucose independent of insulin secretion and action by inhibiting renal reabsorption of glucose, thus promoting increased urinary excretion of glucose...
March 1, 2015: American Journal of Health-system Pharmacy: AJHP
André J Scheen
INTRODUCTION: Dipeptidyl peptidase-4 (DPP-4) inhibitors (gliptins) occupy a growing place in the armamentarium of drugs used for the management of hyperglycemia in type 2 diabetes, although some safety concerns have been raised in recent years. AREAS COVERED: An updated review providing an analysis of available safety data (meta-analyses, randomized controlled trials, observational cohort and case-control studies and pharmacovigilance reports) with five commercialized DPP-4 inhibitors (sitagliptin, vildagliptin, saxagliptin, alogliptin, linagliptin)...
April 2015: Expert Opinion on Drug Safety
Sri Harsha Tella, Marc S Rendell
INTRODUCTION: Dipeptidyl peptidase inhibitors (DPP-4-i) are highly selective inhibitors of the enzyme DPP-4. They act by increasing levels of incretin hormones, which have potent effects on insulin and glucagon release, gastric emptying, and satiety. Our goal is to review the safety issues related to DPP-4-i. AREAS COVERED: This review is based upon a PubMed search of the literature using keywords alogliptin, linagliptin, saxagliptin, sitagliptin and vildagliptin, DPP-4-i, glucagon-like polypeptide-1 agonists, as well as extensive personal clinical trial experience with each of these agents...
January 2015: Expert Opinion on Drug Safety
Youichi Sato, Takanobu Kamada, Aiko Yamauchi
In a previous study, we demonstrated that dipeptidyl peptidase 4 (DPP4)-deficient rats were susceptible to reduced glomerular filtration rate as a result of streptozotocin (STZ)-induced diabetes. Therefore, we proposed that DPP4 might be responsible for the preservation of renal function. In this study, to verify the role of DPP4 in the preservation of renal function, we performed a microarray analysis of the kidneys of WT and DPP4-deficient rats after STZ treatment, and gene expression analysis using rat kidneys, human embryonic kidney 293 (HEK293) cells, and human renal cancer cells (CakI-1)...
November 2014: Journal of Endocrinology
C Y Hsu, R S Sulake, P-K Huang, H-Y Shih, H-W Sie, Y-K Lai, C Chen, C F Weng
BACKGROUND AND PURPOSE: The fungal product (+)-antroquinonol activates AMP kinase (AMPK) activity in cancer cell lines. The present study was conducted to examine whether chemically synthesized (+)-antroquinonol exhibited beneficial metabolic effects in insulin-resistant states by activating AMPK and inhibiting dipeptidyl peptidase IV (DPP IV) activity. EXPERIMENTAL APPROACH: Effects of (+)-antroquinonol on DPP IV activity were measured with a DPPIV Assay Kit and effects on GLP-1-induced PKA were measured in AR42J cells...
January 2015: British Journal of Pharmacology
Theodosios D Filippatos, Vasilios G Athyros, Moses S Elisaf
INTRODUCTION: Dipeptidyl-peptidase-4 (DPP-4) inhibitors are a class of anti-hyperglycemic agents with proven efficacy in patients with type 2 diabetes mellitus (T2DM). AREAS COVERED: This review considers the pharmacokinetic profile, adverse effects and drug interactions of DPP-4 inhibitors. DPP-4 inhibitors have certain differences in their structure, metabolism, route of elimination and selectivity for DPP-4 over structurally related enzymes, such as DPP-8/DPP-9...
June 2014: Expert Opinion on Drug Metabolism & Toxicology
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
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