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Cediranib

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https://www.readbyqxmd.com/read/28392095/real-time-analysis-of-the-binding-of-fluorescent-vegf165a-to-vegfr2-in-living-cells-effect-of-receptor-tyrosine-kinase-inhibitors-and-fate-of-internalized-agonist-receptor-complexes
#1
Laura E Kilpatrick, Rachel Friedman-Ohana, Diana C Alcobia, Kristin Riching, Chloe J Peach, Amanda J Wheal, Stephen J Briddon, Matthew B Robers, Kris Zimmerman, Thomas Machleidt, Keith V Wood, Jeanette Woolard, Stephen J Hill
Vascular endothelial growth factor (VEGF) is an important mediator of angiogenesis. Here we have used a novel stoichiometric protein-labeling method to generate a fluorescent variant of VEGF (VEGF165a-TMR) labeled on a single cysteine within each protomer of the antiparallel VEGF homodimer. VEGF165a-TMR has then been used in conjunction with full length VEGFR2, tagged with the bioluminescent protein NanoLuc, to undertake a real time quantitative evaluation of VEGFR2 binding characteristics in living cells using bioluminescence energy transfer (BRET)...
April 6, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28382802/major-clinical-research-advances-in-gynecologic-cancer-in-2016-10-year-special-edition
#2
REVIEW
Dong Hoon Suh, Miseon Kim, Kidong Kim, Hak Jae Kim, Kyung Hun Lee, Jae Weon Kim
In 2016, 13 topics were selected as major research advances in gynecologic oncology. For ovarian cancer, study results supporting previous ones regarding surgical preventive strategies were reported. There were several targeted agents that showed comparable responses in phase III trials, including niraparib, cediranib, and nintedanib. On the contrary to our expectations, dose-dense weekly chemotherapy regimen failed to prove superior survival outcomes compared with conventional triweekly regimen. Single-agent non-platinum treatment to prolong platinum-free-interval in patients with recurrent, partially platinum-sensitive ovarian cancer did not improve and even worsened overall survival (OS)...
May 2017: Journal of Gynecologic Oncology
https://www.readbyqxmd.com/read/28360207/-18-f-fluoromisonidazole-kinetic-modeling-for-characterization-of-tumor-perfusion-and-hypoxia-in-response-to-antiangiogenic-therapy
#3
Milan Grkovski, Sally-Ann Emmas, Sean D Carlin
Multiparametric imaging of tumor perfusion and hypoxia with (18)F-fluoromisonidazole ((18)F-FMISO) dynamic positron emission tomography (dPET) may allow for an improved response assessment to antiangiogenic therapies. Cediranib (AZD2171) is a potent inhibitor of tyrosine kinase activity associated with vascular endothelial growth factor receptors-1, -2 and -3, currently in Phase II/III clinical trials. Serial (18)F-FMISO dPET was performed to investigate changes in tumor biomarkers of perfusion and hypoxia following cediranib treatment...
March 30, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28339098/quality-of-life-with-cediranib-in-relapsed-ovarian-cancer-the-icon6-phase-3-randomized-clinical-trial
#4
Dan P Stark, Adrian Cook, Julia M Brown, Michael D Brundage, Andrew C Embleton, Richard S Kaplan, Fharat A Raja, Ann Marie W Swart, Galina Velikova, Wendi Qian, Jonathan A Ledermann
BACKGROUND: The ICON6 trial showed that cediranib, an oral inhibitor of vascular endothelial growth factor receptors 1, 2, and 3, improved clinical outcomes for patients with platinum-sensitive relapsed ovarian cancer when it was used with chemotherapy and was continued as maintenance therapy. This study describes health-related quality of life (QOL) during the first year of treatment. METHODS: Four hundred fifty-six women were randomly allocated to receive standard chemotherapy only, chemotherapy with concurrent cediranib, or chemotherapy with cediranib administered concurrently and continued as maintenance...
March 24, 2017: Cancer
https://www.readbyqxmd.com/read/28259301/effectiveness-of-antiangiogenic-drugs-in-glioblastoma-patients-a-systematic-review-and-meta-analysis-of-randomized-clinical-trials
#5
REVIEW
Giuseppe Lombardi, Ardi Pambuku, Luisa Bellu, Miriam Farina, Alessandro Della Puppa, Luca Denaro, Vittorina Zagonel
BACKGROUND: glioblastomas are highly vascularized tumors and various antiangiogenic drugs have been investigated in clinical trials showing unclear results. We performed a systematic review and a meta-analysis to clarify and evaluate their effectiveness in glioblastoma patients. PATIENTS AND METHODS: we searched relevant published and unpublished randomized clinical trials analyzing antiangiogenic drugs versus chemotherapy in glioblastoma patients from January 2006 to January 2016 in MEDLINE, WEB of SCIENCE, ASCO, ESMO and SNO databases...
March 2017: Critical Reviews in Oncology/hematology
https://www.readbyqxmd.com/read/28213941/population-pharmacokinetic-and-exposure-simulation-analysis-for-cediranib-azd2171-in-pooled-phase-i-ii-studies-in-patients-with-cancer
#6
Jianguo Li, Nidal Al-Huniti, Anja Henningsson, Weifeng Tang, Eric Masson
AIMS: A population pharmacokinetic (PPK) model was developed for cediranib to simulate cediranib exposure for different doses, including co-medication with strong UGT/Pgp inducers such as rifampicin, in cancer patients. METHODS: Plasma concentrations and covariates from 625 cancer patients after single or multiple oral cediranib administrations ranging from 0.5 to 90 mg in 19 Phase I and II studies were included in the analysis. Stepwise covariate modelling was used to develop the PPK model...
February 18, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28138259/advances-in-antiangiogenic-treatment-of-small-cell-lung-cancer
#7
REVIEW
Hongyang Lu, Zhiming Jiang
Small-cell lung cancer (SCLC), a poorly differentiated neuroendocrine malignancy, has a rapid growth rate, strong aggressiveness, early metastases, and poor prognosis. Angiogenesis greatly contributes to the metastatic process of SCLC, which has a higher vascularization compared with non-small-cell lung cancer (NSCLC). SCLC might constitute an ideal malignancy for assessing new antiangiogenic drugs and therapeutic strategies. Combining bevacizumab with paclitaxel has therapeutic benefits in chemoresistant, relapsed SCLC...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28002822/the-vegfr-inhibitor-cediranib-improves-the-efficacy-of-fractionated-radiotherapy-in-a-colorectal-cancer-xenograft-model
#8
Elodie Melsens, Bert Verberckmoes, Natacha Rosseel, Christian Vanhove, Benedicte Descamps, Piet Pattyn, Wim Ceelen
BACKGROUND/PURPOSE: Radiotherapy (RT) increases local tumor control in locally advanced rectal cancer, but complete histological response is seen in only a minority of cases. Antiangiogenic therapy has been proposed to improve RT efficacy by "normalizing" the tumor microvasculature. Here, we examined whether cediranib, a pan-vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitor, improves microvascular function and tumor control in combination with RT in a mouse colorectal cancer (CRC) model...
December 22, 2016: European Surgical Research. Europäische Chirurgische Forschung. Recherches Chirurgicales Européennes
https://www.readbyqxmd.com/read/27986807/effects-of-4-multitargeted-receptor-tyrosine-kinase-inhibitors-on-regional-hemodynamics-in-conscious-freely-moving-rats
#9
Joanne J Carter, Laurice V Fretwell, Jeanette Woolard
VEGF inhibitors, including receptor tyrosine kinase inhibitors, are used as adjunct therapies in a number of cancer treatments. An emerging issue with these drugs is that most cause hypertension. To gain insight into the physiological mechanisms involved, we evaluated their regional hemodynamic effects in conscious rats. Male Sprague Dawley rats (350-450 g) were chronically implanted with pulsed Doppler flow probes (renal and mesenteric arteries, and the descending abdominal aorta) and catheters (jugular vein, peritoneal cavity, and distal abdominal aorta)...
March 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/27943222/clinical-pharmacokinetics-and-pharmacodynamics-of-cediranib
#10
REVIEW
Weifeng Tang, Alex McCormick, Jianguo Li, Eric Masson
Cediranib potently and selectively inhibits all three vascular endothelial growth factor receptors (VEGFR-1, -2 and -3), and clinical studies have shown that it is effective in patients with ovarian cancer at a dose of 20 mg/day. Cediranib is absorbed moderately slowly; a high-fat meal reduced the cediranib area under the plasma concentration-time curve (AUC) by 24% and maximum plasma concentration (C max) by 33%. Cediranib binds to serum albumin and α1-acid glycoprotein; protein binding in human plasma is approximately 95%...
December 9, 2016: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/27940520/exploring-the-benefit-risk-associated-with-antiangiogenic-agents-for-the-treatment-of-non-small-cell-lung-cancer-patients
#11
REVIEW
Razelle Kurzrock, David J Stewart
Following the approval of bevacizumab, an antibody targeting VEGF-A, for advanced non-squamous non-small cell lung cancer (NSCLC) in 2006, intensive efforts were put into the clinical development of antiangiogenic agents for NSCLC. Currently, the other antiangiogenic agents approved for NSCLC are ramucirumab, a VEGF receptor-2 (VEGFR-2)-targeting antibody indicated for both squamous and non-squamous NSCLC in the United States, and nintedanib, an anti-VEGFR-1/2/3, platelet-derived growth factor receptor-α/β, fibroblast growth factor receptor-1/2/3 angiokinase inhibitor indicated for adenocarcinoma of the lung in the European Union...
March 1, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/27920695/metastatic-alveolar-soft-part-sarcoma-responsive-to-pazopanib-after-progression-through-sunitinib-and-bevacizumab-two-cases
#12
William L Read, Felicia Williams
Alveolar soft part sarcoma (ASPS) is a rare soft tissue sarcoma with a propensity for lung metastases and indolent progression. ASPS is not responsive to chemotherapy, but there are case reports and small series describing benefit from drugs targeting the VEGF pathway. These drugs include sunitinib, cediranib and bevacizumab. There is no established second-line treatment for persons with ASPS progressing through first-line targeted therapy. We report two individuals with metastatic ASPS who obtained disease stabilization from sunitinib lasting over a year...
September 2016: Case Reports in Oncology
https://www.readbyqxmd.com/read/27781258/-research-status-quo-and-progression-in-targeted-therapy-for-advanced-gastric-cancer
#13
Rui Feng, Xiaotian Zhang, Sheng Yang
With the deeper research of the proliferation, invasion and metastasis mechanisms of the gastric cancer, targeted therapy has become a hot spot in this field. The exploration of targeted agents for gastric cancer is mainly concentrated upon the drugs that target human epidermal growth factor receptor (HER) family, the vascular endothelial growth factor (VEGF), the phosphatidylinositol 3-kinase-protein kinase/mammalian target of rapamycin (PI3K/mTOR) and the NF-κB signaling pathways. The targeted drugs relevant to HER family include the Cetuximab, Nimotuzumab, Matuzumab, Panitumumab and Erlotinib which are aimed at HER-1, the Trastuzumab, Pertuzumab and T-DM1 (trastuzumab emtansine) which are aimed at HER-2, and the Lapatinib and Afatinib which are the multi-target agents of HER...
October 25, 2016: Zhonghua Wei Chang Wai Ke za Zhi, Chinese Journal of Gastrointestinal Surgery
https://www.readbyqxmd.com/read/27748845/microrna-profiling-in-human-breast-cancer-cell-lines-exposed-to-the-anti-neoplastic-drug-cediranib
#14
A L R Bordinhão, A F Evangelista, R J S Oliveira, T Macedo, H C Silveira, R M Reis, M M Marques
Cediranib, a pan-tyrosine kinase inhibitor is showing promising results for the treatment of several solid tumours. In breast cancer, its effects remain unclear, and there are no predictive biomarkers. Several studies have examined the expression profiles of microRNAs (miRNAs) in response to different chemotherapy treatments and found that the expression patterns may be associated with the treatment response. Therefore, our aim was to evaluate the cellular behaviour and differential expression profiles of miRNAs in breast cancer cell lines exposed to cediranib...
December 2016: Oncology Reports
https://www.readbyqxmd.com/read/27486869/the-emerging-role-of-tyrosine-kinase-inhibitors-in-ovarian-cancer-treatment-a-systematic-review
#15
REVIEW
Ioannis Ntanasis-Stathopoulos, George Fotopoulos, Ioannis-Georgios Tzanninis, Elias A Kotteas
The present systematic review summarizes current evidence regarding the mechanisms of action, the efficacy, and the adverse effects of tyrosine kinase inhibitors (TKIs) in ovarian cancer patients. Phase II and III clinical trials were sought in the PubMed database and in the Clinical Trials.gov registry through September 30, 2015. Seventy-five clinical trials regarding TKIs targeting mainly vascular endothelial growth factor receptor, epidermal growth factor receptor, platelet-derived growth factor receptor, and sarcoma tyrosine kinase (Src) were yielded...
August 8, 2016: Cancer Investigation
https://www.readbyqxmd.com/read/27232884/multi-center-randomized-phase-ii-study-comparing-cediranib-plus-gefitinib-with-cediranib-plus-placebo-in-subjects-with-recurrent-progressive-glioblastoma
#16
Nicholas Brown, Catherine McBain, Stephen Nash, Kirsten Hopkins, Paul Sanghera, Frank Saran, Mark Phillips, Fiona Dungey, Laura Clifton-Hadley, Katharina Wanek, Daniel Krell, Sarah Jeffries, Iftekhar Khan, Paul Smith, Paul Mulholland
BACKGROUND: Cediranib, an oral pan-vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitor, failed to show benefit over lomustine in relapsed glioblastoma. One resistance mechanism for cediranib is up-regulation of epidermal growth factor receptor (EGFR). This study aimed to determine if dual therapy with cediranib and the oral EGFR inhibitor gefitinib improved outcome in recurrent glioblastoma. METHODS AND FINDINGS: This was a multi-center randomized, two-armed, double-blinded phase II study comparing cediranib plus gefitinib versus cediranib plus placebo in subjects with first relapse/first progression of glioblastoma following surgery and chemoradiotherapy...
2016: PloS One
https://www.readbyqxmd.com/read/27052640/pharmacotherapies-for-the-treatment-of-glioblastoma-current-evidence-and-perspectives
#17
REVIEW
Katharina Seystahl, Dorothee Gramatzki, Patrick Roth, Michael Weller
INTRODUCTION: Glioblastoma, the most common malignant brain tumor, exhibits a poor prognosis with little therapeutic progress in the last decade. Novel treatment strategies beyond the established standard of care with temozolomide-based radiotherapy are urgently needed. AREAS COVERED: We reviewed the literature on glioblastoma with a focus on phase III trials for pharmacotherapies and/or innovative concepts until December 2015. EXPERT OPINION: In the last decade, phase III trials on novel compounds largely failed to introduce efficacious pharmacotherapies beyond temozolomide in glioblastoma...
June 2016: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/27044097/dual-inhibition-of-ang-2-and-vegf-receptors-normalizes-tumor-vasculature-and-prolongs-survival-in-glioblastoma-by-altering-macrophages
#18
Teresa E Peterson, Nathaniel D Kirkpatrick, Yuhui Huang, Christian T Farrar, Koen A Marijt, Jonas Kloepper, Meenal Datta, Zohreh Amoozgar, Giorgio Seano, Keehoon Jung, Walid S Kamoun, Trupti Vardam, Matija Snuderl, Jermaine Goveia, Sampurna Chatterjee, Ana Batista, Alona Muzikansky, Ching Ching Leow, Lei Xu, Tracy T Batchelor, Dan G Duda, Dai Fukumura, Rakesh K Jain
Glioblastomas (GBMs) rapidly become refractory to anti-VEGF therapies. We previously demonstrated that ectopic overexpression of angiopoietin-2 (Ang-2) compromises the benefits of anti-VEGF receptor (VEGFR) treatment in murine GBM models and that circulating Ang-2 levels in GBM patients rebound after an initial decrease following cediranib (a pan-VEGFR tyrosine kinase inhibitor) administration. Here we tested whether dual inhibition of VEGFR/Ang-2 could improve survival in two orthotopic models of GBM, Gl261 and U87...
April 19, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27025186/cediranib-in-patients-with-relapsed-platinum-sensitive-ovarian-cancer-icon6-a-randomised-double-blind-placebo-controlled-phase-3-trial
#19
RANDOMIZED CONTROLLED TRIAL
Jonathan A Ledermann, Andrew C Embleton, Fharat Raja, Timothy J Perren, Gordon C Jayson, Gordon J S Rustin, Stan B Kaye, Hal Hirte, Elizabeth Eisenhauer, Michelle Vaughan, Michael Friedlander, Antonio González-Martín, Daniel Stark, Elizabeth Clark, Laura Farrelly, Ann Marie Swart, Adrian Cook, Richard S Kaplan, Mahesh K B Parmar
BACKGROUND: Angiogenesis is a validated clinical target in advanced epithelial ovarian cancer. Cediranib is an oral antiangiogenic vascular endothelial growth factor receptor 1-3 inhibitor that has shown antitumour activity in recurrent ovarian cancer. We assessed efficacy and safety of cediranib in combination with platinum-based chemotherapy and as continued maintenance treatment in patients with first relapse of platinum-sensitive ovarian cancer. METHODS: In this randomised, three-arm, double-blind, placebo-controlled phase 3 trial, we randomly assigned patients aged 18 years or older with relapsed platinum-sensitive ovarian cancer at 63 centres in Australia, Canada, New Zealand, Spain, and the UK...
March 12, 2016: Lancet
https://www.readbyqxmd.com/read/27009237/autocrine-vegfr1-and-vegfr2-signaling-promotes-survival-in-human-glioblastoma-models-in-vitro-and-in-vivo
#20
Emese Szabo, Hannah Schneider, Katharina Seystahl, Elisabeth Jane Rushing, Frank Herting, K Michael Weidner, Michael Weller
BACKGROUND: Although the vascular endothelial growth factor (VEGF)/VEGF receptor (VEGFR) system has become a prime target for antiangiogenic treatment, its biological role in glioblastoma beyond angiogenesis has remained controversial. METHODS: Using neutralizing antibodies to VEGF or placental growth factor (PlGF) or the tyrosine kinase inhibitor, cediranib, or lentiviral gene silencing, we delineated autocrine signaling in glioma cell lines. The in vivo effects of VEGFR1 and VEGFR2 depletion were evaluated in orthotopic glioma xenograft models...
September 2016: Neuro-oncology
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