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Cabozantinib

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https://www.readbyqxmd.com/read/29284153/role-of-ret-protein-tyrosine-kinase-inhibitors-in-the-treatment-ret-driven-thyroid-and-lung-cancers
#1
REVIEW
Robert Roskoski, Abdollah Sadeghi-Nejad
RET is a transmembrane receptor protein-tyrosine kinase that is required for the development of the nervous system and several other tissues. The mechanism of activation of RET by its glial-cell derived neurotrophic factor (GDNF) ligands differs from that of all other receptor protein-tyrosine kinases owing to the requirement for additional GDNF family receptor-α (GFRα) co-receptors (GFRα1/2/3/4). RET point mutations have been reported in multiple endocrine neoplasia (MEN2A, MEN2B) and medullary thyroid carcinoma...
December 25, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/29283440/cabozantinib-a-multi-targeted-oral-tyrosine-kinase-inhibitor
#2
Jordan N Markowitz, Karen M Fancher
Cabozantinib is an oral, small-molecule, multitargeted tyrosine kinase inhibitor (TKI) that may confer an advantage over other TKIs that target a single receptor. It has been approved by the United States Food and Drug Administration for the treatment of both advanced renal cell carcinoma and progressive metastatic medullary thyroid cancer, and is being investigated for a wide array of other malignancies. Rationale for use, clinical trial data, and current recommendations for cabozantinib in renal cell cancer, thyroid cancer, prostate cancer, hepatocellular cancer, and lung cancer are detailed in this article...
December 28, 2017: Pharmacotherapy
https://www.readbyqxmd.com/read/29243843/signaling-cascades-in-thyroid-cancer-increasing-the-armory-of-archers-to-hit-bullseye
#3
Faiza Abdul Rashid, Qaisar Mansoor, Hafsa Aziz, Sobia Tabassum, Waleed O Arfat, George E Naoum, Muhammad Ismail, Ammad Ahmad Farooqi
Thyroid cancer is a multifaceted and therapeutically challenging disease and rapidly accumulating experimentally verified findings have considerably improve our understanding of the molecular mechanisms which underlie its development. Substantial fraction of information has been added into existing landscape of molecular oncology and we have started to develop a sharper understanding of the underlying mechanisms of thyroid cancer. Wealth of information demystified different intracellular signaling cascades which are frequently deregulated in thyroid cancer...
December 15, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/29223605/updated-european-association-of-urology-guidelines-recommendations-for-the-treatment-of-first-line-metastatic-clear-cell-renal-cancer
#4
REVIEW
Thomas Powles, Laurence Albiges, Michael Staehler, Karim Bensalah, Saeed Dabestani, Rachel H Giles, Fabian Hofmann, Milan Hora, Markus A Kuczyk, Thomas B Lam, Lorenzo Marconi, Axel S Merseburger, Sergio Fernández-Pello, Rana Tahbaz, Alessandro Volpe, Börje Ljungberg, Axel Bex
The randomised phase III clinical trial Checkmate-214 showed a survival superiority for the combination of ipilimumab and nivolumab when compared with the previous standard of care in first-line metastatic/advanced clear cell renal cell carcinoma (RCC) (Escudier B, Tannir NM, McDermott DF, et al. CheckMate 214: efficacy and safety of nivolumab plus ipilimumab vs sunitinib for treatment-naïve advanced or metastatic renal cell carcinoma, including IMDC risk and PD-L1 expression subgroups. LBA5, ESMO 2017, 2017)...
December 6, 2017: European Urology
https://www.readbyqxmd.com/read/29219214/whole-exome-sequencing-identifies-a-germline-met-mutation-in-two-siblings-with-hereditary-wild-type-ret-medullary-thyroid-cancer
#5
Marialuisa Sponziello, Silvia Benvenuti, Alessandra Gentile, Valeria Pecce, Francesca Rosignolo, Anna Rita Virzì, Melissa Milan, Paolo M Comoglio, Eric Londin, Paolo Fortina, Agnese Barnabei, Marialuisa Appetecchia, Ferdinando Marandino, Diego Russo, Sebastiano Filetti, Cosimo Durante, Antonella Verrienti
Whole exome sequencing (WES) was used to investigate two Italian siblings with wild-type RET genotype, who developed medullary thyroid cancers (MTCs) and, later, primary prostate and breast cancers, respectively. The proband's MTC harbored a p.Met918Thr RET mutation; his sister's MTC was RET/RAS wild-type. Both siblings had a germline mutation (p.Arg417Gln) in the extracellular Sema domain of the proto-oncogene MET. Experiments involving ectopic expression of MET p.Arg417Gln in MET-negative T47D breast cancer cells documented the mutant receptor's functionality and its ability to enhance cell migration and invasion...
December 8, 2017: Human Mutation
https://www.readbyqxmd.com/read/29198329/examining-the-bleeding-incidences-associated-with-targeted-therapies-used-in-metastatic-renal-cell-carcinoma
#6
REVIEW
MacKenzie Crist, Elizabeth Hansen, Lipika Chablani, Elizabeth Guancial
A systematic review was conducted to illustrate the bleeding risks associated with targeted therapies used in the treatment of metastatic renal cell carcinoma (mRCC). Eligible studies included phase II, III, or IV clinical trials using pazopanib, sunitinib, cabozantinib, lenvatinib, everolimus, temsirolimus, bevacizumab, axitinib, and/or sorafenib in the setting of mRCC. Types of bleeding event(s), bleeding event frequency, and incidence of thrombocytopenia were collected from the relevant articles. ClinicalTrials...
December 2017: Critical Reviews in Oncology/hematology
https://www.readbyqxmd.com/read/29191878/the-target-landscape-of-clinical-kinase-drugs
#7
Susan Klaeger, Stephanie Heinzlmeir, Mathias Wilhelm, Harald Polzer, Binje Vick, Paul-Albert Koenig, Maria Reinecke, Benjamin Ruprecht, Svenja Petzoldt, Chen Meng, Jana Zecha, Katrin Reiter, Huichao Qiao, Dominic Helm, Heiner Koch, Melanie Schoof, Giulia Canevari, Elena Casale, Stefania Re Depaolini, Annette Feuchtinger, Zhixiang Wu, Tobias Schmidt, Lars Rueckert, Wilhelm Becker, Jan Huenges, Anne-Kathrin Garz, Bjoern-Oliver Gohlke, Daniel Paul Zolg, Gian Kayser, Tonu Vooder, Robert Preissner, Hannes Hahne, Neeme Tõnisson, Karl Kramer, Katharina Götze, Florian Bassermann, Judith Schlegl, Hans-Christian Ehrlich, Stephan Aiche, Axel Walch, Philipp A Greif, Sabine Schneider, Eduard Rudolf Felder, Juergen Ruland, Guillaume Médard, Irmela Jeremias, Karsten Spiekermann, Bernhard Kuster
Kinase inhibitors are important cancer therapeutics. Polypharmacology is commonly observed, requiring thorough target deconvolution to understand drug mechanism of action. Using chemical proteomics, we analyzed the target spectrum of 243 clinically evaluated kinase drugs. The data revealed previously unknown targets for established drugs, offered a perspective on the "druggable" kinome, highlighted (non)kinase off-targets, and suggested potential therapeutic applications. Integration of phosphoproteomic data refined drug-affected pathways, identified response markers, and strengthened rationale for combination treatments...
December 1, 2017: Science
https://www.readbyqxmd.com/read/29174801/dual-targeting-c-met-and-vegfr2-in-osteoblasts-suppresses-growth-and-osteolysis-of-prostate-cancer-bone-metastasis
#8
Changki Lee, Young Mi Whang, Preston Campbell, Patrick L Mulcrone, Florent Elefteriou, Sun Wook Cho, Serk In Park
Prostate cancer characteristically induces osteoblastic bone metastasis, for which no therapies are available. A dual kinase inhibitor of c-Met and VEGFR-2 (cabozantinib) was shown to reduce prostate cancer growth in bone, with evidence for suppressing osteoblastic activity. However, c-Met and VEGFR2 signaling in osteoblasts in the context of bone metastasis remain unclear. Here we show using cultured osteoblasts that hepatocyte growth factor (HGF) and VEGF-A increased receptor activator of NFκB ligand (RANKL) and M-CSF, two essential factors for osteoclastogenesis...
November 21, 2017: Cancer Letters
https://www.readbyqxmd.com/read/29152128/modulation-of-cabozantinib-efficacy-by-the-prostate-tumor-microenvironment
#9
Manisha Tripathi, Srinivas Nandana, Sandrine Billet, Karen A Cavassani, Rajeev Mishra, Leland W K Chung, Edwin M Posadas, Neil A Bhowmick
The tumor microenvironment (TME) is increasingly recognized as the arbiter of metastatic progression and drug resistance in advanced prostate cancer (PCa). Cabozantinib is a potent tyrosine kinase inhibitor (TKI) with reported biological activity in the PCa epithelia, but failed to provide an overall survival benefit in phase 3 clinical trials. However, the promising biologic efficacy of the drug in early trials warranted a better understanding of the mechanism of action, with the goal of improving patient selection for TKI-based therapy such as cabozantinib...
October 20, 2017: Oncotarget
https://www.readbyqxmd.com/read/29146618/management-of-adverse-events-associated-with-cabozantinib-therapy-in-renal-cell-carcinoma
#10
REVIEW
Manuela Schmidinger, Romano Danesi
Cabozantinib was recently approved for the treatment of advanced renal cell carcinoma (RCC) after treatment with vascular endothelial growth factor (VEGF)-targeted therapy. Cabozantinib is a multikinase inhibitor targeting VEGF receptor (VEGFR) 2, mesenchymal-epithelial transition receptor, and "anexelekto" receptor tyrosine kinase. A 60-mg daily dose led to improved overall survival and progression-free survival (PFS) versus everolimus in advanced RCC patients as a second- or later-line treatment in the METEOR trial...
November 16, 2017: Oncologist
https://www.readbyqxmd.com/read/29134564/seom-clinical-guideline-for-treatment-of-kidney-cancer-2017
#11
E Gallardo, M J Méndez-Vidal, J L Pérez-Gracia, J M Sepúlveda-Sánchez, M Campayo, I Chirivella-González, X García-Del-Muro, A González-Del-Alba, E Grande, C Suárez
The goal of this article is to provide recommendations about the management of kidney cancer. Based on pathologic and molecular features, several kidney cancer variants were described. Nephron-sparing techniques are the gold standard of localized disease. After a randomized trial, sunitinib could be considered in adjuvant treatment in high-risk patients. Patients with advanced disease constitute a heterogeneous population. Prognostic classification should be considered. Both sunitinib and pazopanib are the standard options for first-line systemic therapy in advanced renal cell carcinoma...
November 13, 2017: Clinical & Translational Oncology
https://www.readbyqxmd.com/read/29128427/osimertinib-and-cabozantinib-combinatorial-therapy-in-an-egfr-mutant-lung-adenocarcinoma-patient-with-multiple-met-secondary-site-mutations-after-resistance-to-crizotinib
#12
Jin Kang, Hua-Jun Chen, Zheng Wang, Jing Liu, Bing Li, Tengfei Zhang, Zhenfan Yang, Yi-Long Wu, Jin-Ji Yang
No abstract text is available yet for this article.
November 8, 2017: Journal of Thoracic Oncology
https://www.readbyqxmd.com/read/29089775/practical-management-of-adverse-events-associated-with-cabozantinib-treatment-in-patients-with-renal-cell-carcinoma
#13
REVIEW
Benjamin S Gerendash, Patricia A Creel
Cabozantinib is an oral tyrosine-kinase inhibitor whose targets include VEGFR, MET, and AXL. Cabozantinib is approved for the treatment of patients with advanced clear-cell renal-cell carcinoma (RCC) who have received prior antiangiogenic therapy. In the pivotal Phase III trial of second-line RCC, cabozantinib was associated with a significant improvement in overall survival, progression-free survival, and antitumor response compared with everolimus. Adverse events (AEs) were common for patients receiving cabozantinib, but were effectively managed with supportive care and dose modifications, as discontinuations of cabozantinib due to an AE were infrequent...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/29082855/comparative-efficacy-and-safety-of-second-line-treatments-for-advanced-non-small-cell-lung-cancer-with-wild-type-or-unknown-status-for-epidermal-growth-factor-receptor-a-systematic-review-and-network-meta-analysis
#14
Perrine Créquit, Anna Chaimani, Amélie Yavchitz, Nassima Attiche, Jacques Cadranel, Ludovic Trinquart, Philippe Ravaud
BACKGROUND: Docetaxel, pemetrexed, erlotinib, and gefitinib are recommended as second-line treatment for advanced non-small cell lung cancer (NSCLC) with wild-type or unknown status for epidermal growth factor receptor (EGFR). However, the number of published randomized clinical trials (RCTs) on this topic is increasing. Our objective was to assess the comparative effectiveness and tolerability of all second-line treatments for advanced NSCLC with wild-type or unknown status for EGFR by a systematic review and network meta-analysis...
October 30, 2017: BMC Medicine
https://www.readbyqxmd.com/read/29074560/a-network-meta-analysis-of-short-term-efficacy-of-different-single-drug-targeted-therapies-in-the-treatment-of-renal-cell-carcinoma
#15
Hong-Ling He, Wan-Xia Yao
The network meta-analysis was conducted to compare the short-term efficacy of different single-drug targeted therapies in the treatment of renal cell carcinoma (RCC). We initially searched databases for randomized controlled trials (RCTs) on different single-drug targeted therapies in treating RCC. The meta-analysis combined the direct and indirect evidence to calculate the pooled odds ratios (OR) and draw surface under the cumulative ranking curves (SUCRA). A total of 14 eligible RCTs were ultimately selected...
October 26, 2017: Bioscience Reports
https://www.readbyqxmd.com/read/29063069/targeting-met-in-cancer-therapy
#16
REVIEW
Hong-Nan Mo, Peng Liu
MET encodes a receptor tyrosine kinase c-MET for hepatocyte growth factor (HGF). The specific combination of c-MET and HGF activates downstream signaling pathways to trigger cell migration, proliferation, and angiogenesis. MET exon 14 alterations and MET gene amplification play a critical role in the origin of cancer. Several monoclonal antibodies and small-molecule inhibitors of c-MET have been evaluated in clinical trials. In patients with advanced non-small cell lung cancer, cabozantinib and crizotinib showed clear efficacy with a generally tolerable adverse events profile...
September 2017: Chronic Diseases and Translational Medicine
https://www.readbyqxmd.com/read/29061793/the-anti-tumor-effect-of-cabozantinib-on-ovarian-clear-cell-carcinoma-in-vitro-and-in-vivo
#17
Makiko Nakatani, Hidemichi Watari, Takashi Mitamura, Lei Wang, Yutaka Hatanaka, Kanako C Hatanaka, Kohei Honda, Toshiyuki Nomura, Hiroshi Nishihara, Shinya Tanaka, Noriaki Sakuragi
BACKGROUND: Several reports have shown that the overexpression of the MET proto-oncogene, receptor tyrosine kinase (MET), was more frequently observed in clear cell carcinoma (CCC) than in non-CCC. We evaluated the antitumor activity of cabozantinib, that targets MET. MATERIALS AND METHODS: A gene expression analysis of tumors from human ovarian cancers was carried out by transcriptome sequencing. An in vitro 3-(4, 5-dimethylthiazolyl-2)-2, 5-diphenyltetrazolium bromide assay (MTT assay) and in vivo experiments were performed to determine the activity of cabozantinib...
November 2017: Anticancer Research
https://www.readbyqxmd.com/read/29059635/phase-ii-randomised-discontinuation-trial-of-cabozantinib-in-patients-with-advanced-solid-tumours
#18
RANDOMIZED CONTROLLED TRIAL
Patrick Schöffski, Michael Gordon, David C Smith, Razelle Kurzrock, Adil Daud, Nicholas J Vogelzang, Yihua Lee, Christian Scheffold, Geoffrey I Shapiro
BACKGROUND: Cabozantinib is an inhibitor of tyrosine kinases, including MET, vascular endothelial growth factor receptor, AXL and RET. This multi-cohort phase II randomised discontinuation trial explored anticancer activity of cabozantinib in nine tumour types. PATIENTS AND METHODS: Cabozantinib was administered (100 mg, once daily) to patients with advanced, recurrent or metastatic cancers. Those with stable disease at week 12 were randomised 1:1 to cabozantinib or placebo...
November 2017: European Journal of Cancer
https://www.readbyqxmd.com/read/29057215/targeted-therapy-for-medullary-thyroid-cancer-a-review
#19
REVIEW
S R Priya, Chandra Shekhar Dravid, Raghunadharao Digumarti, Mitali Dandekar
Medullary thyroid cancers (MTCs) constitute between 2 and 5% of all thyroid cancers. The 10-year overall survival (OS) rate of patients with localized disease is around 95% while that of patients with regional stage disease is about 75%. Only 20% of patients with distant metastases at diagnosis survive 10 years which is significantly lower than for differentiated thyroid cancers. Cases with regional metastases at presentation have high recurrence rates. Adjuvant external radiation confers local control but not improved OS...
2017: Frontiers in Oncology
https://www.readbyqxmd.com/read/29045520/overall-survival-analysis-of-exam-a-phase-iii-trial-of-cabozantinib-in-patients-with-radiographically-progressive-medullary-thyroid-carcinoma
#20
M Schlumberger, R Elisei, S Müller, P Schöffski, M Brose, M Shah, L Licitra, J Krajewska, M C Kreissl, B Niederle, E E W Cohen, L Wirth, H Ali, D O Clary, Y Yaron, M Mangeshkar, D Ball, B Nelkin, S Sherman
Background: Primary analysis of the double-blind, phase III Efficacy of XL184 (Cabozantinib) in Advanced Medullary Thyroid Cancer (EXAM) trial demonstrated significant improvement in progression-free survival with cabozantinib versus placebo in patients with progressive medullary thyroid cancer (MTC). Final analysis of overall survival (OS), a key secondary endpoint, was carried out after long-term follow-up. Patients and methods: EXAM compared cabozantinib with placebo in 330 patients with documented radiographic progression of metastatic MTC...
November 1, 2017: Annals of Oncology: Official Journal of the European Society for Medical Oncology
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