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Cabozantinib

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https://www.readbyqxmd.com/read/27922668/dual-inhibition-using-cabozantinib-overcomes-hgf-met-signaling-mediated-resistance-to-pan-vegfr-inhibition-in-orthotopic-and-metastatic-neuroblastoma-tumors
#1
Estelle Daudigeos-Dubus, Ludivine Le Dret, Olivia Bawa, Paule Opolon, Albane Vievard, Irène Villa, Jacques Bosq, Gilles Vassal, Birgit Geoerger
MET is expressed on neuroblastoma cells and may trigger tumor growth, neoangiogenesis and metastasis. MET upregulation further represents an escape mechanism to various anticancer treatments including VEGF signaling inhibitors. We developed in vitro a resistance model to pan-VEGFR inhibition and explored the simultaneous inhibition of VEGFR and MET in neuroblastoma models in vitro and in vivo using cabozantinib, an inhibitor of the tyrosine kinases including VEGFR2, MET, AXL and RET. Resistance in IGR-N91-Luc neuroblastoma cells under continuous in vitro exposure pressure to VEGFR1-3 inhibition using axitinib was associated with HGF and p-ERK overexpression...
December 6, 2016: International Journal of Oncology
https://www.readbyqxmd.com/read/27909994/cabozantinib-a-review-in-advanced-renal-cell-carcinoma
#2
Zaina T Al-Salama, Gillian M Keating
The multiple tyrosine kinase inhibitor (TKI) cabozantinib (Cabometyx™) is approved in the USA for the treatment of patients with advanced renal cell carcinoma (RCC) who have received prior antiangiogenic therapy. In the EU, cabozantinib is indicated for the treatment of advanced RCC in adults following prior vascular endothelial growth factor (VEGF)-targeted therapy. In adults with advanced or metastatic clear-cell RCC who had previously received VEGF receptor (VEGFR) TKIs, progression-free survival (PFS) and overall survival (OS) were significantly prolonged in patients who received oral cabozantinib versus oral everolimus in the pivotal METEOR trial...
December 1, 2016: Drugs
https://www.readbyqxmd.com/read/27904650/cabozantinib-in-the-treatment-of-advanced-renal-cell-carcinoma-clinical-trial-evidence-and-experience
#3
REVIEW
Jose Manuel Ruiz-Morales, Daniel Y C Heng
The treatment of metastatic renal cell carcinoma (mRCC) is rapidly changing. During first-line treatment with targeted therapy, patients ultimately develop resistance to therapy and the disease progresses. Recently, cabozantinib has demonstrated a better response rate, progression-free survival and overall survival compared with everolimus after failure of prior targeted therapy in patients with advanced or metastatic renal cell carcinoma (RCC). Cabozantinib is a small-molecule tyrosine kinase inhibitor (TKI)...
December 2016: Therapeutic Advances in Urology
https://www.readbyqxmd.com/read/27890466/cabozantinib-improves-clinical-outcomes-in-renal-cancer
#4
Manjulika Das
No abstract text is available yet for this article.
November 24, 2016: Lancet Oncology
https://www.readbyqxmd.com/read/27881454/cabozantinib-is-active-in-patients-with-advanced-ret-rearranged-nsclc
#5
(no author information available yet)
Cabozantinib achieved an overall response rate of 28% in patients with RET-rearranged NSCLC.
November 23, 2016: Cancer Discovery
https://www.readbyqxmd.com/read/27881453/cabozantinib-is-more-effective-than-erlotinib-in-egfr-wild-type-nsclc
#6
(no author information available yet)
Cabozantinib alone or in combination with erlotinib extended survival compared with erlotinib alone.
November 23, 2016: Cancer Discovery
https://www.readbyqxmd.com/read/27879272/quantification-of-pathway-crosstalk-reveals-novel-synergistic-drug-combinations-for-breast-cancer
#7
Samira Jaeger, Ana Igea, Rodrigo Arroyo, Victor Alcalde, Begoña Canovas, Modesto Orozco, Angel R Nebreda, Patrick Aloy
Combinatorial therapeutic approaches are an imperative to improve cancer treatment, since it is critical to impede compensatory signaling mechanisms that can engender drug resistance to individual targeted drugs. Currently approved drug combinations result largely from empirical clinical experience and cover only a small fraction of a vast therapeutic space. Here we present a computational network biology approach, based on pathway crosstalk inhibition, to discover new synergistic drug combinations for breast cancer treatment...
November 22, 2016: Cancer Research
https://www.readbyqxmd.com/read/27849399/new-chemical-treatment-options-in-second-line-hepatocellular-carcinoma-what-to-do-when-sorafenib-fails
#8
Hyun Young Woo, So Young Yoo, Jeong Heo
There have been no therapies available for patients who experience disease progression after sorafenib treatment. Regorafenib inhibits multiple kinases involved in tumor proliferation and neoangiogenesis, which has produced a survival benefit in hepatocellular carcinoma (HCC) after sorafenib failure. Other active candidate agents are c-Met inhibitors and immune checkpoint inhibitors. Areas covered: This paper presents an updated summary of the preclinical and clinical experience with regorafenib, c-Met inhibitors (tivantinib, cabozantinib and tepotinib), and a checkpoint inhibitor (nivolumab, pembrolizumab) in HCC...
November 28, 2016: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/27842445/cabozantinib-in-genitourinary-malignancies
#9
Tian Zhang, Se Eun Park, Cierra Hong, Daniel J George
Cabozantinib inhibits a variety of cellular receptors including VEGFR1-3, MET, AXL, RET, FLT3 and KIT. These signaling pathways have been shown to be important in genitourinary malignancies. Along its clinical development, it has shown most activity in advanced renal cell carcinoma; the METEOR study compared cabozantinib to everolimus and showed clinically and statistically significant improvements in both progression-free survival and overall survival. Herein, we review the development of cabozantinib in the genitourinary malignancies of renal cell carcinoma, prostate adenocarcinoma and urothelial carcinoma...
November 15, 2016: Future Oncology
https://www.readbyqxmd.com/read/27835047/cabozantinib-for-the-treatment-of-renal-cell-carcinoma
#10
Bernard Escudier, Julie C Lougheed, Laurence Albiges
Agents that target the vascular endothelial growth factor (VEGF) or mammalian target of rapamycin (mTOR) pathway as well as the PD-1 checkpoint inhibitor nivolumab are standard therapies for advanced renal cell carcinoma (RCC). Recently, cabozantinib, an inhibitor of MET, VEGF receptors, and AXL, was approved by the FDA and European Commission based on improved progression-free survival (PFS), overall survival (OS), and objective response rate (ORR) compared to standard of care treatment with everolimus in a randomized phase 3 trial in advanced RCC after prior VEGFR-tyrosine kinase inhibitor (TKI) therapy...
November 22, 2016: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/27825638/erlotinib-cabozantinib-or-erlotinib-plus-cabozantinib-as-second-line-or-third-line-treatment-of-patients-with-egfr-wild-type-advanced-non-small-cell-lung-cancer-ecog-acrin-1512-a-randomised-controlled-open-label-multicentre-phase-2-trial
#11
Joel W Neal, Suzanne E Dahlberg, Heather A Wakelee, Seena C Aisner, Michaela Bowden, Ying Huang, David P Carbone, Gregory J Gerstner, Rachel E Lerner, Jerome L Rubin, Taofeek K Owonikoko, Philip J Stella, Preston D Steen, Ahmed Ali Khalid, Suresh S Ramalingam
BACKGROUND: Erlotinib is approved for the treatment of all patients with advanced non-small-cell lung cancer (NSCLC), but is most active in the treatment of EGFR mutant NSCLC. Cabozantinib, a small molecule tyrosine kinase inhibitor, targets MET, VEGFR, RET, ROS1, and AXL, which are implicated in lung cancer tumorigenesis. We compared the efficacy of cabozantinib alone or in combination with erlotinib versus erlotinib alone in patients with EGFR wild-type NSCLC. METHODS: This three group, randomised, controlled, open-label, multicentre, phase 2 trial was done in 37 academic and community oncology practices in the USA...
November 4, 2016: Lancet Oncology
https://www.readbyqxmd.com/read/27825636/cabozantinib-in-patients-with-advanced-ret-rearranged-non-small-cell-lung-cancer-an-open-label-single-centre-phase-2-single-arm-trial
#12
Alexander Drilon, Natasha Rekhtman, Maria Arcila, Lu Wang, Andy Ni, Melanie Albano, Martine Van Voorthuysen, Romel Somwar, Roger S Smith, Joseph Montecalvo, Andrew Plodkowski, Michelle S Ginsberg, Gregory J Riely, Charles M Rudin, Marc Ladanyi, Mark G Kris
BACKGROUND: RET rearrangements are found in 1-2% of non-small-cell lung cancers. Cabozantinib is a multikinase inhibitor with activity against RET that produced a 10% overall response in unselected patients with lung cancers. To assess the activity of cabozantinib in patients with RET-rearranged lung cancers, we did a prospective phase 2 trial in this molecular subgroup. METHODS: We enrolled patients in this open-label, Simon two-stage, single-centre, phase 2, single-arm trial in the USA if they met the following criteria: metastatic or unresectable lung cancer harbouring a RET rearrangement, Karnofsky performance status higher than 70, and measurable disease...
November 4, 2016: Lancet Oncology
https://www.readbyqxmd.com/read/27799362/animal-models-of-medullary-thyroid-cancer-state-of-the-art-and-view-to-the-future
#13
Giovanni Vitale, Germano Gaudenzi, Luisa Circelli, Marco Federico Manzoni, Andrea Bassi, Niccolò Fioritti, Antongiulio Faggiano, Annamaria Al Colao
Medullary thyroid carcinoma is a neuroendocrine tumour originating from parafollicular C cells accounting for 5-10% of thyroid cancers. Increased understanding of disease-specific molecular targets of therapy has led to the regulatory approval of two drugs (vandetanib and cabozantinib) for the treatment of medullary thyroid carcinoma. These drugs increase progression free survival, however, they are often poorly tolerated and most treatment responses are transient. Animal models are indispensable tools for investigating the pathogenesis, mechanisms for tumour invasion and metastasis, and new therapeutic approaches for cancer...
October 31, 2016: Endocrine-related Cancer
https://www.readbyqxmd.com/read/27793960/u-s-food-and-drug-administration-approval-cabozantinib-for-treatment-of-advanced-renal-cell-carcinoma
#14
Harpreet Singh, Michael Brave, Julia A Beaver, Joyce Cheng, Shenghui Tang, Eias Zahalka, Todd R Palmby, Rajesh Venugopal, Pengfei Song, Qi Liu, Chao Liu, Jingyu Yu, Xiao Hong Chen, Xing Wang, Yaning Wang, Paul G Kluetz, Selena R Daniels, Elektra J Papadopoulos, Rajeshwari Sridhara, Amy E McKee, Amna Ibrahim, Geoffrey Kim, Richard Pazdur
On April 25, 2016, the U. S. Food and Drug Administration (FDA) approved cabozantinib (CABOMETYX{trade mark, serif}, Exelixis, Inc.) for the treatment of advanced renal cell carcinoma (RCC) in patients who have received prior anti-angiogenic therapy. The approval was based on data from one randomized, open-label, multicenter study in which RCC patients who had received prior anti-angiogenic therapy were treated with either cabozantinib 60 mg orally once daily (N=330) or everolimus 10 mg orally once daily (N=328)...
October 28, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/27792051/advances-and-controversies-in-the-management-of-medullary-thyroid-carcinoma
#15
Ana Luiza Maia, Simone Magagnin Wajner, Carla Vaz Ferreira Vargas
PURPOSE OF REVIEW: Medullary thyroid carcinoma (MTC) comprises approximately 4% of all malignant thyroid neoplasms. Although the majority of patients have a good prognosis, a subgroup of patients develops progressive disease and requires systemic therapy. Here, we focused on the current MTC therapeutic approaches and discussed the advantages and disadvantages of molecular targeted therapies. RECENT FINDINGS: Targeted molecular therapies that inhibit RET and other tyrosine kinase receptors involved in angiogenesis have been shown to improve progression-free survival in patients with advanced MTC...
January 2017: Current Opinion in Oncology
https://www.readbyqxmd.com/read/27789775/phase-ii-and-biomarker-study-of-cabozantinib-in-metastatic-triple-negative-breast-cancer-patients
#16
Sara M Tolaney, David R Ziehr, Hao Guo, Mei R Ng, William T Barry, Michaela J Higgins, Steven J Isakoff, Jane E Brock, Elena V Ivanova, Cloud P Paweletz, Michelle K Demeo, Nikhil H Ramaiya, Beth A Overmoyer, Rakesh K Jain, Eric P Winer, Dan G Duda
: : There are currently no targeted therapies available for metastatic triple-negative breast cancer (mTNBC). We evaluated the safety, efficacy, and biomarkers of response to cabozantinib, a multikinase inhibitor, in patients with mTNBC. We conducted a single-arm phase 2 and biomarker study that enrolled patients with measurable mTNBC. Patients received cabozantinib (60mg daily) on a 3-week cycle, and were restaged after 6 weeks and then every 9 weeks. The primary endpoint was objective response rate...
October 27, 2016: Oncologist
https://www.readbyqxmd.com/read/27777285/cabozantinib-is-active-against-human-gastrointestinal-stromal-tumor-xenografts-carrying-different-kit-mutations
#17
Yemarshet K Gebreyohannes, Patrick Schöffski, Thomas Van Looy, Jasmien Wellens, Lise Vreys, Jasmien Cornillie, Ulla Vanleeuw, Dana T Aftab, Maria Debiec-Rychter, Raf Sciot, Agnieszka Wozniak
In the majority of gastrointestinal stromal tumors (GIST), oncogenic signaling is driven by KIT mutations. Advanced GIST is treated with tyrosine kinase inhibitors (TKI) such as imatinib. Acquired resistance to TKI is mainly caused by secondary KIT mutations, but can also be attributed to a switch of KIT dependency to another receptor tyrosine kinase (RTK). We tested the efficacy of cabozantinib, a novel TKI targeting KIT, MET, AXL, and vascular endothelial growth factor receptors (VEGFR), in patient-derived xenograft (PDX) models of GIST, carrying different KIT mutations...
December 2016: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/27742787/thyroid-cancer-risk-stratified-management-and-individualized-therapy
#18
Friedhelm Raue, Karin Frank-Raue
Thyroid cancer is the most common endocrine malignancy. Differentiated thyroid cancer (DTC) with the two subtypes, papillary thyroid cancer (PTC) and follicular thyroid cancer (FTC), is the most frequent subtype of thyroid cancer; more rare subtypes are medullary thyroid cancer (MTC) and anaplastic thyroid cancer (ATC). The incidence of DTC has increased rapidly in recent years due to the more frequent use of imaging methods such as ultrasound of the neck and fine-needle aspiration (FNA) of thyroid nodules...
October 15, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/27734291/clinical-pharmacokinetics-and-pharmacodynamics-of-cabozantinib
#19
Steven A Lacy, Dale R Miles, Linh T Nguyen
Cabozantinib inhibits receptor tyrosine kinases involved in tumor angiogenesis and metastasis. The capsule formulation (Cometriq(®)) is approved for the treatment of progressive metastatic medullary thyroid cancer at a 140-mg free base equivalent dose. The tablet formulation (Cabometyx™, 60-mg free base equivalent dose) is approved for the treatment of renal cell carcinoma following anti-angiogenic therapy. Cabozantinib displays a long terminal plasma half-life (~120 h) and accumulates ~fivefold by day 15 following daily dosing based on area under the plasma concentration-time curve (AUC)...
October 12, 2016: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/27715452/cabozantinib-inhibits-tumor-growth-and-metastasis-of-a-patient-derived-xenograft-model-of-papillary-renal-cell-carcinoma-with-met-mutation
#20
Hongjuan Zhao, Rosalie Nolley, Andy M W Chan, Erinn B Rankin, Donna M Peehl
MET plays an important role in the development and progression of papillary renal cell carcinoma (pRCC). Evaluation of efficacy of MET inhibitors against pRCC has been hampered by limited preclinical models depicting MET abnormalities. We established a new patient-derived xenograft (PDX) model of pRCC carrying an activating mutation of MET and tested the ability of cabozantinib, an inhibitor of receptor tyrosine kinases including MET, to inhibit tumor growth and metastasis. Precision-cut, thin tissue slices from a pRCC specimen obtained by nephrectomy were implanted under the renal capsule of RAG2(-/-)γC(-/-) mice to establish first generation TSG-RCC-030...
August 11, 2016: Cancer Biology & Therapy
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