نتایج جستجو برای: vemurafenib

تعداد نتایج: 1054  

Journal: :Cancer research 2015
A Kenneth MacLeod Lesley A McLaughlin Colin J Henderson C Roland Wolf

Vemurafenib is a revolutionary treatment for melanoma, but the magnitude of therapeutic response is highly variable, and the rapid acquisition of resistance is frequent. Here, we examine how vemurafenib disposition, particularly through cytochrome P450-mediated oxidation pathways, could potentially influence these outcomes using a panel of knockout and transgenic humanized mouse models. We iden...

2015
Wiebke Sondermann Klaus G. Griewank Bastian Schilling Elisabeth Livingstone Julia C. Leyh Natalia Rompoti Ioana Cosgarea Tobias Schimming Dirk Schadendorf Lisa Zimmer Uwe Hillen

We have previously demonstrated an impact of the BRAF inhibitor vemurafenib on patient lymphocyte counts. In the current study, the extent to which concomitant use of corticosteroids in BRAF inhibitor treated patients affects lymphocyte counts and predisposes to infection was investigated. A cohort of 102 patients receiving either the selective BRAF inhibitor vemurafenib or dabrafenib was analy...

2017
Wei-Jun Wei Zhen-Kui Sun Chen-Tian Shen Hong-Jun Song Xin-Yun Zhang Zhong-Ling Qiu Quan-Yong Luo

Although the prognosis of differentiated thyroid cancer (DTC) is relatively good, 30-40% of patients with distant metastases develop resistance to radioactive iodine therapy due to tumor dedifferentiation. For DTC patients harboring BRAFV600E mutation, Vemurafenib, a BRAF kinase inhibitor, has dramatically changed the therapeutic landscape, but side effects and drug resistance often lead to ter...

2017
Adil Daud Japinder Gill Sheily Kamra Lei Chen Amit Ahuja

BACKGROUND Metastatic melanoma is an aggressive form of skin cancer with a high mortality rate and the fastest growing global incidence rate of all malignancies. The introduction of BRAF/MEK inhibitor combinations has yielded significant increases in PFS and OS for melanoma. However, at present, no direct comparisons between different BRAF/MEK combinations have been conducted. In light of this,...

Journal: :Cancer research 2012
Hong Yang Brian Higgins Kenneth Kolinsky Kathryn Packman William D Bradley Richard J Lee Kathleen Schostack Mary Ellen Simcox Scott Kopetz David Heimbrook Brian Lestini Gideon Bollag Fei Su

The protein kinase BRAF is a key component of the RAS-RAF signaling pathway which plays an important role in regulating cell proliferation, differentiation, and survival. Mutations in BRAF at codon 600 promote catalytic activity and are associated with 8% of all human (solid) tumors, including 8% to 10% of colorectal cancers (CRC). Here, we report the preclinical characterization of vemurafenib...

2017
Daniel Bauer Felix Werth Ha An Nguyen Felix Kiecker Jürgen Eberle

Inhibition of MAP kinase pathways by selective BRAF inhibitors, such as vemurafenib and dabrafenib, have evolved as key therapies of BRAF-mutated melanoma. However, tumor relapse and therapy resistance have remained as major problems, which may be addressed by combination with other pathway inhibitors. Here we identified the potassium channel inhibitor TRAM-34 as highly effective in combination...

2015
Geoffrey T Gibney Geneviève Gauthier Charles Ayas Philip Galebach Eric Q Wu Sarang Abhyankar Carolina Reyes Annie Guérin Yeun Mi Yim

Brain metastases are a common and serious complication among patients with metastatic melanoma. The selective BRAF inhibitor vemurafenib has demonstrated clinical efficacy in patients with BRAF V600E-mutant melanoma brain metastases (MBM). We examined the real-world application and clinical outcomes of vemurafenib in this patient population. Demographic, treatment patterns, response, and surviv...

Journal: :Proceedings of the National Academy of Sciences of the United States of America 2017
Taral R Lunavat Lesley Cheng Berglind O Einarsdottir Roger Olofsson Bagge Somsundar Veppil Muralidharan Robyn A Sharples Cecilia Lässer Yong Song Gho Andrew F Hill Jonas A Nilsson Jan Lötvall

The BRAF inhibitors vemurafenib and dabrafenib can be used to treat patients with metastatic melanomas harboring BRAFV600 mutations. Initial antitumoral responses are often seen, but drug-resistant clones with reactivation of the MEK-ERK pathway soon appear. Recently, the secretome of tumor-derived extracellular vesicles (EVs) has been ascribed important functions in cancers. To elucidate the p...

2016
Selina K. Sutton Daniel R. Carter Patrick Kim Owen Tan Greg M. Arndt Xu Dong Zhang Jonathan Baell Benjamin D. Noll Shudong Wang Naresh Kumar Grant A. McArthur Belamy B. Cheung Glenn M. Marshall

There is an urgent need for better therapeutic options for advanced melanoma patients, particularly those without the BRAFV600E/K mutation. In melanoma cells, loss of TRIM16 expression is a marker of cell migration and metastasis, while the BRAF inhibitor, vemurafenib, induces melanoma cell growth arrest in a TRIM16-dependent manner. Here we identify a novel small molecule compound which sensit...

Journal: :Clinical cancer research : an official journal of the American Association for Cancer Research 2014
Geoffrey Kim Amy E McKee Yang-Min Ning Maitreyee Hazarika Marc Theoret John R Johnson Qiang Casey Xu Shenghui Tang Rajeshwari Sridhara Xiaoping Jiang Kun He Donna Roscoe W David McGuinn Whitney S Helms Anne Marie Russell Sarah Pope Miksinski Jeanne Fourie Zirkelbach Justin Earp Qi Liu Amna Ibrahim Robert Justice Richard Pazdur

On August 17, 2011, the U.S. Food and Drug Administration (FDA) approved vemurafenib tablets (Zelboraf, Hoffmann-LaRoche Inc.) for the treatment of patients with unresectable or metastatic melanoma with the BRAF(V600E) mutation as detected by an FDA-approved test. The cobas 4800 BRAF V600 Mutation Test (Roche Molecular Systems, Inc.) was approved concurrently. An international, multicenter, ran...

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