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https://www.readbyqxmd.com/read/28426905/acantholytic-dyskeratotic-acanthoma-a-possible-skin-adverse-event-of-vemurafenib-treatment
#1
Takaya Komori, Atsushi Otsuka, Yo Kaku, Tetsuya Honda, Kenji Kabashima
Acantholytic dyskeratotic acanthoma (ADA) is a solitary small papule that is pathologically characterized by dyskeratosis with acantholytic acanthosis (1). Vemulafenib is a specific inhibitor of BRAF protein kinase with V600E mutation and is administered to treat metastatic melanoma. Various skin adverse events associated with vemurafenib, including acantholysis and flare up of Darier's disease, have been reported (2, 3). Here we report a case of ADA that developed during vemulafenib treatment for metastatic melanoma...
April 20, 2017: Journal of the European Academy of Dermatology and Venereology: JEADV
https://www.readbyqxmd.com/read/28423208/combined-activity-of-temozolomide-and-the-mtor-inhibitor-temsirolimus-in-metastatic-melanoma-involves-dkk1
#2
Heike Niessner, Corinna Kosnopfel, Tobias Sinnberg, Daniela Beck, Kathrin Krieg, Ines Wanke, Konstantinos Lasithiotakis, Michael Bonin, Claus Garbe, Friedegund Meier
The BRAFV600E inhibitor vemurafenib achieves remarkable clinical responses in patients with BRAF-mutant melanoma, but its effects are limited by the onset of drug resistance. In the case of resistance, chemotherapy can still be applied as second line therapy. However, it yields low response rates and strategies are urgently needed to potentiate its effects. In a previous study, we showed that the inhibition of the PI3K-AKT-mTOR pathway significantly increases sensitivity of melanoma cells to chemotherapeutic drugs (1)...
April 19, 2017: Experimental Dermatology
https://www.readbyqxmd.com/read/28418885/development-of-11c-vemurafenib-employing-a-carbon-11-carbonylative-stille-coupling-and-preliminary-evaluation-in-mice-bearing-melanoma-tumor-xenografts
#3
Paul Slobbe, Albert D Windhorst, Kevin Adamzek, Marije Bolijn, Robert C Schuit, Daniëlle A M Heideman, Guus A M S van Dongen, Alex J Poot
Over the last decade kinase inhibitors have witnessed tremendous growth as anti-cancer drugs. Unfortunately, despite their promising clinical successes, a large portion of patients does not benefit from these targeted therapeutics. Vemurafenib is a serine/threonine kinase inhibitor approved for the treatment of melanomas specifically expressing the BRAFV600E mutation. The aim of this study was to develop vemurafenib as PET tracer to determine its potential for identification of tumors sensitive to vemurafenib treatment...
March 17, 2017: Oncotarget
https://www.readbyqxmd.com/read/28415756/human-melanoma-cells-resistant-to-mapk-inhibitors-can-be-effectively-targeted-by-inhibition-of-the-p90-ribosomal-s6-kinase
#4
Corinna Kosnopfel, Tobias Sinnberg, Birgit Sauer, Heike Niessner, Anja Schmitt, Elena Makino, Andrea Forschner, Stephan Hailfinger, Claus Garbe, Birgit Schittek
The clinical availability of small molecule inhibitors specifically targeting mutated BRAF marked a significant breakthrough in melanoma therapy. Despite a dramatic anti-tumour activity and improved patient survival, rapidly emerging resistance, however, greatly limits the clinical benefit. The majority of the already described resistance mechanisms involve a reactivation of the MAPK signalling pathway. The p90 ribosomal S6 kinase (RSK), a downstream effector of the MAPK signalling cascade, has been reported to enhance survival of melanoma cells in response to chemotherapy...
March 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28414204/docking-based-structural-splicing-and-reassembly-strategy-to-develop-novel-deazapurine-derivatives-as-potent-b-raf-v600e-inhibitors
#5
Gui-Min Wang, Xiang Wang, Jian-Ming Zhu, Bin-Bin Guo, Zhuo Yang, Zhi-Jian Xu, Bo Li, He-Yao Wang, Ling-Hua Meng, Wei-Liang Zhu, Jian Ding
The mutation of B-Raf(V600E) is widespread in a variety of human cancers. Its inhibitors vemurafenib and dabrafenib have been launched as drugs for treating unresectable melanoma, demonstrating that B-Raf(V600E) is an ideal drug target. This study focused on developing novel B-Raf(V600E) inhibitors as drug leads against various cancers with B-Raf(V600E) mutation. Using molecular modeling approaches, 200 blockbuster drugs were spliced to generate 283 fragments followed by molecular docking to identify potent fragments...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28412197/an-uplc-ms-ms-method-for-the-quantification-of-braf-inhibitors-vemurafenib-dabrafenib-and-mek-inhibitors-cobimetinib-trametinib-binimetinib-in-human-plasma-application-to-treated-melanoma-patients
#6
Marine Rousset, Karine Titier, Stephane Bouchet, Caroline Dutriaux, Anne Pham-Ledard, Sorilla Prey, Mireille Canal-Raffin, Mathieu Molimard
Targeted therapies for cancers are fast-growing therapies. For instance kinase inhibitors such as BRAF inhibitors (BRAFi) and MEK inhibitors (MEKi) are increasingly used to treat malignant melanoma. The metabolic profile of these drugs can result in great interindividual variability, justifying therapeutic drug monitoring (TDM). We describe a rapid and specific method for quantification of 2 BRAFi (vemurafenib, dabrafenib) and 3 MEKi (cobimetinib, trametinib and binimetinib). Chromatography was performed on a Waters Acquity-UPLC system with CORTECS C18+ column, under a gradient of 10% acetic acid in water/acetonitrile...
April 12, 2017: Clinica Chimica Acta; International Journal of Clinical Chemistry
https://www.readbyqxmd.com/read/28405510/correlation-between-previous-treatment-with-braf-inhibitors-and-clinical-response-to-pembrolizumab-in-patients-with-advanced-melanoma
#7
Ester Simeone, Antonio Maria Grimaldi, Lucia Festino, Diana Giannarelli, Vito Vanella, Marco Palla, Marcello Curvietto, Assunta Esposito, Giuseppe Palmieri, Nicola Mozzillo, Paolo Antonio Ascierto
The optimal sequencing of targeted treatment and immunotherapy in the treatment of advanced melanoma is a key question and prospective studies to address this are ongoing. Previous observations suggest that treating first with targeted therapy may select for more aggressive disease, meaning that patients may not gain full benefit from subsequent immunotherapy. In a single-center retrospective analysis, we investigated whether response to pembrolizumab was affected by previous BRAF inhibitor therapy. A total of 42 patients with metastatic cutaneous or mucosal melanoma who had received previous treatment with ipilimumab were treated with pembrolizumab as part of the Italian expanded access program...
2017: Oncoimmunology
https://www.readbyqxmd.com/read/28396940/adjunction-of-a-mek-inhibitor-to-vemurafenib-in-the-treatment-of-metastatic-melanoma-results-in-a-60-reduction-of-acute-kidney-injury
#8
Cécile Teuma, Solenne Pelletier, Mona Amini-Adl, Marie Perier-Muzet, Delphine Maucort-Boulch, Luc Thomas, Maurice Laville, Denis Fouque, Stéphane Dalle
INTRODUCTION: A combined therapy MEK inhibitor, Cobimetinib (CB) and BRAF inhibitor, Vemurafenib (VMF), results in an improvement in progression-free survival among patients with BRAF V600-mutated metastatic melanoma. VMF skin adverse effects attributed to ERK paradoxical activation are decreased by the adjunction of CB. The aim of this study was to determine if this combination also improved the renal side effects of VMF. PATIENTS AND METHODS: To investigate the incidence of acute kidney injury (AKI), we conducted a retrospective observational monocentric study in Lyon Sud University Hospital in France...
April 10, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28388658/the-prognostic-significance-of-dapk1-in-bladder-cancer
#9
Jian-Yun Xie, Peng-Chen Chen, Jia-Li Zhang, Ze-Shou Gao, Henrique Neves, Shu-Dong Zhang, Qing Wen, Wei-Dong Chen, Hang Fai Kwok, Yao Lin
Bladder cancer is one of the leading causes of cancer-related death in men, however, there was only limited effective treatment for invasive bladder cancer. DAPK1 has been shown to play important role in apoptosis and autophagy to suppress cancer progression. Previous results have shown that DAPK1 promoter was hypermethylated in the majority of bladder cancer specimens, however, the prognostic significance of DAPK1 in bladder cancer has yet to be demonstrated. In the present study, we found that DAPK1 expression was negatively associated with tumor stage and a low level expression of DAPK1 in bladder cancer specimens were associated with shorter survival in bladder cancer patients in 3 independent bladder cancer datasets (n = 462)...
2017: PloS One
https://www.readbyqxmd.com/read/28387097/-new-paradigms-and-metaphors-in-cutaneous-melanoma-treatment
#10
REVIEW
G E Piérard, J L Nizet, P Humbert
In recent years, new drugs have been designed for treating advanced cutaneous malignant melanoma, in particular the metastases. They afford modest benefits despite the fact they are commonly heralded as breakthroughs in the lay press and by some medical opinion leaders. Unfortunately, the use of inflated descriptors of the drug efficacy leads to misunderstandings among the clinicians in charge of patients. Currently, vemurafenib, ipilimumab, pembrolizumab and nivolumab have demonstrated their relative activity in the control of advanced malignant melanoma...
December 2016: Revue Médicale de Liège
https://www.readbyqxmd.com/read/28382170/obatoclax-and-ly3009120-efficiently-overcome-vemurafenib-resistance-in-differentiated-thyroid-cancer
#11
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 BRAF(V600E) mutation, Vemurafenib, a BRAF kinase inhibitor, has dramatically changed the therapeutic landscape, but side effects and drug resistance often lead to termination of the single agent treatment. In the present study, we showed that either LY3009120 or Obatoclax (GX15-070) efficiently inhibited cell cycle progression and induced massive death of DTC cells...
2017: Theranostics
https://www.readbyqxmd.com/read/28376906/braf-v600e-expression-in-histiocytic-sarcoma-associated-with-splenic-marginal-zone-lymphoma-a-case-report
#12
John L Vaughn, C Eric Freitag, Jessica A Hemminger, Jeffrey A Jones
BACKGROUND: Histiocytic sarcoma is a rare histiocytic neoplasm of unknown etiology that constitutes less than 1% of hematologic malignancies. A few cases of histiocytic sarcoma harboring the BRAF (V600E) mutation have been reported, but this finding has not been confirmed in all studies. CASE PRESENTATION: We report the case of a 63-year-old white woman with a history of splenic marginal zone lymphoma who presented with 2 weeks of right-sided neck swelling. Positron emission tomography revealed an intensely hypermetabolic and destructive soft tissue mass in her right skull base...
April 5, 2017: Journal of Medical Case Reports
https://www.readbyqxmd.com/read/28376479/metastatic-melanoma-treatment-and-survival-in-the-us-after-the-introduction-of-ipilimumab-and-vemurafenib
#13
Lindsey Enewold, Elad Sharon, Linda C Harlan
INTRODUCTION: The 5-year survival of metastatic melanoma is < 18%. Historically, treatment options were limited. In 2011, 2 new agents were approved. METHODS: We re-abstracted the medical records of a random sample (n = 520) of metastatic melanoma patients who had been diagnosed in 2011 and reported to population-based registries in the U.S. We also queried their treating physicians. Factors associated with treatment and survival were assessed using logistic and Cox proportional hazards regressions, respectively...
2017: Oncology Research and Treatment
https://www.readbyqxmd.com/read/28370562/vitamin-c-at-high-concentrations-induces-cytotoxicity-in-malignant-melanoma-but-promotes-tumor-growth-at-low-concentrations
#14
Guang Yang, Yao Yan, Younan Ma, Yixin Yang
Vitamin C has been used in complementary and alternative medicine for cancers regardless of its ineffectiveness in clinical trials and the paradoxical effects antioxidants have on cancer. Vitamin C was found to induce cytotoxicity against cancers. However, the mechanisms of action have not been fully elucidated, and the effects of vitamin C on human malignant melanoma have not been examined. This study revealed that vitamin C at millimolar concentrations significantly reduced the cell viability as well as invasiveness, and induced apoptosis in human malignant melanoma cells...
March 30, 2017: Molecular Carcinogenesis
https://www.readbyqxmd.com/read/28368402/sox2-is-not-required-for-melanomagenesis-melanoma-growth-and-melanoma-metastasis-in-vivo
#15
V Cesarini, E Guida, F Todaro, S Di Agostino, V Tassinari, S Nicolis, R Favaro, S Caporali, P M Lacal, E Botti, A Costanzo, P Rossi, E A Jannini, S Dolci
Melanoma is a dangerous form of skin cancer derived from the malignant transformation of melanocytes. The transcription factor SOX2 is not expressed in melanocytes, however, it has been shown to be differentially expressed between benign nevi and malignant melanomas and to be essential for melanoma stem cell maintenance and expansion in vitro and in xenograft models. By using a mouse model in which BRaf(V600E) mutation cooperates with Pten loss to induce the development of metastatic melanoma, we investigated if Sox2 is required during the process of melanomagenesis, melanoma growth and metastasis and in the acquisition of resistance to BRAF inhibitors (BRAFi) treatments...
April 3, 2017: Oncogene
https://www.readbyqxmd.com/read/28368067/rational-design-synthesis-and-biological-evaluation-of-pan-raf-inhibitors-to-overcome-resistance
#16
Lu Wang, Gaoyuan Zhu, Qing Zhang, Chunqi Duan, Yanmin Zhang, Zhimin Zhang, Yujun Zhou, Tao Lu, Weifang Tang
Selective BRaf(V600E) inhibitors with DFG-in conformation have been proven effective against a subset of melanoma. However, representative inhibitor vemurafenib rapidly acquires resistance in the BRaf(WT) cells through a CRaf or BRaf(WT) dependent manner. Simultaneous targeting of all subtypes of Raf proteins offers the prospect of enhanced efficacy as well as reduced potential for acquired resistance. Herein, we describe the design and characterization of a series of compounds I-01-I-22, based on a pyrimidine scaffold with DFG-out conformation as Pan-Raf inhibitors...
April 18, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28365424/drug-nanocarriers-for-cancer-chemotherapy-based-on-microemulsions-the-case-of-vemurafenib-analog-plx4720
#17
Ioanna Theochari, Maria Goulielmaki, Dganit Danino, Vassiliki Papadimitriou, Alexandros Pintzas, Aristotelis Xenakis
Oil-in-water (O/W) microemulsions based on Tween 80 as the emulsifier and triacetin as the dispersed oil phase were formulated to be used as delivery vehicles of Vemurafenib analog PLX4720. PLX4720 is a lipophilic antitumor drug against various cancer types correlated with the BRAF(V600E) mutation. The limits of the single-phase region corresponding to O/W microemulsions as described by ternary phase diagrams were examined. Droplet size measurements determined by dynamic light scattering (DLS) showed mean droplet diameters equal to 10±0...
March 18, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28356222/neutrophil-to-lymphocyte-ratio-is-associated-with-outcome-during-ipilimumab-treatment
#18
Michael R Cassidy, Rachel E Wolchok, Junting Zheng, Katherine S Panageas, Jedd D Wolchok, Daniel Coit, Michael A Postow, Charlotte Ariyan
BACKGROUND: Ipilimumab (IPI) and BRAF inhibitors (BRAFi) improve survival in melanoma, but not all patients will benefit and toxicity can be significant. Pretreatment neutrophil to lymphocyte ratio (NLR) has been associated with outcome in IPI-treated patients, but has not been studied during treatment or in BRAFi-treated patients. METHODS: Using a prospectively maintained database, patients with unresectable stage III or IV melanoma treated with IPI or a BRAFi (vemurafenib or dabrafenib as monotherapy) from 2006 to 2011 were identified...
March 24, 2017: EBioMedicine
https://www.readbyqxmd.com/read/28353073/erratum-to-ongoing-response-in-braf-v600e-mutant-melanoma-after-cessation-of-intermittent-vemurafenib-therapy-a-case-report
#19
Andrew J Dooley, Avinash Gupta, Mark R Middleton
No abstract text is available yet for this article.
March 28, 2017: Targeted Oncology
https://www.readbyqxmd.com/read/28345133/second-primary-melanoma-on-a-patient-undergoing-vemurafenib-therapy-a-case-report
#20
Giuliana Onnis, Giuseppe Palmieri, Maria Antonietta Montesu, Rosanna Satta
BACKGROUND: Several side effects have been reported during treatment with vemurafenib, including multiple benign lesions and, less frequently, atypical melanocytic proliferations and second primary melanomas. METHODS: A 46-year-old man undergoing vemurafenib therapy for metastatic malignant melanoma was clinically and dermoscopically monitored using total-body mapping. RESULTS: During BRAF inhibitor (BRAFi) treatment, the patient developed atypical melanocytic lesions and particularly secondary primary melanoma...
March 26, 2017: International Journal of Dermatology
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