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https://www.readbyqxmd.com/read/29778085/braf-and-mek-inhibitor-therapy-eliminates-nestin-expressing-melanoma-cells-in-human-tumors
#1
Deon B Doxie, Allison R Greenplate, Jocelyn S Gandelman, Kirsten E Diggins, Caroline E Roe, Kimberly B Dahlman, Jeffrey A Sosman, Mark C Kelley, Jonathan M Irish
Little is known about the in vivo impacts of targeted therapy on melanoma cell abundance and protein expression. Here, 21 antibodies were added to an established melanoma mass cytometry panel to measure 32 cellular features, distinguish malignant cells, and characterize dabrafenib and trametinib responses in BRAFV 600mut melanoma. Tumor cells were biopsied before neoadjuvant therapy and compared to cells surgically resected from the same site after 4 weeks of therapy. Approximately 50,000 cells per tumor were characterized by mass cytometry and computational tools t-SNE/viSNE, FlowSOM, and MEM...
May 19, 2018: Pigment Cell & Melanoma Research
https://www.readbyqxmd.com/read/29777202/aberrant-modulation-of-ribosomal-protein-s6-phosphorylation-confers-acquired-resistance-to-mapk-pathway-inhibitors-in-braf-mutant-melanoma
#2
Ming-Zhao Gao, Hong-Bin Wang, Xiang-Ling Chen, Wen-Ting Cao, Li Fu, Yun Li, Hai-Tian Quan, Cheng-Ying Xie, Li-Guang Lou
BRAF and MEK inhibitors have shown remarkable clinical efficacy in BRAF-mutant melanoma; however, most patients develop resistance, which limits the clinical benefit of these agents. In this study, we found that the human melanoma cell clones, A375-DR and A375-TR, with acquired resistance to BRAF inhibitor dabrafenib and MEK inhibitor trametinib, were cross resistant to other MAPK pathway inhibitors. In these resistant cells, phosphorylation of ribosomal protein S6 (rpS6) but not phosphorylation of ERK or p90 ribosomal S6 kinase (RSK) were unable to be inhibited by MAPK pathway inhibitors...
May 18, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29742076/update-on-hairy-cell-leukemia
#3
Robert J Kreitman, Evgeny Arons
Hairy cell leukemia (HCL) is a chronic B-cell malignancy with multiple treatment options, including several that are investigational. Patients present with pancytopenia and splenomegaly, owing to the infiltration of leukemic cells expressing CD22, CD25, CD20, CD103, tartrate-resistant acid phosphatase (TRAP), annexin A1 (ANXA1), and the BRAF V600E mutation. A variant lacking CD25, ANXA1, TRAP, and the BRAF V600E mutation, called HCLv, is more aggressive and is classified as a separate disease. A molecularly defined variant expressing unmutated immunoglobulin heavy variable 4-34 (IGHV4-34) is also aggressive, lacks the BRAF V600E mutation, and has a phenotype of HCL or HCLv...
March 2018: Clinical Advances in Hematology & Oncology: H&O
https://www.readbyqxmd.com/read/29741568/hemophagocytic-lymphohistiocytosis-associated-with-dabrafenib-and-trametinib-combination-therapy-following-pembrolizumab-administration-for-advanced-melanoma
#4
K Sasaki, J Uehara, S Iinuma, H Doi, M Honma, Y Toki, A Ishida-Yamamoto
No abstract text is available yet for this article.
May 7, 2018: Annals of Oncology: Official Journal of the European Society for Medical Oncology
https://www.readbyqxmd.com/read/29729495/braf-in-non-small-cell-lung-cancer-nsclc-pickaxing-another-brick-in-the-wall
#5
REVIEW
Alessandro Leonetti, Francesco Facchinetti, Giulio Rossi, Roberta Minari, Antonia Conti, Luc Friboulet, Marcello Tiseo, David Planchard
Molecular characterization of non-small cell lung cancer (NSCLC) marked an historical turning point for the treatment of lung tumors harboring kinase alterations suitable for specific targeted drugs inhibition, translating into major clinical improvements. Besides EGFR, ALK and ROS1, BRAF represents a novel therapeutic target for the treatment of advanced NSCLC. BRAF mutations, found in 1.5-3.5% of NSCLC, are responsible of the constitutive activation of mitogen activated protein kinase (MAPK)/extracellular signal-regulated kinase (ERK) pathway...
April 24, 2018: Cancer Treatment Reviews
https://www.readbyqxmd.com/read/29701552/recurrent-papillary-craniopharyngioma-with-braf-v600e-mutation-treated-with-dabrafenib-case-report
#6
Benjamin T Himes, Michael W Ruff, Jaimie J Van Gompel, Sean S Park, Evanthia Galanis, Timothy J Kaufmann, Joon H Uhm
The authors present the case of a man with a papillary craniopharyngioma, first diagnosed at 47 years of age, who experienced multiple recurrences. Review of the pathologic specimen from his first resection demonstrated the BRAF V600E mutation. With his most recent recurrence following previous surgery and radiotherapy, at 52 years of age, the decision was made to initiate treatment with the BRAF V600E inhibitor dabrafenib. Imaging following initiation of dabrafenib demonstrated reduction in tumor size. He remained on dabrafenib therapy for approximately 1 year and continued to demonstrate a good clinical result...
April 27, 2018: Journal of Neurosurgery
https://www.readbyqxmd.com/read/29662630/type-ii-raf-inhibitor-causes-superior-erk-pathway-suppression-compared-to-type-i-raf-inhibitor-in-cells-expressing-different-braf-mutant-types-recurrently-found-in-lung-cancer
#7
Amir Noeparast, Philippe Giron, Sylvia De Brakeleer, Carolien Eggermont, Ulrike De Ridder, Erik Teugels, Jacques De Grève
A large fraction of somatic driver BRAF mutations in lung cancer are non-V600 and impaired-kinase. Non-V600 BRAF mutations predict sensitivity to combination of a type I RAF inhibitor, Dabrafenib, and a MEK inhibitor, Trametinib. Singly, Dabrafenib only weakly suppresses mutant BRAF-induced ERK signaling and can induce ERK paradoxical activation in CRAF-overexpressing cells. The present study compared the effects of Dabrafenib and a type II RAF inhibitor, AZ628, on ERK activity in HEK293T cells expressing several tumor-derived BRAF mutants, and in a non-V600 and impaired-kinase BRAF-mutant lung cancer cell line (H1666)...
March 23, 2018: Oncotarget
https://www.readbyqxmd.com/read/29662327/spotlight-on-dabrafenib-trametinib-in-the-treatment-of-non-small-cell-lung-cancer-place-in-therapy
#8
REVIEW
Thomas C Weart, Kenneth D Miller, Charles B Simone
Advanced non-small-cell lung cancer (NSCLC) remains a challenging disease. The limited utility of chemotherapy indicates the need for additional therapeutic options. Targeted therapy continues to be an important tool in the treatment of NSCLC. Mutations within the RAS-RAF-MEK-MAPK pathway, specifically the BRAF V600E mutation, have become an important target for the subset of NSCLC patients with this mutation. This paper summarizes the clinical evidence that lead to the recent approval of the combination of dabrafenib and trametinib to treat patients with advanced NSCLC who harbor a BRAF V600E mutation...
2018: Cancer Management and Research
https://www.readbyqxmd.com/read/29650281/recent-developments-and-obstacles-in-the-treatment-of-melanoma-with-braf-and-mek-inhibitors
#9
REVIEW
Mohd Wahid, Arshad Jawed, Raju K Mandal, Sajad A Dar, Naseem Akhter, Pallavi Somvanshi, Farah Khan, Mohtashim Lohani, Mohammed Y Areeshi, Shafiul Haque
Metastatic melanoma is a least common form of cancer as it accounts only for 1% of all cancer cases. But, it is most deadly in nature and is haunting mankind for long emotionally as well as economically. The sites for the onset of the disease are pigment-producing cells of the skin, mucosa, eye etc. It has the potential to spread other sites like subcutaneous tissue, lymph nodes, lungs, liver, bone and brain. The United States Food & Drug Administration has approved various drug molecules from time to time...
May 2018: Critical Reviews in Oncology/hematology
https://www.readbyqxmd.com/read/29621181/dabrafenib-treatment-in-a-patient-with-an-epithelioid-glioblastoma-and-braf-v600e-mutation
#10
Garry Ceccon, Jan-Michael Werner, Veronika Dunkl, Caroline Tscherpel, Gabriele Stoffels, Anna Brunn, Martina Deckert, Gereon R Fink, Norbert Galldiks
Novel therapeutic targets in malignant glioma patients are urgently needed. Point mutations of the v-Raf murine sarcoma viral oncogene homolog B ( BRAF ) gene occur predominantly in melanoma patients, but may also occur in gliomas. Thus, this is a target of great interest for this group of patients. In a nine-year-old male patient, an anaplastic astrocytoma in the left temporoparietal region was diagnosed histologically. After first- and second-line treatment, a malignant progression to a secondary glioblastoma was observed ten years after the initial diagnosis...
April 5, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29617934/steroid-refractory-dermatomyositis-following-combination-dabrafenib-and-trametinib-therapy
#11
Stephanie R Harrison, Alice Tew, Neil Steven, Benjamin A Fisher
No abstract text is available yet for this article.
March 30, 2018: Rheumatology
https://www.readbyqxmd.com/read/29595366/dabrafenib-in-combination-with-trametinib-in-the-treatment-of-patients-with-braf-v600-positive-advanced-or-metastatic-non-small-cell-lung-cancer-clinical-evidence-and-experience
#12
Arjun Khunger, Monica Khunger, Vamsidhar Velcheti
Mutations in the BRAF oncogene are found in 2-4% of all non-small cell lung cancer (NSCLC) patients. The most common activating mutation present within the BRAF oncogene is associated with valine substitution for glutamate at position 600 (V600E) within the BRAF kinase. BRAF-targeted therapies are effective in patients with melanoma and NSCLC harboring BRAF V600E mutation. In both melanoma and NSCLC, dual inhibition of both BRAF and the downstream mitogen-activated protein kinase (MEK) improves response rates compared with BRAF inhibition alone...
January 2018: Therapeutic Advances in Respiratory Disease
https://www.readbyqxmd.com/read/29580759/uveitis-and-serous-retinal-detachment-secondary-to-systemic-dabrafenib-and-trametinib
#13
T Rueda-Rueda, J L Sánchez-Vicente, A Moruno-Rodríguez, F E Molina-Socola, A C Martínez-Borrego, F López-Herrero
CASE REPORT: The case is presented of a 39-year-old woman with metastatic melanoma treated with dabrafenib and trametinib. She presented with a severe acute panuveitis with granulomatous anterior uveitis, vitritis, and multiple serous retinal detachments. Dabrafenib and trametinib were suspended, and treatment with a systemic and topical corticosteroid was started. A good response was obtained, with a recovery of visual acuity of 1.0 in both eyes within two weeks. DISCUSSION: Dabrafenib and trametinib can lead to severe uveitis...
March 23, 2018: Archivos de la Sociedad Española de Oftalmología
https://www.readbyqxmd.com/read/29574693/physiologically-based-pharmacokinetic-modelling-to-identify-physiological-and-molecular-characteristics-driving-variability-in-drug-exposure
#14
Andrew Rowland, Madelé van Dyk, Ashley M Hopkins, Reham Mounzer, Thomas M Polasek, Amin Rostami-Hodjegan, Michael J Sorich
Prospectively defining the physiological and molecular characteristics most likely driving between subject variability (BSV) in drug exposure provides the opportunity to inform the assessment of biomarkers to account for this variability. A physiologically-based pharmacokinetic (PBPK) model was constructed and verified for dabrafenib. This model was then used to evaluate the physiological and molecular characteristics driving BSV in dabrafenib exposure. The capacity to discriminate a steady state dabrafenib trough concentration >48ng/mL was also evaluated...
March 25, 2018: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29568360/methotrexate-sensitizes-drug-resistant-metastatic-melanoma-cells-to-braf-v600e-inhibitors-dabrafenib-and-encorafenib
#15
Kayleigh C Ross, Kevin F Chin, Daehwan Kim, Christopher D Marion, Timothy J Yen, Vikram Bhattacharjee
Acquired resistance of metastatic melanoma (MM) tumors to BRAF V600E inhibitors (BRAFi's) is commonplace in the clinic. Habitual relapse of patients contributes to <20% 5-year survival rates in MM. We previously identified serine synthesis as a critical detrminant of late-stage cancer cell resistance to BRAFi's. Pre-treatment with DNA damaging agent gemcitabine (a nucleoside analog) re-sensitized drug-resistant cancer cells to BRAFi's dabrafenib and vemurafenib. Importantly, the combination treatments were effective against BRAF wild type cancer cells potentially expanding the clinical reach of BRAFi's...
March 2, 2018: Oncotarget
https://www.readbyqxmd.com/read/29561296/potential-clinical-and-immunotherapeutic-utility-of-talimogene-laherparepvec-for-patients-with-melanoma-after-disease-progression-on-immune-checkpoint-inhibitors-and-braf-inhibitors
#16
Jason Chesney, Yoannis Imbert-Fernandez, Sucheta Telang, Mary Baum, Smita Ranjan, Mostafa Fraig, Nicolas Batty
Talimogene laherparepvec is a genetically modified herpes simplex virus type 1-based oncolytic immunotherapy for the local treatment of unresectable subcutaneous and nodal tumors in patients with melanoma recurrent after initial surgery. We report on two patients with melanoma who, after progression on numerous systemic therapies, derived clinical benefit from talimogene laherparepvec in an expanded-access protocol (ClinicalTrials.gov, NCT02147951). Intralesional talimogene laherparepvec (day 1, ≤4 ml 10 PFU/ml; after 3 weeks, ≤4 ml 10 PFU/ml every 2 weeks) was administered until complete response, no injectable tumors, progressive disease, or intolerance occurred...
March 21, 2018: Melanoma Research
https://www.readbyqxmd.com/read/29557374/dabrafenib-an-inhibitor-of-rip3-kinase-dependent-necroptosis-reduces-ischemic-brain-injury
#17
Shelly A Cruz, Zhaohong Qin, Alexandre F R Stewart, Hsiao-Huei Chen
Ischemic brain injury triggers neuronal cell death by apoptosis via caspase activation and by necroptosis through activation of the receptor-interacting protein kinases (RIPK) associated with the tumor necrosis factor-alpha (TNF-α)/death receptor. Recent evidence shows RIPK inhibitors are neuroprotective and alleviate ischemic brain injury in a number of animal models, however, most have not yet undergone clinical trials and safety in humans remains in question. Dabrafenib, originally identified as a B-raf inhibitor that is currently used to treat melanoma, was later revealed to be a potent RIPK3 inhibitor at micromolar concentrations...
February 2018: Neural Regeneration Research
https://www.readbyqxmd.com/read/29544202/quantification-of-the-next-generation-oral-anti-tumor-drugs-dabrafenib-trametinib-vemurafenib-cobimetinib-pazopanib-regorafenib-and-two-metabolites-in-human-plasma-by-liquid-chromatography-tandem-mass-spectrometry
#18
Evelina Cardoso, Thomas Mercier, Anna Dorothea Wagner, Krisztian Homicsko, Olivier Michielin, Kim Ellefsen-Lavoie, Laurène Cagnon, Manuel Diezi, Thierry Buclin, Nicolas Widmer, Chantal Csajka, Laurent Decosterd
A sensitive and selective method of high performance liquid chromatography (HPLC) coupled to tandem mass spectrometry (MS/MS) has been developed for the simultaneous quantification of six anticancer protein kinase inhibitors (PKIs), dabrafenib, trametinib, vemurafenib, cobimetinib, pazopanib, regorafenib, and two active metabolites (regorafenib-M2 and regorafenib-M5) in human plasma. Plasma protein precipitation with methanol enables the sample extraction of 100 μL aliquot of plasma. Analytes are detected by electrospray triple-stage quadrupole mass spectrometry and quantified using the calibration curves with stable isotope-labeled internal standards...
April 15, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29534162/braf-and-egfr-inhibitors-synergize-to-increase-cytotoxic-effects-and-decrease-stem-cell-capacities-in-braf-v600e-mutant-colorectal-cancer-cells
#19
Zhenhua Wu, Mingzhu Huang, Yiwei Gong, Chen Lin, Weijian Guo
Mutations in the oncogene BRAF(V600E) are found in ~10% of colorectal cancers (CRCs) and are associated with poor prognosis. However, BRAF(V600E) has a limited response to the small-molecule drug, vemurafenib, a BRAF inhibitor, and BRAF inhibition is thought to cause a feedback activation of EGFR signaling that supports continued proliferation. In this study, we explored the effect of combined use of dabrafenib, a BRAF inhibitor, and cetuximab, an EGFR inhibitor, on BRAF(V600E)-mutant CRC stem cells and its possible mechanisms...
April 1, 2018: Acta Biochimica et Biophysica Sinica
https://www.readbyqxmd.com/read/29526130/fatherhood-during-dabrafenib-and-trametinib-therapy-for-metastatic-melanoma
#20
Emilia Cocorocchio, Laura Pala, Angelo Battaglia, Sara Gandini, Fedro Alessandro Peccatori, Pier Francesco Ferrucci
No abstract text is available yet for this article.
March 11, 2018: Acta Oncologica
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