Combined BRAF and MEK Inhibition in Melanoma with BRAF V600 Mutations
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Summary
Dabrafenib and trametinib were safely combined at full monotherapy doses, and the rate of pyrexia was increased with combination therapy, whereas the rate of proliferative skin lesions was nonsignificantly reduced.
- Type
- article
- Published
- 2012-09-29
- Cited by
- 2,699
- References
- 28
- Access
- Open access
- OpenAlex
- https://openalex.org/W2156078931
- Semantic Scholar
- https://api.semanticscholar.org/CorpusID:23993987
Keywords
Trametinib, Dabrafenib, Medicine, MAPK/ERK pathway, MEK inhibitor
References
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- Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma
- Activity of the MEK Inhibitor Trametinib (GSK1120212) in Advanced Melanoma in a Phase I, Dose-escalation Trial
- RAF inhibitors transactivate RAF dimers and ERK signaling in cells with wild-type BRAF
- MEK1 mutations confer resistance to MEK and B-RAF inhibition
- Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors.
- Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation
- RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)
- Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib.
- RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth
- Melanoma whole exome sequencing identifies V600EB-RAF amplification-mediated acquired B-RAF inhibitor resistance
- Acquired resistance to BRAF inhibitors mediated by a RAF kinase switch in melanoma can be overcome by co-targeting MEK and IGF-1R/PI3K
- Anaplastic Lymphoma Kinase Inhibition in Non–Small-Cell Lung Cancer
- RAF Inhibitor Dabrafenib (GSK2118436) is Active in Melanoma Brain Metastases, Multiple BRAF Genotypes and Diverse Cancers
- Inhibition of Mutated, Activated BRAF in Metastatic Melanoma
- The Mammalian MAPK/ERK Pathway Exhibits Properties of a Negative Feedback Amplifier
- Improved Survival with Vemurafenib in Melanoma with BRAF V600E Mutation
- Improved survival with MEK inhibition in BRAF-mutated melanoma.
- Kinase-Dead BRAF and Oncogenic RAS Cooperate to Drive Tumor Progression through CRAF
- Multinational study of the efficacy and safety of humanized anti-HER2 monoclonal antibody in women who have HER2-overexpressing metastatic breast cancer that has progressed after chemotherapy for metastatic disease.
Cited by
- Society for melanoma research and american heart association scientific sessions.
- Guidelines of care for the management of primary cutaneous melanoma. American Academy of Dermatology.
- A costly revolution for a subgroup of patients with metastatic melanoma
- Why is autophagy important for melanoma? Molecular mechanisms and therapeutic implications.
- Actionable mutations in muscle-invasive bladder cancer
- Detecting mechanisms of acquired BRAF inhibitor resistance in melanoma.
- Intralesional immunotherapy for melanoma
- Neoadjuvant treatment of melanoma: case reports and review
- Epidermal growth factor receptor signalling in keratinocyte biology: implications for skin toxicity of tyrosine kinase inhibitors
- Current options and future directions in the systemic treatment of metastatic melanoma.
- Role of the cystathionine γ lyase/hydrogen sulfide pathway in human melanoma progression
- Melanoma patient-derived xenografts accurately model the disease and develop fast enough to guide treatment decisions
- Immunotherapies and novel combinations: the focus of advances in the treatment of melanoma
- Aurora kinase B inhibition reduces the proliferation of metastatic melanoma cells and enhances the response to chemotherapy
- Evidence of synergy with combined BRAF-targeted therapy and immune checkpoint blockade for metastatic melanoma
- Dabrafenib and trametinib versus dabrafenib and placebo for Val600 BRAF-mutant melanoma: a multicentre, double-blind, phase 3 randomised controlled trial.
- Antitumor effect of pharmacologic ascorbate in the B16 murine melanoma model.
- Absence of RIPK3 predicts necroptosis resistance in malignant melanoma
- TARGETED THERAPY IN CANCER
- New therapeutic strategies for BRAF mutant colorectal cancers.
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- Abstract B056: Non-V600 BRAF mutations in melanoma: actionable targets for rational drug combinations