BRAF Biological Pathways Reviews
BRAF
94 kDa B-raf protein; B-raf 1; B-Raf proto-oncogene serine/threonine-protein kinase; BRAF1; BRAF1_HUMAN; Murine sarcoma viral (v-raf) oncogene homolog B1; p94; RAFB1; v-raf murine sarcoma viral oncogene homolog B
Oncogenic mutations in BRAF genes activate the RAF/MEK/ERK pathway, resulting in increased cell proliferation and resistance to apoptosis.1 BRAF mutations have been identified in 7% to 8% of all cancers.2 V600E is the most common activating mutations in BRAF and is associated with more aggressive cancer and worse prognosis.1,3
Understanding the Role of BRAF
This animation explains the role of the BRAF oncogene in the MAPK pathway and how mutations cause BRAF to function abnormally resulting in abnormal cell proliferation and division, and uncontrolled cell growth, in a cancerous manner.
Expression in Cancer
BRAF Inhibitors
BRAF inhibitors target and block BRAF proteins to slow and control the growth of cancer cells. This table outlines therapies targeting BRAF both approved by the FDA and in the pipeline.
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BRAF Inhibitors Approved by the FDA |
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Brand Name (Generic Drug Name) |
Indications |
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Zelboraf (vemurafenib)1 |
Treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test |
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Treatment of patients with Erdheim-Chester Disease with BRAF V600 mutation |
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Tafinlar (dabrafenib)2 |
Treatment as monotherapy for patients with unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test |
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Treatment in combination with trametinib for patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations as detected by an FDA-approved test |
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Treatment in combination with trametinib for the adjuvant treatment of patients with melanoma with BRAF V600E or V600K mutations, as detected by an FDA-approved test, and involvement of lymph node(s), following complete resection |
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Treatment in combination with trametinib for patients with metastatic NSCLC with BRAF V600E mutation as detected by an FDA-approved test |
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Treatment in combination with trametinib for patients with locally advanced or metastatic anaplastic thyroid cancer with BRAF V600E mutation and with no satisfactory locoregional treatment options |
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Treatment in combination with trametinib for adult and pediatric patients 6 years of age and older with unresectable or metastatic solid tumors with BRAF V600E mutation who have progressed following prior treatment and have no satisfactory alternative treatment options |
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Treatment in combination with trametinib for pediatric patients 1 year of age and older with low-grade glioma with a BRAF V600E mutation who require systemic therapy |
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Braftovi (encorafenib)3 |
Treatment in combination with binimetinib for patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test |
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Treatment in combination with cetuximab for adult patients with metastatic colorectal cancer with a BRAF V600E mutation, as detected by an FDA-approved test, after prior therapy |
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