Class/mechanism: Tyrosine kinase inhibitor of some mutated forms of BRAF serine/threonine
kinase, including BRAF V600E. Also has been observed to inhibit other tyrosine kinases such as RAF1, ARAF, wild-type BRAF, SRMS, ACK1, MAP4K5, and FGR. Certain BRAF mutations, such as V600E, result in constitutive activation of cell proliferation pathways and tumor growth.
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Diseases for which it is used
- BRAF-mutated colorectal cancer
- BRAF-mutated melanoma
- BRAF-mutated tumors (tissue-agnostic)
- Erdheim-Chester disease
- Hairy cell leukemia
- Langerhans cell histiocytosis
- Multiple myeloma
- Thyroid cancer
More drug information
History of changes in FDA indication
- 2011-08-17: Initial FDA approval for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation. (Based on BRIM2, BRIM-3, and MO25743)
- Limitation: vemurafenib is not recommended for use in patients with wild-type BRAF melanoma.
- 2017-11-06: Granted regular FDA approval for the treatment of patients with Erdheim-Chester Disease (ECD) with BRAF V600 mutation. (Based on VE-BASKET)
History of changes in EMA indication
- 2012-02-17: Initial authorization as Zelboraf. Zelboraf is indicated in monotherapy for the treatment of adult patients with BRAF-V600-mutation-positive unresectable or metastatic melanoma. (Based on BRIM-3)
History of changes in Health Canada indication
- 2012-02-15: Initial notice of compliance
History of changes in PMDA indication
- 2014-12-26: Initial approval for the treatment of unresectable malignant melanoma with BRAF mutation.
Also known as
- Code names: PLX-4032, RG-7204, RO-5185426
- Brand name: Zelboraf