Vemurafenib (Zelboraf)
General information
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.[1][2][3]
Route: PO
Extravasation: n/a
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]
Diseases for which it is used
- BRAF-mutated colorectal cancer
- BRAF-mutated melanoma
- BRAF-mutated tumors (tissue-agnostic)
- Craniopharyngioma
- 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
References
- Drugs
- Oral medications
- Mutation-specific medications
- BRAF inhibitors
- MAP2K4 inhibitors
- MAP3K20 inhibitors
- MAP4K5 inhibitors
- RAF1 inhibitors
- Malignant solid neoplasm, BRAF-mutated medications
- Colorectal cancer medications
- Craniopharyngioma medications
- Erdheim-Chester disease medications
- Hairy cell leukemia medications
- Langerhans cell histiocytosis medications
- Melanoma medications
- Multiple myeloma medications
- Thyroid cancer medications
- FDA approved in 2011
- EMA approved in 2012
- Health Canada approved in 2012
- PMDA approved in 2014