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 CRAF, 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 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
- 8/17/2011: Initial FDA approval "for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test."
- 11/6/2017: Granted regular FDA approval "for the treatment of patients with Erdheim-Chester Disease (ECD) with BRAF V600 mutation."
Also known as
- Code names: PLX4032, RG7204, RO5185426
- Brand name: Zelboraf
References
- Drugs
- Oral medications
- Mutation-specific medications
- Kinase inhibitors
- BRAF inhibitors
- MAP2K4 inhibitors
- MAP3K20 inhibitors
- MAP4K5 inhibitors
- BRAF 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