Vemurafenib (Zelboraf)

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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, 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

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