Difference between revisions of "Vemurafenib (Zelboraf)"

Revision as of 22:58, 8 January 2020

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

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."
- Limitation: vemurafenib "is not recommended for use in patients with wild-type BRAF melanoma."
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

[insert-1] 1.0 ^1.1 Vemurafenib (Zelboraf) package insert

[2] Vemurafenib (Zelboraf) package insert (locally hosted backup)

[3] Zelboraf manufacturer's website

[4] Vemurafenib (Zelboraf) patient drug information (UpToDate)

[1]

[2]

[3]

[4]

@@ Line 21: / Line 21: @@
 ==History of changes in FDA indication==
-*8/17/2011: Initial FDA approval "for the treatment of patients with unresectable or metastatic [[Melanoma,_BRAF-mutated|melanoma with BRAFV600E mutation]] as detected by an FDA-approved test."
+*8/17/2011: Initial FDA approval "for the treatment of patients with unresectable or metastatic [[Melanoma|melanoma]] with [[BRAF]] V600E [[Biomarkers#mutation|mutation]] as detected by an FDA-approved test."
-** Limitation: vemurafenib "is '''not recommended''' for use in patients with [[Melanoma|wild-type BRAF melanoma]]."
+** Limitation: vemurafenib "is '''not recommended''' for use in patients with [[Biomarkers#wilt-type|wild-type]] [[Biomarkers#BRAF|BRAF]] [[Melanoma|melanoma]]."
-*11/6/2017: Granted regular FDA approval "for the treatment of patients with [[Erdheim-Chester disease|Erdheim-Chester Disease (ECD) with BRAF V600 mutation]]."
+*11/6/2017: Granted regular FDA approval "for the treatment of patients with [[Erdheim-Chester disease|Erdheim-Chester Disease (ECD)]] with [[Biomarkers#BRAF|BRAF]] V600 [[Biomarkers#Mutation|mutation]]."
 ==Also known as==