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Vemurafenib was the first BRAF inhibitor (2011); it shrank melanomas in weeks and proved that a single mutation could be drugged in a solid tumour.
BRIM-3: OS benefit versus dacarbazine in BRAF V600E melanoma; approved August 2011 alongside ipilimumab in the same year that transformed the disease. Now used with cobimetinib (coBRIM) or displaced by encorafenib-binimetinib and dabrafenib-trametinib. Also approved for Erdheim-Chester disease. Photosensitivity, arthralgia, and cutaneous squamous cell carcinomas (from paradoxical MAPK activation in RAS-mutant keratinocytes) are characteristic.
ATP-competitive inhibitor of BRAF V600 monomers; paradoxically activates wild-type RAF dimers, hence MEK partnering. Connects to BRAF.
1.Vemurafenib enters the cell and binds the ATP pocket of mutant BRAF V600E
Source: www.accessdata.fda.gov/drugsatfda_docs/label/2020/202429s019lbl.pdf. Doses are for orientation; the current label governs.
Oral, self-administered, so it is a Part D drug: covered through a stand-alone Part D plan or Medicare Advantage drug benefit, usually on the specialty tier with 25 to 33% coinsurance until the annual cap ($2,000 in 2025, $2,100 in 2026).
Covered for FDA-labelled and NCCN-listed uses, but almost always behind prior authorisation confirming diagnosis, biomarker and line of therapy; dispensed through a specialty pharmacy.
Part D out-of-pocket capped at $2,000 (2025) / $2,100 (2026). Medicare patients cannot use manufacturer co-pay cards; charity funds (PAN, HealthWell, CancerCare) and the Extra Help subsidy are the routes.
Sources: Medicare.gov: Drug coverage (Part D) · Medicare.gov: Costs for Medicare drug coverage (annual out-of-pocket cap). Not medical or financial advice; verify with your plan.
Sources: NICE TA269 · SMC advice: vemurafenib. Funding decisions are indication-specific and change monthly; verify with NICE and your treating team.
Approved with the cobas BRAF V600 companion test, the first melanoma targeted therapy
Cobimetinib approved in combination (coBRIM)
| Region | Year | Indication |
|---|---|---|
| US | 2011 | Unresectable or metastatic BRAF V600E melanoma |
| US | 2017 | Erdheim-Chester disease with BRAF V600 mutation |
| Adverse event | Any grade | Grade 3+ |
|---|---|---|
| Cutaneous squamous cell carcinoma / keratoacanthoma | 24% | - |
| Arthralgia | 53% | - |
| Photosensitivity | 33% | - |
BRIM-3 vemurafenib arm. Rates read from the source. Blank cells mean the figure was not sourced, not that it is zero.
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The diagnostic and treatment rows on the Erdheim-Chester page follow these recommendations.
Vemurafenib rescues children with refractory BRAF-mutant multisystem LCH, but it controls rather than cures, and how to stop it safely is an open question.
Encorafenib-binimetinib is one of three standard BRAF-MEK doublets for advanced melanoma and is often chosen for its tolerability.
Erdheim-Chester disease with a BRAF V600E mutation is treated first with a BRAF inhibitor; the first targeted approval in any histiocytosis.
BRAF testing became mandatory in advanced melanoma and vemurafenib the first approved BRAF inhibitor; combination with MEK inhibitors soon replaced monotherapy.
Query for this drug: (TITLE:"Vemurafenib" OR ABSTRACT:"Vemurafenib" OR TITLE:"Zelboraf" OR ABSTRACT:"Zelboraf") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Vemurafenib, not a curated reading list.
Shares Keith T. Flaherty, Single-system Langerhans cell histiocytosis (bone, skin or one other organ), Multisystem Langerhans cell histiocytosis (with or without risk-organ involvement), Langerhans cell histiocytosis (LCH).
Shares COLUMBUS: encorafenib plus binimetinib versus vemurafenib or encorafenib in BRAF-mutant melanoma, COLUMBUS, Melanoma (KEGG map), BRAF V600E (and V600K).
Shares COLUMBUS: encorafenib plus binimetinib versus vemurafenib or encorafenib in BRAF-mutant melanoma, SWOG S1406, COLUMBUS, Melanoma (KEGG map).
Shares BRIM-3: improved survival with vemurafenib in melanoma with BRAF V600E mutation, coBRIM, COLUMBUS, BRAF.
Shares Erdheim-Chester disease: consensus recommendations for evaluation, diagnosis and treatment in the molecular era, Erdheim-Chester disease, Hairy cell leukaemia, Craniopharyngioma.
Shares Single-system Langerhans cell histiocytosis (bone, skin or one other organ), Multisystem Langerhans cell histiocytosis (with or without risk-organ involvement), Langerhans cell histiocytosis (LCH), Erdheim-Chester disease.
Shares Single-system Langerhans cell histiocytosis (bone, skin or one other organ), Erdheim-Chester disease, Erdheim-Chester disease, Rosai-Dorfman disease and other histiocytic neoplasms, Cobimetinib.
Shares coBRIM, COLUMBUS, BRAF V600-mutant melanoma, BRAF.