OnCo
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Vemurafenib

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.

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Vemurafenib
PubChem
Mechanism, step by step
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1.Vemurafenib enters the cell and binds the ATP pocket of mutant BRAF V600E

Modality
Small-molecule kinase inhibitor (BRAF V600)
Mechanism
ATP-competitive inhibitor of BRAF V600 monomers; paradoxically activates wild-type RAF dimers, hence MEK partnering.
Brand / code
Zelboraf
Dosing & schedule
Route
Oral
Schedule
960 mg twice daily continuously
Dose modifications
Dose reduction for grade 2-3 rash, arthralgia, photosensitivity, QT prolongation
Monitoring
Dermatology exams for squamous cell carcinoma; ECG; liver enzymes

Source: www.accessdata.fda.gov/drugsatfda_docs/label/2020/202429s019lbl.pdf. Doses are for orientation; the current label governs.

Medicare
Part D (self-administered)

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).

Commercial insurance
covered with prior authorisation

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.

Assistance programmes

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.

NICE recommendedNICE TA269 · 2012SMC: accepted
Appraised for
BRAF V600 mutation-positive unresectable or metastatic melanoma
NHS England
Routinely funded for the appraised indication (or via managed access)

Sources: NICE TA269 · SMC advice: vemurafenib. Funding decisions are indication-specific and change monthly; verify with NICE and your treating team.

Regulatory

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  1. 17 Aug 2011ApprovalUS

    Approved with the cobas BRAF V600 companion test, the first melanoma targeted therapy

  2. 10 Nov 2015ApprovalUS

    Cobimetinib approved in combination (coBRIM)

Approvals

RegionYearIndication
US2011Unresectable or metastatic BRAF V600E melanoma
US2017Erdheim-Chester disease with BRAF V600 mutation

Safety

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Toxicity profile
Adverse eventAny gradeGrade 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.

Trials

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ClinicalTrials.gov · phase 2/3
refreshed 2026-09-09
100 studies17 recruiting89 Phase 214 Phase 3
Search “Vemurafenib” on ClinicalTrials.gov →
Counts are from a name search and may include unrelated studies; up to 100 studies are summarised.

Recruiting now (live from ClinicalTrials.gov)

Recruiting trials near you · live from ClinicalTrials.gov
Vemurafenib
intervention: Vemurafenib
Open on ClinicalTrials.gov →

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Landmark trials in OnCo

Latest papers

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Literature trend115 papers in the last 12 months-12% vs prior 12How this is computed
Latest papers · live from Europe PMC
Open in Europe PMC

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.

Connected

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