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.
1.Vemurafenib enters the cell and binds the ATP pocket of mutant BRAF V600E
- 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
- Genentech Access Solutions
- Genentech Patient Foundation — Free medicine for eligible patients regardless of insurance type.
- PAN Foundation — Disease-specific co-pay and premium funds; open and closed funds change monthly.
- HealthWell Foundation
- CancerCare Co-Payment Assistance Foundation
- Patient Advocate Foundation Co-Pay Relief
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.
- 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.
- 17 Aug 2011ApprovalUS
Approved with the cobas BRAF V600 companion test, the first melanoma targeted therapy
- 10 Nov 2015ApprovalUS
Cobimetinib approved in combination (coBRIM)
Approvals
| 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.
Trials
topRecruiting now (live from ClinicalTrials.gov)
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Landmark trials in OnCo
Latest papers
topQuery 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.
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