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Zelboraf (vemurafenib)
Zelboraf blocks the activity of the B-raf protein, which is involved in cell growth and division.
Zelboraf (vemurafenib) is a small molecule kinase inhibitor developed by Hoffmann La Roche, targeting the serine/threonine-protein kinase B-raf. It was FDA-approved in 2011 for the treatment of malignant melanoma with a BRAF V600E mutation and Erdheim-Chester Disease. Zelboraf is a patented medication with no generic manufacturers available. Key safety considerations include potential skin reactions, photosensitivity, and increased risk of secondary cancers. As a kinase inhibitor, Zelboraf works by blocking the activity of the B-raf protein, which is involved in cell growth and division.
At a glance
| Generic name | vemurafenib |
|---|---|
| Sponsor | Hoffmann La Roche |
| Drug class | Kinase Inhibitor [EPC] |
| Target | Serine/threonine-protein kinase B-raf |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2011 |
| Annual revenue | 100 |
Mechanism of action
Vemurafenib is low molecular weight, orally available inhibitor of some mutated forms of BRAF serine- threonine kinase, including BRAF V600E. Vemurafenib also inhibits other kinases in vitro such as CRAF, ARAF, wild-type BRAF, SRMS, ACK1, MAP4K5, and FGR at similar concentrations. Some mutations in the BRAF gene including V600E result in constitutively activated BRAF proteins, which can cause cell proliferation in the absence of growth factors that would normally be required for proliferation. Vemurafenib has anti-tumor effects in cellular and animal models of melanomas with mutated BRAF V600E.
Approved indications
- Erdheim-Chester Disease
- Malignant Melanoma with BRAF V600E Mutation
Common side effects
- Arthralgia
- Rash maculo-papular
- Alopecia
- Fatigue
- Photosensitivity reaction
- Nausea
- Pruritus
- Skin papilloma
- Gamma-glutamyltransferase increased
- Hyperkeratosis
- Actinic keratosis
- Dry skin
Drug interactions
- High Risk QT Prolonging Agents
- P-glycoprotein Substrates
- amiodarone
- artemether
- clozapine
- disopyramide
- dronedarone
- droperidol
- pimozide
- tacrine
- theophylline
- thioridazine
Key clinical trials
- Phase II Trial of Vemurafenib and Sorafenib in Pancreatic Cancer (PHASE2)
- TAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer (PHASE2)
- Optimization of the Time and Dosage of Trametinib in BRAF Negative Juvenile Patients (PHASE2)
- Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR) (PHASE2)
- Optimization of the Time and Dosage of Vemurafenib in BRAF Positive Juvenile Patients With Refractory Histiocytosis (PHASE2)
- A Study of Vemurafenib and Obinutuzumab Compared to Cladribine and Rituximab in People With Hairy Cell Leukemia (HCL) (PHASE2)
- A Study to Evaluate the Efficacy and Safety of Multiple Targeted Therapies as Treatments for Participants With Non-Small Cell Lung Cancer (NSCLC) (PHASE2,PHASE3)
- A Study of Multiple Therapies in Biomarker-selected Participants With Resectable Stages IB-III Non-small Cell Lung Cancer (NSCLC) (PHASE2)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
| SEC EDGAR | Revenue + earnings |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Zelboraf CI brief — competitive landscape report
- Zelboraf updates RSS · CI watch RSS
- Hoffmann La Roche portfolio CI