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Zelboraf

vemurafenib
BRAF Kinase Inhibitor FDA Approved 2011 Genentech / Roche
Route
Oral
Half-Life
57 hrs
FDA Approved
2011
Manufacturer
Genentech / Roche
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1. Indications and Usage

Melanoma: BRAF V600E unresectable/metastatic melanoma.
Erdheim-Chester disease: BRAF V600 mutation.

2. Dosage and Administration

960 mg orally twice daily.

3. Dosage Forms and Strengths

Tablets: 240 mg

4. Contraindications

None listed.

5. Warnings and Precautions
  • New Primary Malignancies: cuSCC ~24%.
  • QT Prolongation: Monitor ECGs.
  • Photosensitivity: Severe. Use sunscreen.
  • Embryo-Fetal Toxicity: Can cause fetal harm.
6. Adverse Reactions
Most Common Adverse Reactions

Arthralgia (53%), Alopecia (45%), Fatigue (38%), Rash (37%), Nausea (35%), Photosensitivity (33%), Diarrhea (28%), Skin Papilloma (21%)

Arthralgia
53%
Alopecia
45%
Fatigue
38%
Rash
37%
Nausea
35%
Photosensitivity
33%
Diarrhea
28%
Skin Papilloma
21%

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

7. Drug Interactions

CYP1A2 Substrates: Moderate inhibitor.
QTc Drugs: Avoid.

8. Use in Specific Populations
Pregnancy

Consult the full prescribing information for pregnancy-related considerations.

Lactation

Refer to prescribing information for lactation guidance.

Pediatric Use

Pediatric safety and efficacy information is detailed in the full label.

Hepatic/Renal Impairment

Dose modifications for organ impairment are specified in the complete prescribing information.

12. Clinical Pharmacology
Mechanism of Action

Selective BRAF V600E kinase inhibitor blocking constitutive MAPK pathway activation.

Pharmacokinetics

Tmax: ~3h. Protein binding: >99%. t½: ~57h. Feces 94%.

14. Clinical Studies

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

Pivotal Clinical Trials
Additional Resources
📋 All Zelboraf Trials on ClinicalTrials.gov ↗ 📚 PubMed: Zelboraf Clinical Trials ↗
FDA-Approved Tumor Types

Zelboraf has FDA-approved indications across the following cancer types covered on CancerDrugEvidence:

Melanoma
External Resources
📋 DailyMed Label ↗ 🏛️ FDA Drugs@FDA ↗ 🔬 ClinicalTrials.gov ↗ 📚 PubMed Pivotal Trials ↗
Important Notice: This page is intended as a navigational reference to the FDA-approved prescribing information for Zelboraf. It does not replace the full prescribing information. Healthcare professionals should consult the complete package insert available at DailyMed before making prescribing decisions. Patient-specific factors should always guide clinical decision-making.

Frequently Asked Questions

What is Zelboraf (vemurafenib) approved for?

Zelboraf (vemurafenib) is an FDA-approved oncology agent. Refer to the full prescribing information for complete indication details.

How is Zelboraf (vemurafenib) administered?

Refer to the full prescribing information for dosing schedules, administration instructions, and dose modifications.

How does Zelboraf (vemurafenib) work?

Selective BRAF V600E kinase inhibitor blocking constitutive MAPK pathway activation.

What are the most common side effects?

Arthralgia (53%), Alopecia (45%), Fatigue (38%), Rash (37%), Nausea (35%), Photosensitivity (33%), Diarrhea (28%), Skin Papilloma (21%) Arthralgia 53% Alopecia 45% Fatigue 38% Rash 37% Nausea 35% Photosensitivity 33% Diarrhea 28% Skin Papilloma 21%

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