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General Medication Fact Sheet for Zelboraf
| Field | Information |
|---|---|
| Medication Name | Zelboraf |
| Generic Name | Vemurafenib |
| Boxed/Label Warning | New primary malignancies (cutaneous squamous cell carcinoma, keratoacanthoma) and other BRAF inhibitor toxicities. |
| Purpose | Treatment of melanoma with BRAF V600E mutation |
| Mechanism of Action | Inhibits the BRAF kinase, which is often mutated in melanoma cells, disrupting the MAPK signaling pathway |
| Dosage Forms | Oral tablets |
| Available Strengths | 240 mg |
| Dosage Frequency | Twice daily |
| Common Side Effects | Arthralgia, fatigue, rash, photosensitivity, alopecia, nausea |
| Serious Side Effects | Cutaneous squamous cell carcinoma, keratoacanthoma, QT prolongation, hypersensitivity reactions, uveitis |
| Drug Interactions | CYP1A2 inhibitors/inducers, CYP3A4 inhibitors/inducers, drugs that prolong QT interval |
| Important Notes | Avoid prolonged sun exposure; regular skin exams are crucial; report any new skin lesions immediately. Confirm BRAF V600E mutation prior to starting. |
| Storage | Store at room temperature away from moisture and light. |
| Missed Dose | Take the dose as soon as you remember, unless it is less than 4 hours until your next dose. Do not double the dose. |
| Alternatives | Dabrafenib, Trametinib, Cobimetinib, Ipilimumab, Pembrolizumab, Nivolumab |
Zelboraf Alternatives
| Medication | Mechanism of Action | Notes |
|---|---|---|
| Dabrafenib (Tafinlar) | BRAF inhibitor | Used in combination with Trametinib for BRAF V600E or V600K mutation-positive melanoma. |
| Trametinib (Mekinist) | MEK inhibitor | Used in combination with Dabrafenib or as a single agent for BRAF V600E or V600K mutation-positive melanoma. |
| Cobimetinib (Cotellic) | MEK inhibitor | Used in combination with vemurafenib for BRAF V600 mutation-positive melanoma. |
| Ipilimumab (Yervoy) | CTLA-4 inhibitor | Immunotherapy agent; blocks CTLA-4, enhancing T-cell activation and anti-tumor response. |
| Pembrolizumab (Keytruda) | PD-1 inhibitor | Immunotherapy agent; blocks PD-1, enhancing T-cell activation and anti-tumor response. |
| Nivolumab (Opdivo) | PD-1 inhibitor | Immunotherapy agent; blocks PD-1, enhancing T-cell activation and anti-tumor response. |
Zelboraf Side Effects
| Common Side Effects | Serious Side Effects |
|---|---|
| Arthralgia | Cutaneous squamous cell carcinoma |
| Fatigue | QT prolongation |
| Rash | Hypersensitivity reactions (anaphylaxis, angioedema) |
| Photosensitivity | Uveitis |
| Alopecia | Liver abnormalities |
| Nausea | New primary melanomas |
Zelboraf Dosage Guide
| Condition | Starting Dose | Maintenance Dose | Administration Notes |
|---|---|---|---|
| BRAF V600E Mutation-Positive Melanoma | 960 mg (4 x 240 mg tablets) | 960 mg twice daily | Take tablets whole with water. Can be taken with or without food. |
