ZELBORAF 240 MG TAB (VEMURAFENIB)

📘 Introduction

Zelboraf is a cancer medicine that interferes with the growth and spread of cancer cells in the body.

Zelboraf is used to treat melanoma (skin cancer) that has spread to other parts of the body or cannot be removed by surgery.

Zelboraf is also used to treat Erdheim-Chester Disease (a rare blood cancer)

• Generic Name (Salt): Vemurafenib

• Brand Name: Zelboraf

• Drug Class: BRAF kinase inhibitor

• Manufacturer: Genentech (Roche) / Plexxikon

📋 Indications

        Zelboraf is approved to treat:

• Unresectable or metastatic melanoma with confirmed BRAF V600E or V600K mutation

• Erdheim-Chester Disease with the BRAF V600 mutation

💊 Dosage & Administration

• Tablet Strength: 240 mg

• Standard Dose: 960 mg (four 240 mg tablets) twice daily, ~12 hours apart

• Administration Tips: With or without food; avoid taking two doses within 4 hours

       Dose Modifications for Side Effects/QT prolongation:

• Interrupt for Grade ≥2 intolerable or Grade 3 AEs, then resume at 720 mg BID → reduce further to 480 mg BID as needed — do not go below 480 mg BID

⚠️ Warnings & Precautions

1. New Primary Skin Cancers (cuSCC, KA, melanoma): Occur in ~24–29% of patients—skin exams before initiation and every 2 months during treatment

2. QT Prolongation/Cardiac Monitoring: ECG and electrolytes at baseline and periodically; interrupt dosing if QTc >500 ms or increased by >60 ms

3. Photosensitivity: Severe sunburn risk—use high-SPF sunscreen and protective clothing

4. Severe Dermatologic Reactions: Stevens–Johnson or DRESS syndrome—discontinue immediately

5. Allergic Reactions & Eye Inflammation: Seek care for rash, breathing difficulty, vision changes

6. Liver, Kidney Impairment: Monitor LFTs, creatinine regularly

⚠️ Side Effects

     Common

• Arthralgia/myalgia, fatigue, rash, hair thinning, photosensitivity, nausea, diarrhea, headache, edema, pruritus, fever

    Serious

• cuSCC, new melanomas, Stevens–Johnson/DRESS, QT prolongation, hepatitis, ocular disorders, cardiac arrhythmias, allergic reactions, skin peeling, blistering

🔄 Drug Interactions

• Strong CYP3A4 inducers reduce vemurafenib levels—avoid if possible; if necessary, increase dose by 240 mg BID and taper after discontinuation

• No formal dose reductions for CYP3A4 inhibitors, but monitoring is advised

🚻 Special Populations

• Pregnancy/Breastfeeding: Avoid—teratogenic risk; use effective contraception during treatment and 2 weeks after

• Renal/Hepatic impairment: Use caution; close monitoring required

• Sun exposure: Minimize—can cause severe sunburn for weeks after dosing

✅ Conclusion

      Zelboraf is a first-in-class BRAF V600E/K kinase inhibitor offering improved survival in metastatic BRAF-mutant melanoma and Erdheim-Chester Disease.

      While highly effective, it requires:

• Regular skin cancer screening

• ECG and electrolyte monitoring

• Sun protection strategies

• Dose adjustments for toxicity

• Awareness of serious dermatologic, cardiac, hepatic, ocular, and hypersensitivity risks