Zelboraf (vemurafenib)Tablet
HIGHLIGHTS OF PRESCRIBING INFORMATION
Indications And Usage
ZELBORAF™ is a kinase inhibitor indicated for the treatment of patients with unresectable or metastatic melanoma with BRAFV600E mutation as detected by an FDA-approved test. (1, 5.10)
Limitation of Use: ZELBORAF is not recommended for use in patients with wild-type BRAF melanoma. (5.10, 14)
Dosage And Administration
Recommended dose: 960 mg orally twice daily. (2.1)
Administer ZELBORAF approximately 12 hours apart with or without a meal. (2.1)
ZELBORAF should be swallowed whole with a glass of water. ZELBORAF should not be chewed or crushed. (2.1)
Management of symptomatic adverse drug reactions may require dose reduction, treatment interruption, or treatment discontinuation of ZELBORAF. Dose reductions resulting in a dose below 480 mg twice daily are not recommended. (2.2)
Dosage And Administration 2
Film-coated tablet: 240 mg (3)
Contraindications
None (4)
Warnings And Precautions
Cutaneous squamous cell carcinomas (cuSCC) occurred in 24% of patients. Perform dermatologic eva luations prior to initiation of therapy and every two months while on therapy. Manage with excision and continue treatment without dose adjustment. (5.1)
Serious hypersensitivity reactions, including anaphylaxis, have been reported during and upon re-initiation of treatment. Discontinue ZELBORAF in patients who experience severe hypersensitivity reactions. (5.2)
Severe dermatologic reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis, have been reported. Discontinue treatment in patients who experience severe dermatologic reactions. (5.3)
QT prolongation has been reported. Monitor ECG and electrolytes before treatment and after dose modification. Monitor ECGs at day 15, monthly during the first 3 months of treatment, every 3 months thereafter, or more often as clinically indicated. If the QTc exceeds 500 ms, temporarily interrupt ZELBORAF, correct electrolyte abnormalities, and control for cardiac risk factors for QT prolongation. (5.4)
Liver laboratory abnormalities may occur. Monitor liver enzymes and bilirubin before initiation of treatment and monthly during treatment, or as clinically indicated. (5.5)
Photosensitivity has been reported. Advise patients to avoid sun exposure while taking ZELBORAF. (5.6)
Serious ophthalmologic reactions, including uveitis, iritis and retinal vein occlusion, have been reported. Monitor patients routinely for ophthalmologic reactions. (5.7)
New primary malignant melanomas have been reported. Manage with excision, and continue treatment without dose modification. Perform dermatologic monitoring as outlined above. (5.8)
Pregnancy: May cause fetal harm. Advise women of potential risk to the fetus. (5.9, 8.1)
BRAFV600E testing – confirmation of BRAFV600E mutation using an FDA-approved test is required for selection of patients appropriate for ZELBORAF therapy. The efficacy and safety of ZELBORAF have not been studied in patients with wild-type BRAF melanoma. (5.10, 14)
Adverse Reactions
Most common adverse reactions (≥ 30%) are arthralgia, rash, alopecia, fatigue, photosensitivity reaction, nausea, pruritus and skin papilloma. (6.1)
To report SUSPECTED ADVERSE REACTIONS, contact Genentech at 1-888-835-2555 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
Drug Interactions
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