Zelboraf

Vemurafenib (Zobovu) instructions

Common name: Vemurafenib

Commercial name: Zobovo

All names: Vemurafenib, Vemurafenib, Zobovo, Vemurafenib, Z elboraf, vemurafenib

[Indications and uses of vemurafenib tablets]

Applicable to unresectable or metastatic BRAF Treatment of patients with V600E-mutated melanoma.

Restrictions on use: ZELBORAF is not recommended in patients with melanoma who have wild-type BRAF.

[Vemurafenib dosage and administration]

(1) Recommended dosage: 960 mg orally. u2003u2003

(2) Give ZELBORAF approximately 12 hours apart with or without meals. u2003

(3) Swallow ZELBORAF completely with a glass of water. ZELBORAF should not be chewed or crushed. u2003u2003

(4) Management of symptomatic adverse drug reactions may require dose reduction, treatment interruption, or discontinuation of ZELBORAF treatment. Dose reduction resulting in doses below 480 mg is not recommended.

[Vemurafenib Warnings and Precautions]

(1) Cutaneous squamous cell carcinoma (cuSCC) occurs in 24% of patients. Dermatological evaluations were performed prior to initiation of treatment and every 2 months while treatment was being used. No dose adjustment is required for resection and continuation of treatment. u2003u2003

(2) Serious hypersensitivity reactions, including anaphylaxis, have been reported during treatment and when treatment is restarted. Discontinue ZELBORAF in patients who experience severe hypersensitivity reactions. u2003u2003

(3) Serious dermatological reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis, have been reported. Discontinue treatment in patients who experience severe dermatological reactions. u2003u2003

(4) QT prolongation has been reported. Monitor ECG and electrolytes before treatment and after dose adjustment. Monitor ECGs on Day 15, every 3 months during the first 3 months of treatment, and every 3 months thereafter, or more often as clinically indicated. If QTc exceeds 500 ms, briefly interrupt ZELBORAF, correct electrolyte abnormalities, and control risk factors for QT prolongation. u2003u2003

(5) Liver laboratory abnormalities may occur. Monitor liver enzymes and bilirubin prior to initiation of treatment and monthly during treatment, or as clinically indicated. u2003u2003

(6) Photosensitivity has been reported. Advise patients to avoid sun exposure while taking ZELBORAF. u2003u2003

(7) Serious ophthalmic reactions, including uveitis, iritis, and retinal vein occlusion, have been reported. Monitor patients routinely for ophthalmic reactions. u2003u2003

(8) New primary malignant melanoma has been reported. Resection management, and continuation of treatment without dose adjustment. Dermatological surveillance was performed as described above. u2003

(9) Pregnancy: May cause fetal harm. Advise women of the potential risk to the fetus. u2003

(10) To select patients suitable for ZELBORAF treatment, use an FDA-approved test for BRAF mutations. The efficacy and safety of ZELBORAF have not been studied in patients with melanoma who have wild-type BRAF.

[Adverse reactions of Zobovo]

The most common adverse reactions (≥30%) are joint pain, rash, alopecia, fatigue, photosensitivity, nausea, pruritus and skin papilloma.

[Zelboraf drug interactions]

(1) CYP substrate: It is not recommended to use ZELBORAF concurrently with drugs with a narrow therapeutic window that are metabolized by CYP3A4, CYP1A2 or CYP2D6. If coadministration cannot be avoided, exercise caution and consider reducing the dose of the concurrent CYP1A2 or CYP2D6 substrate drug. u2003u2003

(2) ZELBORAF may increase exposure to warfarin when administered concomitantly. Use caution and consider additional INR monitoring when ZELBORAF is used concurrently with warfarin.

[Use of ZELBORAF in special populations]

Nasting mothers: Discontinue breastfeeding while receiving ZELBORAF.