Vemurafenib (ZELBORAF)

Melanoma, advanced or metastatic with BRAF V600E or BRAF V600K mutation

Melanoma, advanced or metastatic with BRAF V600E or BRAF V600K mutation

• Oral: 960 mg twice daily continuously until disease progression or unacceptable toxicity.
• Given as monotherapy or in combination with cobimetinib

Available as 240 mg film-coated tablets. Tablets should NOT be crushed or broken. Store at room temperature, keep in original packaging, and protect from moisture.

BRAF Inhibitor

Take with or without food

If a dose is missed, patients should be instructed to take it as soon as they can if there are > 4 hours until the next dose. If there are < 4 hours until the next dose, patients should skip the missed dose and resume with the next scheduled dose.

Common: Nausea, Fatigue, Arthralgia, Cutaneous squamous cell carcinoma, Alopecia, Photosensitivity reaction, Pruritus, Rash, Creatinine increase.

Less Common: QTc prolongation, Dupuytren’s contracture, plantar fascial fibromatosis, Secondary cutaneous and non-cutaneous malignancies, Tumor Lysis Syndrome, Radiation sensitization, Acute kidney injury, Hepatic injury, Hypersensitivity reactions.

The adverse effects listed above are not exhaustive. Please refer to the relevant product monograph for full details.

Baseline before treatment: CBC & differential, platelets, sodium, potassium, calcium, magnesium, creatinine, alkaline phosphatase, ALT, bilirubin, GGT, albumin, LDH, ECG, dermatologic evaluation for other skin cancer, blood pressure, Chest CT, MUGA scan or echocardiogram, pap smear if indicated.

During treatment: sodium, potassium, calcium, magnesium, creatinine, alkaline phosphatase, creatine kinase, ALT, bilirubin, LDH, GGT, albumin, ECG (prior to cycle for first 12 cycles then every 12 weeks), dermatologic evaluation (at week 8, then every 12 weeks).

If clinically indicated: Chest CT (every 6 months and with monitoring of metastases).

• May increase the risk for QT interval prolongation. Avoid concurrent therapy with drugs associated with QTc prolongation and/or Torsades de pointes, if possible. If unavoidable, monitor for QT prolongation or cardiac arrhythmias.
• Avoid grapefruit, grapefruit juice, Seville oranges, or Seville orange juice.
• This drug can impact or be impacted by metabolic enzymes for absorption and excretion. Many drugs can also affect or be affected by these enzymes, so please consult with pharmacy to assess for interactions.
• Current drug interaction databases should be consulted for more information.

• Avoid in pregnancy and lactation.
• Secondary malignancies have been reported with vemurafenib including cutaneous squamous cell carcinoma, new primary melanomas, and non-cutaneous malignancies. Skin examination should be performed prior to, during, and after treatment has ended.
• Patients taking Vemurafenib have a potential for photosensitivity upon sun exposure. Patients should wear protective clothing and/or sunblock during treatment.

BC Cancer. BC Cancer Drug Manual. Vemurafenib. Vancouver, British Columbia: BC Cancer Agency. Available at: http://www.bccancer.bc.ca/drug-database-site/Drug%20Index/Vemurafenib_monograph.pdf. Updated March 1, 2018. Accessed January 22, 2024.

Lexicomp. Vemurafenib Monograph. In: Lexi-Drugs. Hudson, Ohio: Lexi-Comp, Inc. Available at: https://online-lexi-com.qe2a-proxy.mun.ca/lco/action/doc/retrieve/docid/patch_f/3508791?cesid=3Us5kYUViww&searchUrl=%2Flco%2Faction%2Fsearch%3Fq%3Dvemurafenib%26t%3Dname%26acs%3Dtrue%26acq%3Dvemurafenib. Updated January 24, 2024. Accessed January 28, 2024.

Cancer Care Ontario. Vemurafenib Monograph. Drug Formulary. Toronto, Ontario: Cancer Care Ontario. Available at: https://www.cancercareontario.ca/en/drugformulary/drugs/monograph/44281. Updated August 2023. Accessed January 22, 2024.

Hoffmann-La Roche Limited. ZELBORAF® Product monograph. Mississauga, Ontario. Updated December 10, 2019.