Vemurafenib

(Zelboraf®)

Vemurafenib

Drug updated on 6/11/2024

Dosage FormTablet (oral; 240 mg)
Drug ClassKinase inhibitors
Ongoing and
Completed Studies
ClinicalTrials.gov

Indication

  • For the treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test.
  • For the treatment of patients with Erdheim Chester Disease with BRAF V600 mutation.

Latest News

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Summary
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  • Vemurafenib (Zelboraf) is used in the treatment of metastatic melanoma with BRAF V600 mutations and Erdheim-Chester Disease with BRAF V600 mutation, showing prominent efficacy when compared to other treatments.
  • Fifteen studies on vemurafenib's safety and effectiveness were reviewed.
  • PD-(L)1/BRAF/MEK inhibitor triplets, which include vemurafenib combinations, were found superior to dual checkpoint inhibitor combinations such as ipilimumab/nivolumab in terms of progression-free survival (PFS) and overall response rate (ORR), but these combinations are associated with higher toxicity rates.
  • Treatments pairing BRAF inhibitors like vemurafenib with MEK inhibitors demonstrated notable efficacy for advanced melanoma; however, encorafenib + binimetinib might be superior in efficacy and have a more favorable safety profile relative to vemurafenib combinations.
  • Dermatological adverse events including cutaneous squamous cell carcinoma, rash, photosensitivity, among others, are common among patients treated with Zelboraf; cardiovascular adverse events also warrant close monitoring, especially when combination therapy involving both BRAF & MEK inhibitors is administered.
  • For Erdheim-Chester Disease patients carrying the BRAF V600 mutation, Zelboraf has shown significant strides, although its tolerance level varies from patient to patient, requiring careful management due to side effects.
  • Adjuvant therapy using targeted treatments like Zelboraf shows significant recurrence-free survival benefits across various patient subgroups, such as those based on age or specific genetic markers, e.g., presence of a particular type of BRAF mutation seems particularly beneficial for outcomes under combination therapies involving BRAF/MEK inhibition.
  • Zelboraf remains an important option given its marked influence over progression-free and overall survival rates in patients with melanoma or Erdheim-Chester Disease; however, its use is challenged by higher toxicity profiles compared to some alternative regimens.

Product Monograph / Prescribing Information

Document TitleYearSource
Zelboraf (vemurafenib) Prescribing Information.2020Genentech USA, Inc., South San Francisco, CA

Systematic Reviews / Meta-Analyses

Document TitleYearSource
Activity and safety of first-line treatments for advanced melanoma: A network meta-analysis.2023European Journal of Cancer
Vemurafenib in the treatment of erdheim chester disease: A systematic review.2022Cureus
Comparative efficacy and safety of targeted therapies for BRAF-mutant unresectable or metastatic melanoma: Results from a systematic literature review and a network meta-analysis.2022Cancer treatment Reviews
Acceptability of Drugs in the Treatment of Unresectable/Metastatic BRAF V600-Mutant Melanoma: A Systematic Review and Network Meta-Analysis.2022Frontiers in Oncology
Adjuvant therapy of high-risk (Stages IIC-IV) malignant melanoma in the post interferon-alpha era: A systematic review and meta-analysis.2021Frontiers in Oncology
Comparative efficacy of dabrafenib + trametinib versus treatment options for metastatic melanoma in first-line settings2021Journal of Comparative Effectiveness Research
Systematic review of BRAF/MEK inhibitors-induced Severe Cutaneous Adverse Reactions (SCARs).2021Journal of the European Academy of Dermatology and Venereology
Efficacy and safety of dabrafenib–trametinib in the treatment of unresectable advanced/metastatic melanoma with BRAF-V600 mutation: A systematic review and network meta-analysis.2020Dermatologic Therapy
Systematic review and meta-analysis of prevalence of dermatological toxicities associated with vemurafenib treatment in patients with melanoma.2019Clinical and Experimental Dermatology
A systematic literature review and network meta-analysis of effectiveness and safety outcomes in advanced melanoma.2019European Journal of Cancer
Efficacy and adverse events in metastatic melanoma patients treated with combination BRAF plus MEK inhibitors versus BRAF inhibitors: A systematic review.2019Cancers
Adjuvant therapy for cutaneous melanoma: A systematic review and network meta-analysis of new therapies.2019European Academy of Dermatology and Venereology
Cardiovascular adverse events associated with BRAF and MEK inhibitors: A systematic review and meta-analysis.2019JAMA
Efficacy and safety of dabrafenib–trametinib in the treatment of unresectable advanced/metastatic melanoma with BRAF-V600 mutation: A systematic review and network meta-analysis.2019Dermatologic Therapy
Systematic review and meta-analysis of prevalence of dermatological toxicities associated with vemurafenib treatment in patients with melanoma.2019Clinical and Experimental Dermatology

Clinical Practice Guidelines