Trametinib

(Mekinist®)

Mekinist®

Drug updated on 12/11/2024

Dosage FormTablet (oral; 0.5 mg, 2 mg)
Drug ClassKinase inhibitors
Ongoing and
Completed Studies
ClinicalTrials.gov

Indication

  • Indicated for the treatment of BRAF-inhibitor treatment-nave patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations as detected by an FDA approved test
  • Indicated in combination with dabrafenib, for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations as detected by an FDA-approved test
  • Indicated in combination with dabrafenib, for the adjuvant treatment of patients with melanoma with BRAF V600E or V600K mutations, as detected by an FDA-approved test, and involvement of lymph node(s), following complete resection
  • Indicated in combination with dabrafenib, for the treatment of patients with metastatic non-small cell lung cancer (NSCLC) with BRAF V600E mutation as detected by an FDA-approved test
  • Indicated in combination with dabrafenib, for the treatment of patients with locally advanced or metastatic anaplastic thyroid cancer (ATC) with BRAF V600E mutation and with no satisfactory locoregional treatment options
  • Indicated in combination with dabrafenib, for the treatment of adult and pediatric patients 1 year of age and older with unresectable or metastatic solid tumors with BRAF V600E mutation who have progressed following prior treatment and have no satisfactory alternative treatment options
  • This indication is approved under accelerated approval based on overall response rate and duration of response
  • Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial(s)
  • Indicated in combination with dabrafenib, for the treatment of pediatric patients 1 year of age and older with low-grade glioma (LGG) with a BRAF V600E mutation who require systemic therapy.

Latest News

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Summary
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  • This summary is based on the review of 21 systematic review(s)/meta-analysis(es). [1-21]
  • BRAF-Mutant Melanoma: Dabrafenib + trametinib demonstrates high efficacy and manageable safety profiles, significantly prolonging overall survival (OS) and progression-free survival (PFS) compared to monotherapies and other combination therapies.
  • Acral Melanoma: Adjuvant therapy with dabrafenib + trametinib achieves high rates of 12-month recurrence-free survival (RFS) in BRAF-mutated cases, indicating effectiveness in this specific population.
  • Anaplastic Thyroid Cancer: Evidence supports the combination of dabrafenib + trametinib, showing a median OS of 6.37 months and a median PFS of 5.50 months in real-world clinical practice, highlighting its utility beyond melanoma.
  • Adverse Events (AEs): The combination of dabrafenib + trametinib was associated with a high incidence of AEs, reporting 50% AEs and 43% death events in BRAF V600-mutant glioma patients. Common AEs included rash, cutaneous squamous-cell carcinoma (cSCC), alopecia, keratoacanthoma (KA), hyperkeratosis (HK), and pruritus.
  • Comparison to Other Drugs: Encorafenib + binimetinib showed fewer serious adverse events and lower rates of discontinuations due to AEs compared to dabrafenib + trametinib. In contrast, nivolumab + ipilimumab had the highest risk of AEs among the therapies compared.
  • BRAF-Mutant Melanoma: Dabrafenib + trametinib is recommended for both adjuvant and unresectable/metastatic settings in patients with BRAF-mutant cutaneous melanoma, demonstrating high efficacy and manageable safety profiles across multiple studies.

Product Monograph / Prescribing Information

Document TitleYearSource
Mekinist (trametinib) Prescribing Information.2024Novartis Pharmaceuticals Corporation, East Hanover, NJ

Systematic Reviews / Meta-Analyses

Document TitleYearSource
Adjuvant Therapy in Acral Melanoma: A Systematic Review2024Clinical, Cosmetic And Investigational Dermatology
Tyrosine kinase inhibitors in patients with advanced anaplastic thyroid cancer: an effective analysis based on real-world retrospective studies2024Frontiers In Endocrinology
The effects of dabrafenib and/or trametinib treatment in Braf V600-mutant glioma: a systematic review and meta-analysis2024Neurosurgical Review
Efficacy and safety of immune checkpoint inhibitors and targeted therapies in resected melanoma: a systematic review and network meta-analysis2023Frontiers In Pharmacology
BRAF inhibitors in BRAF V600E-mutated ameloblastoma: systematic review of rare cases in the literature2023Medical Oncology (Northwood, London, England)
Neoadjuvant treatment for stage III and IV cutaneous melanoma2023The Cochrane Database Of Systematic Reviews
Comparative efficacy and safety of targeted therapies for BRAF-mutant unresectable or metastatic melanoma: Results from a systematic literature review and a network meta-analysis2022Cancer Treatment Reviews
Adjuvant Treatments of Adult Melanoma: A Systematic Review and Network Meta-Analysis2022Frontiers In Oncology
Acceptability of Drugs in the Treatment of Unresectable/Metastatic BRAF V600-Mutant Melanoma: A Systematic Review and Network Meta-Analysis2022Frontiers In Oncology
Impact of Previous Local Treatment for Brain Metastases on Response to Molecular Targeted Therapy in BRAF-Mutant Melanoma Brain Metastasis: A Systematic Review and Meta-Analysis2022Frontiers In Oncology
Comparative efficacy of dabrafenib + trametinib versus treatment options for metastatic melanoma in first-line settings2021Journal Of Comparative Effectiveness Research
A matching-adjusted indirect comparison of combination nivolumab plus ipilimumab with BRAF plus MEK inhibitors for the treatment of BRAF-mutant advanced melanoma(☆)2021Esmo Open
Comparative efficacy and safety of adjuvant nivolumab versus other treatments in adults with resected melanoma: a systematic literature review and network meta-analysis2021Bmc Cancer
Neuromuscular Complications of Targeted Anticancer Agents: Can Tyrosine Kinase Inhibitors Induce Myasthenia Gravis? Getting Answers From a Case Report up to a Systematic Review2021Frontiers In Oncology
Contemporary Neoadjuvant Therapies for High-Risk Melanoma: A Systematic Review2021Cancers
The incidence and risk of cutaneous toxicities associated with dabrafenib in melanoma patients: a systematic review and meta-analysis2021European Journal Of Hospital Pharmacy : Science And Practice
Systemic Therapy for Melanoma: ASCO Guideline2020Journal Of Clinical Oncology : Official Journal Of The American Society Of
Economic Evaluation of Systemic Treatments for Advanced Melanoma: A Systematic Review2020Value In Health : The Journal Of The International Society For Pharmacoeconomics
Adjuvant Therapy of High-Risk (Stages IIC-IV) Malignant Melanoma in the Post Interferon-Alpha Era: A Systematic Review and Meta-Analysis2020Frontiers In Oncology
Efficacy and Adverse Events in Metastatic Melanoma Patients Treated with Combination BRAF Plus MEK Inhibitors Versus BRAF Inhibitors: A Systematic Review2019Cancers
Comparative efficacy and safety of dabrafenib in combination with trametinib versus competing adjuvant therapies for high-risk melanoma2019Journal Of Comparative Effectiveness Research

Clinical Practice Guidelines