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Trametinib Kinase Inhibitor Targeting BRAF V600 Mutation-Positive Cancers

Reference price: USD 8-15/g

  • Product Name Trametinib
  • CAS No. 871700-17-3
  • MF C26H23FIN5O4
  • MW 615.402623
  • Density 1.743
  • Melting point 293-303°C

Detailed Description

Trametinib is a potent and selective kinase inhibitor primarily used in the treatment of unresectable or metastatic melanoma with the BRAF V600 mutation, as well as specific types of advanced or metastatic non-small cell lung cancer. This article explores the mechanism of action, clinical indications, and benefits of trametinib in the treatment of BRAF V600 mutation-positive cancers.

I. Understanding Trametinib:
A. Oral, potent, and selective kinase inhibitor
B. Belongs to the MEK inhibitors class
C. Blocks kinase activity of MEK1 and MEK2
D. Inhibits downstream ERK1 and ERK2 signaling

II. Clinical Indications:
A. Unresectable or metastatic melanoma harboring BRAF V600 mutation:
Combination therapy with dabrafenib mesylate
B. Postoperative adjuvant therapy for BRAF V600 mutation-positive melanoma:
Adjuvant treatment with dabrafenib mesylate after complete resection

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III. Role in Non-Small Cell Lung Cancer:

A. Non-small cell lung cancer as the leading cause of morbidity and mortality

B. BRAF gene mutation rate and prevalence of BRAF V600E mutation

C. Trametinib's inhibitory effect on BRAF V600 mutation-positive melanoma cells


IV. Mechanism of Action:

A. Reversible inhibition of mitogen-activated extracellular signal-regulated kinase (MEK) 1 and MEK2

B. Impact on the MAPK pathway and MEK protein

C. Inhibition of cell proliferation and downstream ERK pathway


V. Postoperative Adjuvant Therapy:

A. Benefits of targeted combination therapy with Dabrafenib and Trametinib

B. Long-term, durable recurrence-free survival (RFS) benefits in high-risk stage III BRAF mutation-positive melanoma patients



Trametinib, a targeted kinase inhibitor, shows significant efficacy in the treatment of BRAF V600 mutation-positive cancers, particularly unresectable or metastatic melanoma and specific types of non-small cell lung cancer. Its mechanism of action, inhibiting MEK1 and MEK2 kinase activity, leads to downstream ERK pathway inhibition and suppression of cell proliferation. Trametinib, in combination with dabrafenib mesylate, provides therapeutic benefits in both advanced and adjuvant settings for BRAF V600 mutation-positive melanoma patients.
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Specification

171611254334271z