MedPath

Trametinib

Generic Name
Trametinib
Brand Names
Mekinist, Spexotras
Drug Type
Small Molecule
Chemical Formula
C26H23FIN5O4
CAS Number
871700-17-3
Unique Ingredient Identifier
33E86K87QN

Overview

Trametinib is an orally bioavailable mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and MEK2 inhibitor. It was first approved by the FDA in May 2013 for the treatment of melanoma. It was later approved by Health Canada on July 18, 2013 and by the European Commission on June 30, 2014. Trametinib is currently approved to treat a variety of cancers with BRAF mutations, such as non-small cell lung cancer and thyroid cancer, as monotherapy or in combination with dabrafenib, a BRAF inhibitor, for improved therapeutic efficacy. Originally developed by Japan Tobacco, trametinib was initially investigated for treating inflammation, but further studies for this indication were not pursued.

Background

Trametinib is an orally bioavailable mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and MEK2 inhibitor. It was first approved by the FDA in May 2013 for the treatment of melanoma. It was later approved by Health Canada on July 18, 2013 and by the European Commission on June 30, 2014. Trametinib is currently approved to treat a variety of cancers with BRAF mutations, such as non-small cell lung cancer and thyroid cancer, as monotherapy or in combination with dabrafenib, a BRAF inhibitor, for improved therapeutic efficacy. Originally developed by Japan Tobacco, trametinib was initially investigated for treating inflammation, but further studies for this indication were not pursued.

Indication

Trametinib is indicated as monotherapy for the treatment of BRAF-inhibitor treatment-naïve patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations. It is used in combination with dabrafenib for the: In the US, BRAF V600E or V600K mutations must be detected by an FDA-approved test. Trametinib is not indicated for the treatment of patients with colorectal cancer because of known intrinsic resistance to BRAF inhibition.

Associated Conditions

  • Advanced Non-Small Cell Lung Cancer (NSCLC)
  • Locally Advanced Anaplastic Thyroid Cancer
  • Low-Grade Glioma
  • Melanoma
  • Metastatic Anaplastic Thyroid Cancer
  • Metastatic Melanoma
  • Metastatic Non-Small Cell Lung Cancer
  • Stage III Melanoma
  • Unresectable Melanoma
  • Unresectable or Metastatic Solid Tumors

FDA Approved Products

No FDA products found for this drug

Singapore Approved Products

No Singapore products found for this drug

Drug Development Updates

Stay informed with timely notifications on clinical trials and research advancements.

© Copyright 2025. All Rights Reserved by MedPath