Trametinib
- Generic Name
- Trametinib
- Brand Names
- Mekinist, Spexotras
- Drug Type
- Small Molecule
- Chemical Formula
- C26H23FIN5O4
- CAS Number
- 871700-17-3
- Unique Ingredient Identifier
- 33E86K87QN
- 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
Investigate Safety, Pharmacokinetics and Pharmacodynamics of GSK2118436 & GSK1120212
- First Posted Date
- 2010-02-19
- Last Posted Date
- 2019-07-05
- Lead Sponsor
- Novartis Pharmaceuticals
- Target Recruit Count
- 430
- Registration Number
- NCT01072175
- Locations
- 🇦🇺
Novartis Investigative Site, Heidelberg, Victoria, Australia
Study to Determine the Effectiveness of GSK1120212 in BRAF Mutation-positive Melanoma Previously Treated With or Without a BRAF Inhibitor
- First Posted Date
- 2009-12-21
- Last Posted Date
- 2014-03-31
- Lead Sponsor
- GlaxoSmithKline
- Target Recruit Count
- 97
- Registration Number
- NCT01037127
- Locations
- 🇦🇺
GSK Investigational Site, Nedlands, Western Australia, Australia
Open-label Study to Evaluate the Safety, PK, and PD of MEK Inhibitor GSK1120212 in Subjects With Relapsed or Refractory Leukemias
- First Posted Date
- 2009-06-15
- Last Posted Date
- 2014-04-02
- Lead Sponsor
- GlaxoSmithKline
- Target Recruit Count
- 97
- Registration Number
- NCT00920140
- Locations
- 🇩🇪
GSK Investigational Site, Leipzig, Sachsen, Germany
Open-label Study to Investigate the Safety, PK, and Pharmacodynamics of GSK1120212 in Subjects With Solid Tumors or Lymphoma
- First Posted Date
- 2008-06-02
- Last Posted Date
- 2017-11-13
- Lead Sponsor
- GlaxoSmithKline
- Target Recruit Count
- 206
- Registration Number
- NCT00687622
- Locations
- 🇺🇸
GSK Investigational Site, Norfolk, Virginia, United States
Drug Development Updates
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