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
An Open-label Study of GSK1120212 Compared With Docetaxel in Stage IV KRAS-mutant Non-small Cell Lung Cancer
- First Posted Date
- 2011-05-30
- Last Posted Date
- 2014-07-11
- Lead Sponsor
- GlaxoSmithKline
- Target Recruit Count
- 134
- Registration Number
- NCT01362296
- Locations
- 🇪🇸
GSK Investigational Site, Pamplona, Spain
Study of Selective BRAF Kinase Inhibitor Dabrafenib Monotherapy Twice Daily and in Combination With Dabrafenib Twice Daily and Trametinib Once Daily in Combination Therapy in Subjects With BRAF V600E Mutation Positive Metastatic (Stage IV) Non-small Cell Lung Cancer.
- First Posted Date
- 2011-04-18
- Last Posted Date
- 2022-04-04
- Lead Sponsor
- Novartis Pharmaceuticals
- Target Recruit Count
- 177
- Registration Number
- NCT01336634
- Locations
- 🇬🇧
Novartis Investigative Site, Sutton, United Kingdom
Efficacy and Safety Study of GSK1120212, a MEK Inhibitor, in Subjects With Uveal Melanoma
- Conditions
- GNAQ Mutation-positive Metastatic MelanomaCancerMetastatic Uveal MelanomaGNA11 Mutation-positive Metastatic Melanoma
- Interventions
- First Posted Date
- 2011-04-04
- Last Posted Date
- 2017-12-12
- Lead Sponsor
- GlaxoSmithKline
- Registration Number
- NCT01328106
Trial of GSK1120212 and GSK1120212 in Combination With GEM in Japanese Subjects With Solid Tumors
- First Posted Date
- 2011-03-28
- Last Posted Date
- 2017-11-13
- Lead Sponsor
- GlaxoSmithKline
- Target Recruit Count
- 19
- Registration Number
- NCT01324258
- Locations
- 🇯🇵
GSK Investigational Site, Tokyo, Japan
GSK1120212 vs Chemotherapy in Advanced or Metastatic BRAF V600E/K Mutation-positive Melanoma
- First Posted Date
- 2010-11-22
- Last Posted Date
- 2018-04-05
- Lead Sponsor
- GlaxoSmithKline
- Target Recruit Count
- 322
- Registration Number
- NCT01245062
- Locations
- 🇬🇧
GSK Investigational Site, Southampton, United Kingdom
A Rollover Study to Provide Continued Treatment With GSK2118436 to Subjects With BRAF Mutation-Positive Tumors
- Conditions
- Cancer
- Interventions
- First Posted Date
- 2010-11-01
- Last Posted Date
- 2019-03-22
- Lead Sponsor
- Novartis Pharmaceuticals
- Target Recruit Count
- 214
- Registration Number
- NCT01231594
- Locations
- 🇬🇧
Novartis Investigative Site, London, United Kingdom
Study of GSK1120212 Plus Gemcitabine vs Placebo Plus Gemcitabine in Metastatic Pancreatic Cancer
- First Posted Date
- 2010-11-01
- Last Posted Date
- 2013-09-26
- Lead Sponsor
- GlaxoSmithKline
- Target Recruit Count
- 160
- Registration Number
- NCT01231581
- Locations
- 🇨🇳
GSK Investigational Site, Taipei, Taiwan
Safety and Tolerability Study of GSK1120212, a MEK Inhibitor, in Combination With Docetaxel, Erlotinib, Pemetrexed, Pemetrexed + Carboplatin, Pemetrexed + Cisplatin, or Nab-Paclitaxel
- Conditions
- Cancer
- Interventions
- First Posted Date
- 2010-08-31
- Last Posted Date
- 2017-11-13
- Lead Sponsor
- GlaxoSmithKline
- Target Recruit Count
- 169
- Registration Number
- NCT01192165
- Locations
- 🇰🇷
GSK Investigational Site, Seoul, Korea, Republic of
A Study to Investigate Safety, Pharmacokinetics (PK) and Pharmacodynamics (PD) of BKM120 Plus GSK1120212 in Selected Advanced Solid Tumor Patients
- Conditions
- Advanced and Selected Solid Tumors
- Interventions
- First Posted Date
- 2010-07-01
- Last Posted Date
- 2020-12-09
- Lead Sponsor
- Novartis Pharmaceuticals
- Target Recruit Count
- 113
- Registration Number
- NCT01155453
- Locations
- 🇺🇸
University of Texas/MD Anderson Cancer Center Dept of MD Anderson (8), Houston, Texas, United States
🇨🇭Novartis Investigative Site, Bellinzona, Switzerland
🇺🇸University of California at Los Angeles Div. of Hematology/Oncology, Los Angeles, California, United States
Safety, Pharmacokinetics (PK) of AKT and MEK Combination
- First Posted Date
- 2010-06-07
- Last Posted Date
- 2017-11-13
- Lead Sponsor
- GlaxoSmithKline
- Target Recruit Count
- 240
- Registration Number
- NCT01138085
- Locations
- 🇺🇸
GSK Investigational Site, Salt Lake City, Utah, United States
Drug Development Updates
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