Trametinib

Generic Name: Trametinib

Brand Names: Mekinist, Spexotras

Drug Type: Small Molecule

Chemical Formula: C_₂₆H_₂₃FIN_₅O_₄

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

Clinical Trials

BRAF/MEK/EGFR Inhibitor Combination Study in Colorectal Cancer (CRC)

Phase 1

Completed

Conditions: Cancer

Interventions: Device: 5-fluorouracil
Drug: Dabrafenib
Drug: Panitumumab
Drug: Trametinib

First Posted Date: 2012-12-17

Last Posted Date: 2021-10-29

Lead Sponsor: Novartis Pharmaceuticals

Target Recruit Count: 166

Registration Number: NCT01750918

Locations: 🇬🇧
Novartis Investigative Site, Birmingham, United Kingdom

Trametinib, Fluorouracil, and Radiation Therapy Before Surgery in Treating Patients With Stage II-III Rectal Cancer

Phase 1

Completed

Conditions: Stage IIB Rectal Cancer
Recurrent Rectal Cancer
Stage IIIC Rectal Cancer
Stage IIA Rectal Cancer
Stage IIC Rectal Cancer
Stage IIIA Rectal Cancer
Stage IIIB Rectal Cancer

Interventions: Drug: trametinib
Drug: fluorouracil
Radiation: radiation therapy

First Posted Date: 2012-12-04

Last Posted Date: 2023-09-18

Lead Sponsor: Ohio State University Comprehensive Cancer Center

Target Recruit Count: 19

Registration Number: NCT01740648

Locations: 🇺🇸
Arthur G. James Cancer Hospital and Solove Research Institute at Ohio State University Medical Center, Columbus, Ohio, United States
🇺🇸
Roswell Park Cancer Institute, Buffalo, New York, United States
🇺🇸
Siteman Cancer Center at Washington University, Saint Louis, Missouri, United States

and more 1 locations

Dabrafenib With or Without Trametinib in Treating Patients With Recurrent Thyroid Cancer

Phase 2

Active, not recruiting

Conditions: Follicular Thyroid Cancer
Papillary Thyroid Cancer
Insular Thyroid Cancer
Recurrent Thyroid Cancer

Interventions: Drug: dabrafenib
Other: Correlative Studies
Drug: trametinib

First Posted Date: 2012-11-07

Last Posted Date: 2022-11-17

Lead Sponsor: Bhavana Konda

Target Recruit Count: 53

Registration Number: NCT01723202

Locations: 🇺🇸
The University of Texas-MD Anderson Cancer Center, Houston, Texas, United States
🇺🇸
University of Chicago Medical Center, Chicago, Illinois, United States
🇺🇸
University of California, San Diego, San Diego, California, United States

and more 2 locations

Dabrafenib and Trametinib With Radiosurgery in Melanoma Brain Mets

Phase 2

Terminated

Conditions: BRAFV600E Melanoma Patients

Interventions: Drug: Dabrafenib
Procedure: Gamma Knife Radiosurgery
Drug: Trametinib

First Posted Date: 2012-11-06

Last Posted Date: 2018-01-23

Lead Sponsor: University of California, San Francisco

Target Recruit Count: 2

Registration Number: NCT01721603

Locations: 🇺🇸
University of San Francisco, California, San Francisco, California, United States

Dabrafenib Alone and in Combination With Trametinib Before Surgery in Treating Patients With Locally or Regionally Advanced Melanoma That Can Be Removed By Surgery

Phase 2

Terminated

Conditions: Stage IIIA Melanoma
Stage IIB Melanoma (Locally Advanced)
Recurrent Melanoma
Stage IIC Melanoma (Locally Advanced)
Stage IIIB Melanoma
Stage IIIC Melanoma
Stage IV Melanoma (Limited, Resectable)