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

Trametinib With or Without Whole Brain Radiation Therapy in Treating Patients With Brain Metastases

Phase 1

Active, not recruiting

Conditions: Metastatic Malignant Neoplasm in the Brain

Interventions: Other: Laboratory Biomarker Analysis
Other: Pharmacological Study
Procedure: Therapeutic Conventional Surgery
Drug: Trametinib
Radiation: Whole-Brain Radiotherapy

First Posted Date: 2013-12-19

Last Posted Date: 2025-03-26

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 10

Registration Number: NCT02015117

Locations: 🇺🇸
Ohio State University Comprehensive Cancer Center, Columbus, Ohio, United States

Neoadjuvant Phase 2 Study Comparing the Effects of AR Inhibition With/Without SRC or MEK Inhibition in Prostate Cancer

Phase 2

Active, not recruiting

Conditions: Prostate Cancer

Interventions: Drug: degarelix
Drug: enzalutamide
Drug: trametinib
Drug: dasatinib

First Posted Date: 2013-11-21

Last Posted Date: 2024-10-01

Lead Sponsor: Jonsson Comprehensive Cancer Center

Target Recruit Count: 45

Registration Number: NCT01990196

Locations: 🇺🇸
University of California, Los Angeles, Los Angeles, California, United States

Trametinib and Akt Inhibitor GSK2141795 in Treating Patients With Relapsed or Refractory Multiple Myeloma

Phase 2

Completed

Conditions: Refractory Plasma Cell Myeloma
Recurrent Plasma Cell Myeloma

Interventions: Other: Laboratory Biomarker Analysis
Other: Pharmacological Study
Drug: Trametinib
Drug: Uprosertib

First Posted Date: 2013-11-21

Last Posted Date: 2022-03-02

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 25

Registration Number: NCT01989598

Locations: 🇨🇦
University Health Network-Princess Margaret Hospital, Toronto, Ontario, Canada
🇨🇦
Tom Baker Cancer Centre, Calgary, Alberta, Canada
🇨🇦
Cross Cancer Institute, Edmonton, Alberta, Canada

and more 2 locations

Testing the Addition of Navitoclax to the Combination of Dabrafenib and Trametinib in People Who Have BRAF Mutant Melanoma

Phase 1

Active, not recruiting

Conditions: Clinical Stage IV Cutaneous Melanoma AJCC v8
Metastatic Melanoma
Clinical Stage III Cutaneous Melanoma AJCC v8
Unresectable Melanoma
Malignant Solid Neoplasm

Interventions: Procedure: Biopsy Procedure
Procedure: Biospecimen Collection
Procedure: Computed Tomography
Drug: Dabrafenib
Procedure: Echocardiography Test
Other: Laboratory Biomarker Analysis
Procedure: Magnetic Resonance Imaging
Procedure: Multigated Acquisition Scan
Other: Pharmacological Study
Biological: Navitoclax
Drug: Trametinib

First Posted Date: 2013-11-21

Last Posted Date: 2025-05-15

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 75

Registration Number: NCT01989585

Locations: 🇺🇸
Mayo Clinic Hospital in Arizona, Phoenix, Arizona, United States
🇺🇸
Mayo Clinic in Arizona, Scottsdale, Arizona, United States
🇺🇸
Los Angeles General Medical Center, Los Angeles, California, United States

and more 46 locations

Trametinib With or Without GSK2141795 in Treating Patients With Metastatic Uveal Melanoma

Phase 2

Completed

Conditions: Recurrent Uveal Melanoma
Stage IV Uveal Melanoma AJCC v7

Interventions: Other: Laboratory Biomarker Analysis
Other: Pharmacological Study
Drug: Trametinib
Drug: Uprosertib

First Posted Date: 2013-11-08

Last Posted Date: 2020-02-24

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 42

Registration Number: NCT01979523

Locations: 🇺🇸
M D Anderson Cancer Center, Houston, Texas, United States
🇫🇷
Institut Curie Paris, Paris, France
🇺🇸
Emory University Hospital/Winship Cancer Institute, Atlanta, Georgia, United States

and more 4 locations

Dabrafenib/Trametinib, BRAF or BRAF AND MEK Pre-op With BRAF and MEK Post-op, Phase IIB, Melanoma With Brain Mets,Biomarkers and Metabolites

Phase 2

Terminated

Conditions: Melanoma and Brain Metastases

Interventions: Drug: Dabrafenib 150 mg
Drug: Trametinib 2.0 mg

First Posted Date: 2013-11-07

Last Posted Date: 2018-08-17

Lead Sponsor: GlaxoSmithKline

Target Recruit Count: 6

Registration Number: NCT01978236

Locations: 🇦🇺
GSK Investigational Site, North Sydney, New South Wales, Australia

Neoadjuvant Dabrafenib + Trametinib for AJCC Stage IIIB-C BRAF V600 Mutation Positive Melanoma

Phase 2

Active, not recruiting

Conditions: Melanoma

Interventions: Drug: Dabrafenib
Drug: Trametinib

First Posted Date: 2013-10-30

Last Posted Date: 2025-01-23

Lead Sponsor: Melanoma Institute Australia

Target Recruit Count: 35

Registration Number: NCT01972347

Locations: 🇦🇺
Melanoma Institute Australia, North Sydney, New South Wales, Australia

Trametinib and Akt Inhibitor GSK2141795 in Treating Patients With Metastatic Triple-Negative Breast Cancer

Phase 2

Completed

Conditions: Progesterone Receptor Negative
Recurrent Breast Carcinoma
Stage IV Breast Cancer
Estrogen Receptor Negative
HER2/Neu Negative
Invasive Breast Carcinoma
Triple-Negative Breast Carcinoma

Interventions: Drug: Akt Inhibitor GSK2141795
Other: Laboratory Biomarker Analysis
Drug: Trametinib

First Posted Date: 2013-10-17

Last Posted Date: 2019-09-20

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 37

Registration Number: NCT01964924

Locations: 🇺🇸
Case Western Reserve University, Cleveland, Ohio, United States
🇺🇸
UNC Lineberger Comprehensive Cancer Center, Chapel Hill, North Carolina, United States
🇺🇸
Ohio State University Comprehensive Cancer Center, Columbus, Ohio, United States

and more 5 locations

A Phase IIa Study of the MEK Inhibitor Trametinib Monotherapy in the Treatment of Biliary Tract Cancers

Phase 2

Completed

Conditions: Cancer

Interventions: Drug: Trametinib (Multiple tablet)
Drug: Trametinib (single tablet)

First Posted Date: 2013-09-17

Last Posted Date: 2017-05-31

Lead Sponsor: GlaxoSmithKline

Target Recruit Count: 20

Registration Number: NCT01943864

Locations: 🇯🇵
GSK Investigational Site, Tokyo, Japan

Trametinib With GSK2141795 in BRAF Wild-type Melanoma

Phase 2

Completed

Conditions: Melanoma

Interventions: Drug: Trametinib (GSK1120212)
Drug: GSK2141795

First Posted Date: 2013-09-13

Last Posted Date: 2020-02-12

Lead Sponsor: Adil Daud

Target Recruit Count: 20

Registration Number: NCT01941927

Locations: 🇺🇸
Memorial Sloan-Kettering Cancer Center, New York, New York, United States
🇺🇸
University of California, San Francisco, San Francisco, California, United States

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