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

Dabrafenib and/or Trametinib Rollover Study

Phase 4

Recruiting

Conditions: Melanoma
Non Small Cell Lung Cancer
Solid Tumor
Rare Cancers
High Grade Glioma

Interventions: Drug: dabrafenib
Drug: trametinib

First Posted Date: 2017-11-13

Last Posted Date: 2025-04-06

Lead Sponsor: Novartis Pharmaceuticals

Target Recruit Count: 100

Registration Number: NCT03340506

Locations: 🇺🇸
Honor Health Research Institute, Scottsdale, Arizona, United States
🇺🇸
National Institute Of Health, Bethesda, Maryland, United States
🇺🇸
James Cancer Hospital and Solove Research Institute Ohio State, Columbus, Ohio, United States

and more 2 locations

Study of EGF816 in Combination With Selected Targeted Agents in EGFR-mutant NSCLC

Phase 1

Active, not recruiting

Conditions: EGFR-mutant Non-small Cell Lung Cancer

Interventions: Drug: EGF816
Drug: trametinib
Drug: LXH254
Drug: ribociclib
Drug: gefitinib
Drug: INC280

First Posted Date: 2017-11-06

Last Posted Date: 2025-05-08

Lead Sponsor: Novartis Pharmaceuticals

Target Recruit Count: 105

Registration Number: NCT03333343

Locations: 🇨🇳
Novartis Investigative Site, Taipei, Taiwan

Trametinib and Trifluridine and Tipiracil Hydrochloride in Treating Patients With Colon or Rectal Cancer That is Advanced, Metastatic, or Cannot Be Removed by Surgery

Phase 1

Completed

Conditions: Metastatic Colon Carcinoma
Metastatic Colorectal Carcinoma
Metastatic Rectal Carcinoma
RAS Family Gene Mutation
Stage III Colon Cancer AJCC v7
Stage III Colorectal Cancer AJCC v7
Stage III Rectal Cancer AJCC v7
Stage IIIA Colon Cancer AJCC v7
Stage IIIA Colorectal Cancer AJCC v7
Stage IIIA Rectal Cancer AJCC v7

Interventions: Other: Laboratory Biomarker Analysis
Drug: Trametinib
Drug: Trifluridine and Tipiracil Hydrochloride

First Posted Date: 2017-10-23

Last Posted Date: 2024-04-08

Lead Sponsor: City of Hope Medical Center

Target Recruit Count: 26

Registration Number: NCT03317119

Locations: 🇺🇸
City of Hope Antelope Valley, Lancaster, California, United States
🇺🇸
City of Hope Corona, Corona, California, United States
🇺🇸
City of Hope Medical Center, Duarte, California, United States

and more 5 locations

Pembrolizumab and Trametinib in Treating Patients With Stage IV Non-Small Cell Lung Cancer and KRAS Gene Mutations

Phase 1

Completed

Conditions: KRAS Gene Mutation
Metastatic Non-Squamous Non-Small Cell Lung Carcinoma
Stage IV Non-Small Cell Lung Cancer AJCC v7
Recurrent Non-Squamous Non-Small Cell Lung Carcinoma

Interventions: Biological: Pembrolizumab
Drug: Trametinib

First Posted Date: 2017-10-02

Last Posted Date: 2025-05-21

Lead Sponsor: Jonathan Riess

Target Recruit Count: 15

Registration Number: NCT03299088

Locations: 🇺🇸
University of California Davis Comprehensive Cancer Center, Sacramento, California, United States

INCB039110 in Combination With Dabrafenib and Trametinib in Patients With BRAF-mutant Melanoma and Other Solid Tumors.

Phase 1

Terminated

Conditions: Melanoma

Interventions: Drug: Trametinib
Drug: Dabrafenib
Drug: INCB039110

First Posted Date: 2017-09-05

Last Posted Date: 2023-09-22

Lead Sponsor: Massachusetts General Hospital

Target Recruit Count: 1

Registration Number: NCT03272464

Locations: 🇺🇸
Massachusetts General Hospital, Boston, Massachusetts, United States

A Dose Escalation Study to Investigate the Safety, Pharmacokinetics (PK), Pharmacodynamics (PD), and Clinical Activity of GSK525762 Plus Trametinib in Subjects With Solid Tumors

Phase 2

Withdrawn

Conditions: Solid Tumours

Interventions: Drug: GSK525762 Besylate tablets
Drug: Trametinib tablets

First Posted Date: 2017-08-30

Last Posted Date: 2017-12-08

Lead Sponsor: GlaxoSmithKline

Registration Number: NCT03266159

Efficacy of MEK (Trametinib) and BRAFV600E (Dabrafenib) Inhibitors With Radioactive Iodine (RAI) for the Treatment of Refractory Metastatic Differentiated Thyroid Cancer

Phase 2

Conditions: Metastatic Radioactive Iodine Refractory Thyroid Cancer Patients With RAS or BRAF Mutation

Interventions: Drug: Trametinib
Drug: Dabrafenib
Radiation: 131I
Drug: rhTSH

First Posted Date: 2017-08-10

Last Posted Date: 2021-09-28

Lead Sponsor: Gustave Roussy, Cancer Campus, Grand Paris

Target Recruit Count: 40

Registration Number: NCT03244956

Locations: 🇫🇷
Gustave Roussy, Villejuif, Val De Marne, France

Trametinib in Patients With Advanced Neurofibromatosis Type 1 (NF1)-Mutant Non-small Cell Lung Cancer

Phase 2

Terminated

Conditions: Non-small Cell Lung Cancer

Interventions: Drug: Trametinib

First Posted Date: 2017-07-28

Last Posted Date: 2019-12-03

Lead Sponsor: University of California, San Francisco

Target Recruit Count: 1

Registration Number: NCT03232892

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

Trametinib and Pembrolizumab in Treating Patients With Recurrent Non-small Cell Lung Cancer That Is Metastatic, Unresectable, or Locally Advanced

Phase 1

Active, not recruiting

Conditions: Recurrent Lung Non-Small Cell Carcinoma
Stage IIIC Lung Cancer AJCC v8
Stage III Lung Cancer AJCC v8
Stage IIIA Lung Cancer AJCC v8
Stage IIIB Lung Cancer AJCC v8
Stage IV Lung Cancer AJCC v8
Stage IVB Lung Cancer AJCC v8
Metastatic Lung Non-Small Cell Carcinoma
Stage IVA Lung Cancer AJCC v8
Unresectable Lung Non-Small Cell Carcinoma

Interventions: Biological: Pembrolizumab
Other: Pharmacokinetic Study
Drug: Trametinib

First Posted Date: 2017-07-21

Last Posted Date: 2025-01-24

Lead Sponsor: M.D. Anderson Cancer Center

Target Recruit Count: 37

Registration Number: NCT03225664

Locations: 🇺🇸
M D Anderson Cancer Center, Houston, Texas, United States
🇺🇸
Yale University, New Haven, Connecticut, United States

Trametinib in Treating Patients With Relapsed or Refractory Juvenile Myelomonocytic Leukemia

Phase 2

Active, not recruiting

Conditions: Juvenile Myelomonocytic Leukemia
Neurofibromatosis Type 1

Interventions: Procedure: Bone Marrow Aspiration and Biopsy
Drug: Trametinib

First Posted Date: 2017-06-19

Last Posted Date: 2025-01-16

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 10

Registration Number: NCT03190915

Locations: 🇺🇸
Children's Healthcare of Atlanta - Arthur M Blank Hospital, Atlanta, Georgia, United States
🇺🇸
Children's Hospital of Alabama, Birmingham, Alabama, United States
🇺🇸
Phoenix Childrens Hospital, Phoenix, Arizona, United States

and more 54 locations

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