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

Concurrent Dabrafenib + Trametinib With Sterotactic Radiation in BRAF Mutation-Positive Malignant Melanoma and Brain Metastases

Phase 2

Terminated

Conditions: Melanoma
Brain Metastases

Interventions: Drug: Dabrafenib
Drug: Trametinib

First Posted Date: 2016-11-28

Last Posted Date: 2021-08-20

Lead Sponsor: Canadian Cancer Trials Group

Target Recruit Count: 6

Registration Number: NCT02974803

Locations: 🇨🇦
QEII Health Sciences Centre, Halifax, Nova Scotia, Canada
🇨🇦
Saskatoon Cancer Centre, Saskatoon, Saskatchewan, Canada
🇨🇦
Odette Cancer Centre, Toronto, Ontario, Canada

and more 3 locations

A Phase Ib Study of LXH254-centric Combinations in NSCLC or Melanoma

Phase 1

Terminated

Conditions: Non-Small Cell Lung Cancer
Melanoma

Interventions: Drug: LXH254
Drug: LTT462
Drug: Trametinib
Drug: Ribociclib

First Posted Date: 2016-11-28

Last Posted Date: 2025-04-13

Lead Sponsor: Novartis Pharmaceuticals

Target Recruit Count: 241

Registration Number: NCT02974725

Locations: 🇸🇪
Novartis Investigative Site, Stockholm, Sweden
🇺🇸
Uni of TX MD Anderson Cancer Cntr, Houston, Texas, United States
🇺🇸
Sarah Cannon Research Institute Tennessee Oncology, Nashville, Tennessee, United States

and more 4 locations

A Study of the Anti-PD1 Antibody PDR001, in Combination With Dabrafenib and Trametinib in Advanced Melanoma

Phase 3

Terminated

Conditions: Melanoma

Interventions: Biological: Spartalizumab
Other: Placebo
Drug: Dabrafenib
Drug: Trametinib

First Posted Date: 2016-11-18

Last Posted Date: 2025-04-29

Lead Sponsor: Novartis Pharmaceuticals

Target Recruit Count: 568

Registration Number: NCT02967692

Locations: 🇺🇸
California Cancer Associates for Research and Excellence, Encinitas, California, United States
🇺🇸
UC Irvine Medical Center, Orange, California, United States
🇺🇸
California Pacific Medical Center, San Francisco, California, United States

and more 15 locations

Pharmacokinetics of Single and Repeat Oral Doses of Trametinib in Chinese Subjects With Solid Tumours

Phase 1

Withdrawn

Conditions: Cancer

Interventions: Drug: Trametinib

First Posted Date: 2016-10-20

Last Posted Date: 2018-09-14

Lead Sponsor: GlaxoSmithKline

Registration Number: NCT02939846

The Drug Rediscovery Protocol (DRUP Trial)

First Posted Date: 2016-10-05

Last Posted Date: 2024-01-24

Lead Sponsor: The Netherlands Cancer Institute

Target Recruit Count: 1550

Registration Number: NCT02925234

Locations: 🇳🇱
Meander medisch centrum, Amersfoort, Netherlands
🇳🇱
Netherlands Cancer Institute, Amsterdam, Netherlands
🇳🇱
Amsterdam UMC, locatie AMC, Amsterdam, Netherlands

and more 33 locations

A Clinical Trial of Patients With Melanoma

Phase 1

Withdrawn

Conditions: Melanoma

Interventions: Drug: Digoxin Combination
Drug: Dabrafenib
Drug: Trametinib

First Posted Date: 2016-09-27

Last Posted Date: 2018-05-15

Lead Sponsor: University of Texas Southwestern Medical Center

Registration Number: NCT02915666

Locations: 🇺🇸
University of Texas Southwestern Medical Center, Dallas, Texas, United States

Nivolumab With Trametinib and Dabrafenib, or Encorafenib and Binimetinib in Treating Patients With BRAF Mutated Metastatic or Unresectable Stage III-IV Melanoma

Phase 2

Active, not recruiting

Conditions: Stage IV Cutaneous Melanoma AJCC v6 and v7
Unresectable Melanoma
Stage IIIA Cutaneous Melanoma AJCC v7
Metastatic Malignant Neoplasm in the Brain
Metastatic Melanoma
Stage III Cutaneous Melanoma AJCC v7
Stage IIIB Cutaneous Melanoma AJCC v7
Stage IIIC Cutaneous Melanoma AJCC v7

Interventions: Drug: Dabrafenib
Drug: Binimetinib
Drug: Encorafenib
Other: Laboratory Biomarker Analysis
Biological: Nivolumab
Other: Pharmacological Study
Drug: Trametinib

First Posted Date: 2016-09-22

Last Posted Date: 2025-04-27

Lead Sponsor: M.D. Anderson Cancer Center

Target Recruit Count: 52

Registration Number: NCT02910700

Locations: 🇺🇸
M D Anderson Cancer Center, Houston, Texas, United States

A Study of PDR001 in Combination With CJM112, EGF816, Ilaris® (Canakinumab) or Mekinist® (Trametinib)

Phase 1

Completed

Conditions: Colorectal Cancer, Triple Negative Breast Cancer, NSCLC - Adenocarcinoma

Interventions: Biological: PDR001
Drug: EGF816
Biological: CJM112
Biological: ACZ885
Drug: TMT212

First Posted Date: 2016-09-14

Last Posted Date: 2022-03-29

Lead Sponsor: Novartis Pharmaceuticals

Target Recruit Count: 283

Registration Number: NCT02900664

Locations: 🇺🇸
Sarah Cannon Research Institute, Nashville, Tennessee, United States
🇺🇸
Sidney Kimmel Comprehensive Cancer Center SC-3, Baltimore, Maryland, United States
🇺🇸
Dana Farber Cancer Center, Boston, Massachusetts, United States

and more 2 locations

Trametinib in Treating Patients With Progressive Metastatic Hormone-Resistant Prostate Cancer

Phase 2

Active, not recruiting

Conditions: Hormone-Resistant Prostate Cancer
Stage IV Prostate Cancer
Recurrent Prostate Carcinoma
Metastatic Prostate Carcinoma

Interventions: Other: Laboratory Biomarker Analysis
Other: Quality-of-Life Assessment
Drug: Trametinib

First Posted Date: 2016-08-26

Last Posted Date: 2023-05-01

Lead Sponsor: Jonsson Comprehensive Cancer Center

Target Recruit Count: 14

Registration Number: NCT02881242

Locations: 🇺🇸
UCLA / Jonsson Comprehensive Cancer Center, Los Angeles, California, United States

BGB324 in Combination With Pembrolizumab or Dabrafenib/Trametinib in Metastatic Melanoma

Phase 1

Completed

Conditions: Melanoma

Interventions: Drug: dabrafenib and trametinib
Drug: BGB324+pembrolizumab
Drug: BGB324+dabrafenib and trametinib
Drug: pembrolizumab

First Posted Date: 2016-08-19

Last Posted Date: 2025-01-14

Lead Sponsor: Haukeland University Hospital

Target Recruit Count: 74

Registration Number: NCT02872259

Locations: 🇳🇴
St. Olavs Hospital, Trondheim, Norway
🇳🇴
Oslo University Hospital, Radiumhospitalet, Oslo, Norway
🇳🇴
Haukeland University Hospital, Bergen, Norway

and more 2 locations

Drug Development Updates

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