Drug · Small Molecule

Trametinib

CI-DRUG-00000602Explore in graph →NCIt C77908 CHEMBL2103875 CIViC Approved

Regulatory

Approvals (33)

Each record names the authority, jurisdiction, indication text and status. A drug approved in one jurisdiction for one indication is not 'approved' in general.

health-canada-dpdRegulatory33 approval records from 3 sources (hover a row badge for its dataset) · authority, jurisdiction and indication text as published.

Jurisdiction · authority	Cancer	Indication	Status	Approval date	Source
CA Health Canada	—	Marketed in Canada as MEKINIST (DIN 02539993) under ATC L01EE01 TRAMETINIB. Indications are not published in the Drug Product Database — see the Health Canada Product Monograph.	approvedsource: Marketed	Nov 30, 2023	health-canada-dpd
CA

Health Canada records are DIN-level: one row per marketed product (brand, strength, form). The Drug Product Database does not publish indications, so no cancer is stated for these rows, and a cancelled or dormant DIN is the status of that one product — not a withdrawal of the molecule.

Data updated 19 hours agoSource updated unknown

Derived

Development pipeline

Most advanced stage across all cancers, then per top-level cancer reached through trial conditions or approval indications. Approval in any ingested jurisdiction outranks trial phase; counts are interventional studies.

Scope	Stage	Max phase	Active	Recruiting	Phase 3	Trials	Approvals	Jurisdictions	First approval	First trial
All cancers	Approved	Phase 4	67	24	13	214	33	CA, EU, US	May 29, 2013	Jul 28, 2008
Malignant Thyroid Gland Neoplasm	Approved	Phase 3	10	3	2	16	2	US	May 29, 2013	2011-10
Malignant Lung Neoplasm	Approved	Phase 4	8	2	1	26	2	US	May 29, 2013	2011-09
Malignant Central Nervous System Neoplasm	Phase4	Phase 4	2	0	0

Curated evidence

Clinical evidence (162)

CIViC items in which this therapy appears, grouped by cancer context, then molecular profile. 50 items per page.

civicCuratedShowing 151–162 of 162 evidence items · levels, directions and significance as curated at the source; each row links to its CIViC record.

Therapy	Cancer	Type	Level	Direction · significance	Rating (1–5)	Status	Evidence	Source
BRAF V600E1
Dabrafenib + Trametinib

Clinical trials

Trials with this intervention (224)

Most recently updated first, 50 per page.

clinicaltrialsPublishedShowing 1–50 of 224 studies · status and phase as posted by the registrant; each row links to the study record.

NCT	Title	Status	Phase	Enrollment (n)	Sponsor	Countries	Last update	Source
NCT02015117	Trametinib With or Without Whole Brain Radiation Therapy in Treating Patients With Brain Metastases	active not recruiting	Phase 1	10	National Cancer Institute (NCI)NIH	1	Sep 25, 2026	clinicaltrials
NCT06475989	Study of Targeted Therapy vs. Chemotherapy in Patients With Thyroid Cancer	recruiting	Phase 3

Molecule

Record

Kind: Small Molecule
Mechanism: Dual specificity mitogen-activated protein kinase kinase 2 inhibitor; Dual specificity mitogen-activated protein kinase kinase 1 inhibitor; Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor
Targets: 2 genes
UNII: BSB9VJ5TUT
Aliases: CPD 8B, GSK 1120212, GSK-1120212, GSK1120212, GSK1120212B, GSK-1120212TRAMETINIBMEKINISTA-1083G1357N-(3-{3-CYCLOPROPYL-5-[(2-FLUORO-4-IODOPHENYL)AMINO]-6,8-DIMETHYL-2,4,7-TRIOXO-3,4,6,7-TETRAHYDROPYRIDO[4,3-D]PYRIMIDIN-1(2H)-YL}PHENYL)ACETAMIDE GENERAL, GSK 212, GSK212, JTP 74057, JTP74057, MEK Inhibitor GSK1120212, Mekinist, N-(3-{3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl}phenyl)acetamide, Spexotras, Tmt212, TMT-212, TMT212, Trametinib, TRAMETINIB DIMETHYL SULFOXIDE, TRAMETINIB (GSK1120212)

Data updated 22 hours agoSource updated unknown

Identifiers

Codes (11)

Upstream identifiers kept as first-class codes; each links to its registry where a stable public URL exists.

System	Code	Label
ATC (WHO)	L01EE01	TRAMETINIB

BRAF Fusion1

Trametinib

Transitional Cell Carcinoma

Predictive

Supports Sensitivity Response

accepted

EID7763

In a case report, a patient with metastatic urothelial carcinoma harboring an NRF1-BRAF fusion was treated with trametinib. After two and a half months of treatment, MRI revealed 48.4% decrease in siz… (full text at CIViC)

PMID 31010895 · Isaacson et al., 2019 · Open in CIViC

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DDX43 Overexpression1

Mirdametinib + Selumetinib + TrametinibSubstitutes

Uveal Melanoma

Predictive

Supports Resistance

accepted

EID1135

MEK inhibitor-resistant (selumetinib, PD0325901, GSK1129212) uveal melanoma cell lines were created from two GNAQ Q209L mutant cell lines. Overexpression of DDX43 mediated RAS-induced selumetinib resi… (full text at CIViC)

PMID 24899684 · Ambrosini et al., 2014 · Open in CIViC

civic

ERBB3 Overexpression1

Selumetinib + TrametinibSubstitutes

Uveal Melanoma

Predictive

Supports Resistance

submitted

EID3050

MEK inhibitors improve survival in cutaneous melanoma patients but show only modest efficacy in metastatic uveal melanoma patients. In this study, we screened for growth factors that elicited resistan… (full text at CIViC)

PMID 25952648 · Cheng et al., 2015 · Open in CIViC

Predictive

Supports Sensitivity Response

accepted

EID1228

Phase 1 study of trametinib in 97 patients with melanoma (16 with uveal melanoma). Analysis in patients with uveal melanoma identified GNAQ and GNA11 mutations in six patients, in which three SD and t… (full text at CIViC)

PMID 22805292 · Falchook et al., 2012 · Open in CIViC

Predictive

Supports Sensitivity Response

accepted

EID1229

PMID 22805292 · Falchook et al., 2012 · Open in CIViC

civic

MET Overexpression1

Selumetinib + TrametinibSubstitutes

Uveal Melanoma

Predictive

Supports Resistance

accepted

EID3038

In this study the authors screened for growth factors that elicited resistance in newly characterized metastatic uveal melanoma cell lines to clinical-grade MEK inhibitors, trametinib and selumetinib,… (full text at CIViC)

PMID 25952648 · Cheng et al., 2015 · Open in CIViC

civic

BRAF Fusion1

Trametinib

Large Congenital Melanocytic NevusUNRESOLVED

Predictive

Supports Sensitivity Response

submitted

EID7759

Case report of a 7-year-old girl with a giant congenital melanocytic nevus that had an AKAP9-BRAF fusion and was treated with trametinib, which resulted in rapid resolution of the patient's pain and p… (full text at CIViC)

PMID 30792255 · Mir et al., 2019 · Open in CIViC

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BRAF Mutation1

Trametinib

Low-grade Serous Ovarian CarcinomaUNRESOLVED

Predictive

Supports Sensitivity Response

submitted

EID13127

GOG-281/LOGS was a multinational, open-label, randomised phase 2/3 study evaluating trametinib against conventional therapy in recurrent low-grade serous ovarian or peritoneal carcinoma. A total of 26… (full text at CIViC)

PMID 35123694 · Gershenson et al., 2022 · Open in CIViC

civic

KRAS Mutation1

Trametinib

Low-grade Serous Ovarian CarcinomaUNRESOLVED

Predictive

Supports Sensitivity Response

submitted

EID13126

In the GOG-281/LOGS study, 260 patients with relapsed low-grade serous ovarian or peritoneal carcinoma were enrolled in an international, open-label, randomised phase 2/3 trial and allocated equally t… (full text at CIViC)

PMID 35123694 · Gershenson et al., 2022 · Open in CIViC

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NRAS Mutation1

Trametinib

Low-grade Serous Ovarian CarcinomaUNRESOLVED

Predictive

Supports Sensitivity Response

submitted

EID13128

GOG-281/LOGS was a multinational, open-label, randomised phase 2/3 study comparing trametinib with established systemic therapies in patients with recurrent low-grade serous carcinoma arising from the… (full text at CIViC)

PMID 35123694 · Gershenson et al., 2022 · Open in CIViC

civic

EPHA2 Expression1

Dasatinib + TrametinibCombination

Uterine Corpus Endometrial CarcinomaUNRESOLVED

Predictive

Supports Sensitivity Response

submitted

EID12577

In uterine corpus endometrial carcinoma (TCGA, n = 382), EPHA2 overexpression correlated with JAG1, MYC, NOTCH1, NOTCH3, and HES1 expression (Spearman r = 0.25-0.43; p < 0.01). Elevated MAP3K15, DLL3,… (full text at CIViC)

PMID 34391578 · Wu et al., 2021 · Open in CIViC

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