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trametinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
MEK (MAPK kinase) tyrosine kinase inhibitors	4802	871700-17-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: GSK1120212B trametinib dimethyl sulfoxide trametinib GSK1120212 mekinist	a reversible inhibitor of mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and MEK2 activation and of MEK1 and MEK2 kinase activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway, which promotes cellular proliferation Molecular weight: 615.40 Formula: C26H23FIN5O4 CLOGP: 4.68 LIPINSKI: 1 HAC: 9 HDO: 2 TPSA: 102.06 ALOGS: -4.30 ROTB: 5 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

GSK1120212B
trametinib dimethyl sulfoxide
trametinib
GSK1120212
mekinist

a reversible inhibitor of mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and MEK2 activation and of MEK1 and MEK2 kinase activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway, which promotes cellular proliferation

Molecular weight: 615.40
Formula: C26H23FIN5O4
CLOGP: 4.68
LIPINSKI: 1
HAC: 9
HDO: 2
TPSA: 102.06
ALOGS: -4.30
ROTB: 5

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
2	mg	O

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	229 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	13.94 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.03 %	Lombardo F, Berellini G, Obach RS

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Approvals:

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Date	Agency	Company
June 30, 2014	EMA	NOVARTIS EUROPHARM LIMITED
March 28, 2016	PMDA	Novartis Pharma K.K.
May 29, 2013	FDA	NOVARTIS PHARMS CORP

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FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Pyrexia	1326.38	18.99	1053	16096	469425	63002448
Malignant neoplasm progression	1021.03	18.99	479	16670	81642	63390231
Chills	372.09	18.99	280	16869	113098	63358775
Product use in unapproved indication	335.15	18.99	320	16829	178760	63293113
Death	299.65	18.99	432	16717	373949	63097924
Uveitis	225.26	18.99	95	17054	12458	63459415
Visual impairment	196.93	18.99	171	16978	84275	63387598
Metastases to central nervous system	188.91	18.99	85	17064	13020	63458853
Rash	183.09	18.99	440	16709	560431	62911442
Ejection fraction decreased	135.58	18.99	81	17068	22251	63449622

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Pyrexia	1272.24	17.89	1149	16212	331864	34607706
Malignant neoplasm progression	820.29	17.89	521	16840	87525	34852045
Metastases to central nervous system	395.56	17.89	150	17211	8055	34931515
Chills	379.70	17.89	317	17044	80726	34858844
Death	251.77	17.89	585	16776	397464	34542106
Product use in unapproved indication	195.59	17.89	265	17096	117234	34822336
Ejection fraction decreased	186.46	17.89	117	17244	19037	34920533
Rash	132.87	17.89	321	17040	222431	34717139
Visual impairment	121.50	17.89	117	17244	35685	34903885
Uveitis	118.72	17.89	63	17298	7472	34932098

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Pyrexia	1929.60	16.52	1694	25864	677015	79039815
Malignant neoplasm progression	1456.73	16.52	776	26782	135214	79581616
Chills	478.62	16.52	415	27143	159819	79557011
Metastases to central nervous system	438.59	16.52	177	27381	16198	79700632
Death	361.73	16.52	676	26882	565838	79150992
Ejection fraction decreased	326.13	16.52	182	27376	34395	79682435
Uveitis	273.79	16.52	128	27430	16702	79700128
Product use in unapproved indication	225.53	16.52	349	27209	250010	79466820
Blood creatine phosphokinase increased	208.71	16.52	177	27381	65913	79650917
Dermatitis acneiform	181.29	16.52	82	27476	9911	79706919

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01EE01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Mitogen-activated protein kinase (MEK) inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:79091	MEK inhibitor
CHEBI has role	CHEBI:149553	anticoronaviral drug
CHEBI has role	CHEBI:176497	geroprotectors
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000175076	Protein Kinase Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID
Locally advanced or metastatic anaplastic thyroid cancer (ATC) with BRAF V600E mutation	indication	255031003
Metastatic malignant melanoma	indication	443493003
Malignant Melanoma with BRAF V600E Mutation	indication	830150003
Malignant Melanoma with BRAF V600K Mutation	indication
Metastatic non-small cell lung cancer (NSCLC) with BRAF V600E mutation	indication
Unresectable or metastatic solid tumors with BRAF V600E mutation	indication

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 0.05MG BASE/ML	MEKINIST	NOVARTIS	N217513	March 16, 2023	RX	SOLUTION	ORAL	8835443	June 10, 2025	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA (LGG) WITH A BRAF V600E MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 0.05MG BASE/ML	MEKINIST	NOVARTIS	N217513	March 16, 2023	RX	SOLUTION	ORAL	8703781	Oct. 15, 2030	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA (LGG) WITH A BRAF V600E MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8835443	June 10, 2025	IN COMBINATION WITH DABRAFENIB FOR THE TREATMENT OF UNRESECTABLE OR METASTATIC MELANOMA.
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8835443	June 10, 2025	MEKINIST IS INDICATED, AS A SINGLE AGENT OR IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8835443	June 10, 2025	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8835443	June 10, 2025	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8835443	June 10, 2025	MEKINIST IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8835443	June 10, 2025	TREATMENT OF UNRESECTABLE OR METASTATIC MELANOMA
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8703781	Oct. 15, 2030	MEKINIST IN COMBINATION WITH DABRAFENIB FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	8703781	Oct. 15, 2030	MEKINIST IS INDICATED, AS A SINGLE AGENT OR IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF PATIENTS WITH UNRESECTABLE OR METASTATIC MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 0.05MG BASE/ML	MEKINIST	NOVARTIS	N217513	March 16, 2023	RX	SOLUTION	ORAL	March 16, 2026	NEW PRODUCT
EQ 0.05MG BASE/ML	MEKINIST	NOVARTIS	N217513	March 16, 2023	RX	SOLUTION	ORAL	March 16, 2030	TREATMENT OF PEDIATRIC PATIENTS 1 YEAR OF AGE AND OLDER WITH LOW-GRADE GLIOMA (LGG) WITH A BRAF V600E MUTATION WHO REQUIRE SYSTEMIC THERAPY
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	June 22, 2024	TRAMETINIB IN COMBINATION WITH DABRAFENIB, FOR THE TX. OF PTS WITH METASTATIC NON-SMALL CELL LUNG CANCER WITH BRAF V600E MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	Dec. 22, 2024	PEDIATRIC EXCLUSIVITY
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	April 30, 2025	TRAMETINIB IS INDICATED, IN COMBINATION WITH DABRAFENIB, FOR THE ADJUVANT TREATMENT OF PATIENTS WITH MELANOMA WITH BRAF V600E OR V600K MUTATIONS, AS DETECTED BY AN FDA-APPROVED TEST, AND INVOLVEMENT OF LYMPH NODE(S), FOLLOWING COMPLETE RESECTION
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	May 4, 2025	TRAMETINIB AND DABRAFENIB IN COMBINATION, FOR THE TREATMENT OF PATIENTS WITH LOCALLY ADVANCED OR METASTATIC ANAPLASTIC THYROID CANCER (ATC) WITH BRAF V600E MUTATION AND WITH NO SATISFACTORY LOCOREGIONAL TREATMENT OPTIONS
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	June 22, 2025	TRAMETINIB IS INDICATED IN COMBINATION WITH DABRAFENIB, FOR THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 6 YEARS OF AGE AND OLDER WITH UNRESECTABLE OR METASTATIC SOLID TUMORS WITH BRAF V600E MUTATION WHO HAVE PROGRESSED FOLLOWING PRIOR TREATMENT AND HAVE NO SATISFACTORY ALTERNATIVE TREATMENT OPTIONS
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	Oct. 30, 2025	PEDIATRIC EXCLUSIVITY
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	Nov. 4, 2025	PEDIATRIC EXCLUSIVITY
EQ 0.5MG	MEKINIST	NOVARTIS	N204114	May 29, 2013	RX	TABLET	ORAL	Dec. 22, 2025	PEDIATRIC EXCLUSIVITY

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Dual specificity mitogen-activated protein kinase kinase 2	Kinase	P36507	MP2K2_HUMAN	INHIBITOR	IC50	9.04	WOMBAT-PK	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 1	Kinase	Q02750	MP2K1_HUMAN	INHIBITOR	IC50	8.75	WOMBAT-PK	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		EC50	6.61	CHEMBL

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External reference:

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ID	Source
QOM	PDB_CHEM_ID
015044	NDDF
015045	NDDF
11707110	PUBCHEM_CID
1187431-43-1	SECONDARY_CAS_RN
1425098	RXNORM
203115	MMSL
29478	MMSL
33E86K87QN	UNII
4032511	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0666	TABLET, FILM COATED	0.50 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0666	TABLET, FILM COATED	0.50 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0666	TABLET, FILM COATED	0.50 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0666	TABLET, FILM COATED	0.50 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0668	TABLET, FILM COATED	2 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0668	TABLET, FILM COATED	2 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0668	TABLET, FILM COATED	2 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0668	TABLET, FILM COATED	2 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1105	TABLET, FILM COATED	0.50 mg	ORAL	NDA	32 sections
Mekinist	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1105	TABLET, FILM COATED	0.50 mg	ORAL	NDA	32 sections

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