Trametinib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2013
- First approval year
- 2013
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Trametinib
- Molecular weight
- 615.4
- Structure (SMILES)
- CC(=O)Nc1cccc(-n2c(=O)n(C3CC3)c(=O)c3c(Nc4ccc(I)cc4F)n(C)c(=O)c(C)c32)c1
- mekinist
- Mekinist
- carboplatin gsk1120212
- cpd 8b
- CPD 8B
- gsk 1120212
- GSK 1120212
- 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-1120212
- 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
- gsk1120212
- GSK1120212
- GSK1120212 (trametinib)
- gsk1120212b
- GSK1120212B
- jtp 74057
- JTP 74057
- JTP-74057
- mekinist
- MEKINIST
- tmt 212
- TMT-212
- tmt212
- Tmt212
- TMT212
- trametinib
- Trametinib
And 30 more, listed on the interactive page.
- ATC classification codes
- L01EE01
Sources for recorded values
- CAS registry numbers
- 871700-17-3
- ChEMBL ID
- CHEMBL2103875
- InChIKey
- LIRYPHYGHXZJBZ-UHFFFAOYSA-N
- PubChem compound IDs
- 11707110
- FDA ingredient codes (UNII)
- 33E86K87QN
- 1425098
- 1425099
- Applicant
- NOVARTIS
- Approval date
- 29 May 2013
- Application number
- NDA204114
- Status
- Authorised
- Status date
- 30 Jun 2014
- Authorisation date
- 30 Jun 2014
- Approved indications
- Melanoma Trametinib as monotherapy or in combination with dabrafenib is indicated for the treatment of adults and adolescents aged 12 years and older with unresectable or metastatic melanoma with a BRAF V600 mutation (see sections 4.4 and 5.1). Trametinib monotherapy has not demonstrated clinical activity in patients who have progressed on a prior BRAF inhibitor therapy (see section 5.1). Adjuvant treatment of melanoma Trametinib in combination with dabrafenib is indicated for the adjuvant treatment of adults and adolescents aged 12 years and older with Stage III melanoma with a BRAF V600 mutation, following complete resection. Non-small cell lung cancer (NSCLC) Trametinib in combination with dabrafenib is indicated for the treatment of adults with advanced non-small cell lung cancer with a BRAF V600 mutation. Differentiated thyroid cancer (DTC) Trametinib in combination with dabrafenib is indicated for the treatment of adult patients with locally advanced or metastatic differentiated thyroid cancer with a BRAF V600E mutation, refractory to or not eligible for radioactive iodine (RAI) who have progressed during or after prior systemic therapy (for biomarker-based patient selection, see section 4.2).
- Product number
- EMEA/H/C/002643
- Authorisation holder
- Novartis Europharm Limited
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Melanoma
European medicines record
- Patents
- 0
- Designations
- 4
- First in class
- Yes
- Fast track
- Yes
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Pharmacology name
- trametinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- mitogen-activated protein kinase kinase 2
- Gene symbol
- MAP2K2
- Protein identifier
- P36507
- Median affinity
- 8.74
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- mitogen-activated protein kinase kinase 1
- Gene symbol
- MAP2K1
- Protein identifier
- Q02750
- Affinity units
- pIC50
- Primary target
- Yes
- Mechanism
- Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor
- Action type
- Inhibitor
- Target
- Dual specificity mitogen-activated protein kinase kinase; MEK1/2
- Protein identifier
- P36507
- Mechanism
- Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor
- Action type
- Inhibitor
- Target
- Dual specificity mitogen-activated protein kinase kinase; MEK1/2
- Protein identifier
- Q02750
- Mechanism
- Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
- Action type
- Inhibitor
- Target
- Dual specificity mitogen-activated protein kinase kinase 1
- Mechanism
- Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
- Action type
- Inhibitor
- Target
- Dual specificity mitogen-activated protein kinase kinase 2
- Mechanism
- Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor
- Action type
- Inhibitor
- Target
- Dual specificity mitogen-activated protein kinase kinase; MEK1/2
- Action type
- Inhibitor
- Gene symbol
- MAP2K2
- Protein identifier
- P36507
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- MAP2K1
- Protein identifier
- Q02750
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Carcinoma, Hepatocellular
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000182
- Subject identifier
- D006528
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000196
- Subject identifier
- D011471
- Condition
- Leukemia, Myeloid, Acute
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000222
- Subject identifier
- D015470
- Condition
- Breast Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000305
- Subject identifier
- D001943
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000365
- Subject identifier
- D015179
- Condition
- Melanoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000389
- Subject identifier
- D008545
- Condition
- Adenocarcinoma, Follicular
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000501
- Subject identifier
- D018263
- Condition
- Leukemia
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000565
- Subject identifier
- D007938
- Condition
- Adenocarcinoma of Lung
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000571
- Subject identifier
- D000077192
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Thyroid Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000641
- Subject identifier
- D013964
- Condition
- Melanoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000756
- Subject identifier
- D008545
- Condition
- Multiple Myeloma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001378
- Subject identifier
- D009101
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001663
- Subject identifier
- D011471
- Condition
- Melanoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:0002617
- Subject identifier
- D008545
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002618
- Subject identifier
- D010190
- Condition
- Thyroid Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0002892
- Subject identifier
- D013964
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Mouth Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003868
- Subject identifier
- D009062
- Condition
- Biliary Tract Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003891
- Subject identifier
- D001661
- Condition
- Cholangiocarcinoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005221
- Subject identifier
- D018281
- Condition
- Triple Negative Breast Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005537
- Subject identifier
- D064726
- Condition
- Carcinoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0006772
- Subject identifier
- D002277
- Condition
- Craniopharyngioma
- Highest recorded phase
- 2
- Condition identifier
- EFO:1000209
- Subject identifier
- D003397
- Condition
- Thyroid Carcinoma, Anaplastic
- Highest recorded phase
- 2
- Condition identifier
- EFO:1000595
- Subject identifier
- D065646
And 27 more, listed on the interactive page.
- Condition identifier
- EFO_0000389
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000658
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000756
- Condition identifier
- EFO_0001378
- Highest recorded phase
- 2
- Condition identifier
- EFO_0002617
- Condition identifier
- EFO_0002618
- Highest recorded phase
- 2
- Condition identifier
- EFO_0002892
- Highest recorded phase
- 3
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003868
- Highest recorded phase
- 2
- Condition identifier
- EFO_0004920
- Highest recorded phase
- 2
- Condition identifier
- EFO_0005221
- Condition identifier
- EFO_0006772
- Highest recorded phase
- 2
- Condition identifier
- EFO_0020985
- Highest recorded phase
- 1
- Condition identifier
- EFO_0700100
- Condition identifier
- EFO_0700100
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000209
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000318
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000447
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000616
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000760
- Highest recorded phase
- 1
- Condition identifier
- EFO_1000849
- Highest recorded phase
- 1
- Condition identifier
- EFO_1001480
- Highest recorded phase
- 2
- Condition identifier
- HP_0100727
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0000873
- Highest recorded phase
- 1
And 83 more, listed on the interactive page.
- Event
- blood creatine phosphokinase increased
- Reports
- 142
- Reporting signal score
- 152.911
- Event
- chills
- Reports
- 416
- Reporting signal score
- 575.595
- Event
- chorioretinopathy
- Reports
- 43
- Reporting signal score
- 111.405
- Event
- dehydration
- Reports
- 189
- Reporting signal score
- 99.7476
- Event
- dermatitis acneiform
- Reports
- 66
- Reporting signal score
- 144.965
- Event
- detachment of retinal pigment epithelium
- Reports
- 29
- Reporting signal score
- 79.8597
- Event
- ejection fraction decreased
- Reports
- 150
- Reporting signal score
- 290.747
- Event
- malignant melanoma
- Reports
- 88
- Reporting signal score
- 160.364
- Event
- malignant neoplasm progression
- Reports
- 428
- Reporting signal score
- 765.955
- Event
- metastases to central nervous system
- Reports
- 92
- Reporting signal score
- 187.069
- Event
- metastatic malignant melanoma
- Reports
- 75
- Reporting signal score
- 281.22
- Event
- panniculitis
- Reports
- 68
- Reporting signal score
- 200.682
- Event
- pyrexia
- Reports
- 1,612
- Reporting signal score
- 2,570.24
- Event
- rash
- Reports
- 492
- Reporting signal score
- 215.667
- Event
- uveitis
- Reports
- 126
- Reporting signal score
- 266.421
- Event
- visual impairment
- Reports
- 141
- Reporting signal score
- 113.279
- NCT00687622
- NCT01155453
- NCT01324258
- NCT01767454
- NCT01827384
- NCT01928940
- NCT01938443
- NCT02079740
- NCT02705963
- NCT02925234
- NCT03065387
- NCT03266159
- NCT04111458
- NCT04116541
- NCT04185883
- NCT05071183
- NCT05159245
- NCT05907304
- NCT00920140
- NCT01037127
- NCT01072175
- NCT01138085
- NCT01192165
- NCT01231581
- NCT01231594
And 149 more, listed on the interactive page.
- Dose
- 2 mg
- Route
- Oral
- How often
- Once daily
Conditions of use
- Take on an empty stomach (at least 1 hour before or 2 hours after a meal)
- Hydrogen bond acceptors
- 8
- Hydrogen bond donors
- 2
- Polar surface area
- 107.13
- Calculated partition coefficient (ALogP)
- 3.94
- Calculated partition coefficient (XLogP)
- 3.4
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 1
- Rotatable bonds
- 5
- Heavy atoms
- 37
- Molecular formula
- C26H23FIN5O4
- Monoisotopic mass
- 615.07788
- Natural product
- No
- Recorded assays
- 2,249
- Active assays
- 398
- Confirmatory
- Other
- Screening
- Antineoplastic Agents
- Protein Kinase Inhibitors
These details could not be displayed.
Related records
Trials (647)
- "Cocktail" Therapy for Hepatitis B Related Hepatocellular Carcinoma
- "Dabrafenib and Trametinib in Circulating Free DNA BRAFV600 Mutated Metastatic Melanoma Patients: a Prospective Phase II, Open Label, Multicentre Study - (Bioliquid TAILOR Study - BIOTAILOR)"
- 24VA021; VATCH Trametinib for Ras/MAPK Pathway VAs
- 601 Versus Ranibizumab in Patients With Branch Retinal Vein Occlusion (BRVO)
- 601 Versus Ranibizumab in Patients With Central Retinal Vein Occlusion (CRVO)
- A Bioequivalence Study Comparing A Fixed Dose Combination Formulation Of Myrin P Forte That Contains Rifampicin, Isoniazid, Ethambutol And Pyrazinamide Per Tablet To An Equivalent Dose Of Single Drug Reference Preparations Of Similar Combination Following Oral Administration In Healthy Adults
- A Clinical Study Evaluating the Safety and Efficacy of BCMA-GPRC5D CAR-T in Patients With Relapsed/Refractory Multiple Myeloma Who Have Received Three or More Lines of Treatment
- A Clinical Study Evaluating the Safety, Tolerability, and Efficacy of MT1013 in Hemodialysis Subjects With Secondary Hyperparathyroidism
- A Clinical Study Evaluating the Safety, Tolerability, and Initial Efficacy of Single Intravenous Infusion of JWK007 in Patients With Duchenne Muscular Dystrophy (DMD)
- A Clinical Study, to Evaluate the Safety and Tolerability of Intradermal IMM-101 in Adult Melanoma Cancer Patients
- A Clinical Trial of Patients With Melanoma
- A Clinical Trial to Evaluate a Melanoma Helper Peptide Vaccine Plus Dabrafenib and Trametinib
- A Cohort Study on the Safety and Efficacy of XH-02 in Treating Hypoparathyroidism
- A Combination Product of Sumatriptan and Naproxen Sodium Versus Single-entity Oral Triptans: An Analysis of Real World Data
- A Comparison of VR647 and Conventionally Nebulized Budesonide in Healthy Volunteers and Adult Asthma Subjects
- A Dose Escalation Study to Assess Safety of GSK2256098 (FAK Inhibitor) in Combination With Trametinib (MEK Inhibitor) in Subjects With Advanced Solid Tumors
- A Dose Escalation Study to Investigate the Safety, Pharmacokinetics (PK), Pharmacodynamics (PD), and Clinical Activity of GSK525762 Plus Trametinib in Subjects With Solid Tumors
- A Drug-Drug Interaction Study to Assess the Effect of Trametinib on the Pharmacokinetics of an Oral Contraceptive in Female Patients With Solid Tumors
- A First in Human Single and Multiple Ascending Dose and Open Label Food Effect Study of OR-101 in Healthy Subjects
- A First in Human Study to Evaluate the Safety, Tolerability and Pharmacokinetics of Single and Multiple Ascending Doses of Inhaled ETD001 in Healthy Subjects
Approved for (2)
- Cancer
- Neoplasm
In development for (51)
- Acute myeloid leukemia Phase 2
- Ameloblastoma Phase 2
- Amyotrophic lateral sclerosis Phase 1
- Arteriovenous malformations of the brain Phase 2
- Biliary tract neoplasm Phase 2
- Breast cancer Phase 2
- Breast carcinoma Phase 2
- Bronchial neoplasm Phase 1
- Cervical cancer Phase 2
- Cholangiocarcinoma Phase 2
- Colorectal adenocarcinoma Phase 2
- Colorectal cancer Phase 2
- Colorectal carcinoma Phase 2
- Craniopharyngioma Phase 2
- Cutaneous melanoma Phase 3
- Epithelioid hemangioendothelioma Phase 2
- Erdheim-Chester disease Phase 2
- Exocrine pancreatic carcinoma Phase 2
- Gastric cancer Phase 1
- Gastrointestinal stromal tumor Phase 2