General
Preferred name
TRAMETINIB
Synonyms
GSK1120212 ()
JTP-74057 ()
GSK-1120212 (DMSO solvate) ()
JTP-74057 (DMSO solvate) ()
GSK1120212, GSK1120212B, Trametinib Dimethyl Sulfoxide ()
GSK-1120212 ()
GSK1120212B ()
TRAMETINIB DIMETHYL SULFOXIDE ()
Trametinib DMSO solvate ()
GSK-1120212 DMSO solvate ()
GSK 1120212 ()
cpd 8b ()
MEKINIST ()
A-1083 ()
G1357 ()
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 GENERAL ()
Trametinib (DMSO solvate) ()
JTP 74057 ()
TMT-212 ()
TMT212 ()
Trametinib (GSK1120212) ()
JTP-74057, Mekinist ()
GSK1120212, JTP-74057, Mekinist ()
GSK-1120212B ()
Trametinib-d6 ()
Trametinib-13C-d3 ()
P&D ID
PD003250
CAS
871700-17-3
1187431-43-1
2712126-59-3
Tags
available
drug
probe
Approved by
FDA
PMDA
EMA
First approval
2013
Drug indication
Melanoma
Severe acute respiratory syndrome (SARS)
Middle East Respiratory Syndrome (MERS)
Discovery agent
Drug Status
approved
Max Phase
4.0
Probe info
Probe selectivity
family-selective
Probe type
experimental probe
P&D approved
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
21
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
INDICATION
Trametinib is indicated for the treatment of unresectable or metastatic melanoma with BRAF V600E or V600K mutations, as detected by an FDA-approved test [FDA].; ; In May 2018, it was approved for use with [DB08912] for the treatment of treat anaplastic thyroid cancer caused by an abnormal BRAF V600E gene [L2726].
DESCRIPTION
Trametinib is a Type-3 kinase inhibitor. Marketed formulations contain trametinib dimethyl sulfoxide (PubChem CID 50992434).
(GtoPdb)
TOXICITY
Most common adverse reactions (≥20%) for trametinib include rash, diarrhea, and lymphedema [FDA label].; ; The most common adverse reactions (≥20%) for Tafinlar in combination with Trametinib are pyrexia, chills, fatigue, rash, nausea, vomiting, diarrhea, abdominal pain, peripheral edema, cough, headache, arthralgia, night sweats, decreased appetite, constipation, and myalgia [FDA Label].; ; The following is a list of toxicities that may occur with the combination of Dabrafenib and Trametinib:; ; **New primary malignancies**: These may occur when Tafinlar is administered as a single agent or in combination with Trametinib. Monitor patients for new malignancies prior to initiation of therapy, while on therapy, and following discontinuation of TAFINLAR or the combination therapy. Tumor Promotion in BRAF Wild-Type Melanoma: Increased cell proliferation can occur with BRAF inhibitors [FDA Label].; ; **Hemorrhage**: Major hemorrhagic events can occur in patients receiving TAFINLAR in combination with trametinib. Monitor for signs and symptoms of bleeding [FDA Label].; ; **Venous Thromboembolism**: Deep vein thrombosis and pulmonary embolism can occur in patients receiving the drug combination [FDA Label].; ; **Cardiomyopathy**: Assess LVEF before treatment with TAFINLAR in combination with trametinib, after one month of treatment, then every 2 to 3 months thereafter [FDA Label].; ; **Ocular toxicities**: Perform an ophthalmologic evaluation for any visual disturbances [FDA Label].; ; **Serious Febrile Reactions**: Incidence and severity of pyrexia are increased with TAFINLAR in combination with trametinib [FDA Label].; ; **Serious Skin Toxicity**: Monitor for skin toxicities and for secondary infections. Discontinue for intolerable Grade 2, or Grade 3 or 4 rash not improving within 3 weeks despite the interruption of TAFINLAR [FDA Label].; ; **Hyperglycemia**: Monitor serum glucose levels in patients with pre-existing diabetes or hyperglycemia [FDA Label].; ; **Glucose-6-Phosphate Dehydrogenase Deficiency**: Closely monitor for hemolytic anemia [FDA Label].; ; **Embryofetal Toxicity**: Can cause fetal harm. Advise females of reproductive potential of potential risk to a fetus. TAFINLAR may render hormonal contraceptives less effective and an alternative method of contraception should be used [FDA Label].
MOA
Allosteric inhibitor
(Chemical Probes.org)
DESCRIPTION
inhibitor of MEK1 and MEK2
(Informer Set)
DESCRIPTION
Trametinib is indicated for the treatment of unresectable or metastatic melanoma with BRAF V600E or V600K mutations, as detected by an FDA-approved test.
(PKIDB)
DESCRIPTION
Trametinib is a reversible, selective, allosteric MEK1/MEK2 kinase activity inhibitor with IC50 of 0.7 and 0.9 nM for MEK1 and MEK2.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
7
Organisms
1
Compound Sets
39
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
ChEMBL Approved Drugs
ChEMBL Drugs
Chemical Probes.org
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP Approved Drugs
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
High-quality chemical probes
Informer Set
Kinase Inhibitors (best-in-class)
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
NCATS Inxight Approved Drugs
NIH Approved Oncology Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
Welcome Trust Cancer Drugs
ZINC Tool Compounds
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
65
Molecular Weight
615.08
Hydrogen Bond Acceptors
8
Hydrogen Bond Donors
2
Rotatable Bonds
5
Ring Count
5
Aromatic Ring Count
4
cLogP
3.94
TPSA
107.13
Fraction CSP3
0.23
Chiral centers
0.0
Largest ring
6.0
QED
0.33
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
MAP2K1
MAP2K2
MEK1, MEK2
MAP2K
MEK1/2
MEK1
MEK2
MAP2K1, MAP2K2
BRAF
Apoptosis related,Autophagy,MEK
Compound status
clinical
Pathway
ERK MAPK signaling
MAPK
Apoptosis
Autophagy
MAPK/ERK Pathway
Kinase group
STE
Targets
MAP2K1,MAP2K2
MOA
MEK
MEK inhibitor
MEK1 Inhibitors
MEK2 Inhibitors
Mitogen-Activated Protein (MAP) Kinase Kinase (MEK) Inhibitors
Inhibitors of Signal Transduction Pathways
Member status
member
Indication
melanoma
Target class
Protein kinase
Kinase, Kinase
Orthogonal probe
Selumetinib
Therapeutic Class
Antiviral Agents
Target subclass
STE, STE
Recommended Cell Concentration
100 nM
Source data
