General
Preferred name
Tepotinib
Synonyms
MSC-2156119J, MSC-2156119, EMD-1214063 ()
EMD-1214063 ()
MSC2156119 ()
EMD 1214063 ()
EMD1214063 ()
MSC-2156119 ()
MSC-2156119J ()
Tepotinib (EMD 1214063) ()
MSC2156119J ()
Tepotinib hydrochloride hydrate ()
Tepmetko ()
Tepotinib hydrochloride monohydrate ()
TEPOTINIB HYDROCHLORIDE ()
P&D ID
PD012734
CAS
1100598-32-0
Tags
available
drug
Approved by
FDA
PMDA
EMA
First approval
2021
2020
Drug indication
Solid tumour/cancer
Hepatocellular carcinoma
Non-small cell lung cancer
Drug Status
approved
investigational
Max Phase
4.0
Probe control
Probe control not defined
Orthogonal probes
0
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)
DESCRIPTION
Tepotinib is a potent and selective, orally available inhibitor of MET tyrosine kinase . It was designed to inhibit the pro-oncogenic signalling caused by MET gene alterations that occur in 3-5% of NSCLC cases, and which correlate with poor prognosis.
Novel tepotinib derivatives are being assessed for antiproliferative activity . (GtoPdb)
Novel tepotinib derivatives are being assessed for antiproliferative activity . (GtoPdb)
DESCRIPTION
On February 2021, FDA approved tepotinib to treat non-small cell lung cancer
(PKIDB)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
4
Organisms
0
Compound Sets
19
ChEMBL Approved Drugs
ChEMBL Drugs
Clinical kinase drugs
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
NCATS Inxight Approved Drugs
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
44
Molecular Weight
492.23
Hydrogen Bond Acceptors
8
Hydrogen Bond Donors
0
Rotatable Bonds
7
Ring Count
5
Aromatic Ring Count
4
cLogP
4.01
TPSA
96.93
Fraction CSP3
0.28
Chiral centers
0.0
Largest ring
6.0
QED
0.38
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Targets
MET
Pathway
Tyrosine Kinase/Adaptors
Autophagy
Protein Tyrosine Kinase/RTK
Target
c-Met
AXL
TrkA
c-Met/HGFR
Autophagy,c-Met
MOA
hepatocyte growth factor receptor inhibitor
Source data
