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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5424 1100598-32-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tepotinib
  • tepotinib hydrochloride
  • tepmetko
  • EMD-1214063
  • MSC-2156119
  • MSC-2156119J
Tepotinib is a MET (mesenchymal-epithelial transition factor) tyrosine kinase inhibitor being developed for the treatment of solid tumours. It selectively binds to MET and inhibits MET phosphorylation disrupting the oncogenic MET receptor signalling caused by MET gene alterations, including both MET exon 14 (METex14) skipping alterations and MET protein overexpression. This results in cell death in tumour cells overexpressing MET protein or expressing constitutively activated MET protein.
  • Molecular weight: 492.58
  • Formula: C29H28N6O2
  • CLOGP: 3.40
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 0
  • TPSA: 94.71
  • ALOGS: -4.69
  • ROTB: 7

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Feb. 16, 2022 EMA Merck Europe B.V.
Feb. 3, 2021 FDA EMD SERONO INC
March 25, 2020 PMDA Merck KGaA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EX21 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Other protein kinase inhibitors
MeSH PA D000970 Antineoplastic Agents
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000193929 Mesenchymal Epithelial Transition Inhibitors

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

DiseaseRelationSNOMED_IDDOID
Non-small cell lung cancer indication 254637007 DOID:3908
Metastatic non-small cell lung cancer indication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 225MG BASE TEPMETKO EMD SERONO INC N214096 Feb. 3, 2021 RX TABLET ORAL 8658643 July 4, 2028 TREATING A SOLID TUMOR, INCLUDING LUNG CANCER, WITH A MET ALTERATION(S), OR STABILIZING OR IMPROVING SYMPTOMS ASSOCIATED WITH HAVING A SOLID TUMOR, INCLUDING LUNG CANCER, WITH A MET ALTERATION(S), BY ADMINISTERING AN EFFECTIVE AMOUNT OF TEPOTINIB
EQ 225MG BASE TEPMETKO EMD SERONO INC N214096 Feb. 3, 2021 RX TABLET ORAL 9403799 July 4, 2028 TREATING A SOLID TUMOR, INCLUDING LUNG CANCER, WITH A MET ALTERATION(S), OR STABILIZING OR IMPROVING SYMPTOMS ASSOCIATED WITH HAVING A SOLID TUMOR, INCLUDING LUNG CANCER, WITH A MET ALTERATION(S), BY ADMINISTERING AN EFFECTIVE AMOUNT OF TEPOTINIB
EQ 225MG BASE TEPMETKO EMD SERONO INC N214096 Feb. 3, 2021 RX TABLET ORAL 8927540 July 21, 2028 TREATING A SOLID TUMOR, INCLUDING LUNG CANCER, HAVING A MET KINASE ALTERATION(S) BY ADMINISTERING AN EFFECTIVE AMOUNT OF TEPOTINIB

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 225MG BASE TEPMETKO EMD SERONO INC N214096 Feb. 3, 2021 RX TABLET ORAL Feb. 3, 2026 NEW CHEMICAL ENTITY
EQ 225MG BASE TEPMETKO EMD SERONO INC N214096 Feb. 3, 2021 RX TABLET ORAL Feb. 3, 2028 TREATMENT OF ADULT PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) HARBORING MESENCHYMAL-EPITHELIAL TRANSITION (MET) EXON 14 SKIPPING ALTERATIONS

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Hepatocyte growth factor receptor Kinase INHIBITOR IC50 8.77 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Ribosyldihydronicotinamide dehydrogenase [quinone] Enzyme Kd 6.06 CHEMBL
Interleukin-1 receptor-associated kinase 4 Kinase INHIBITOR IC50 6.21 SCIENTIFIC LITERATURE

External reference:

IDSource
D11073 KEGG_DRUG
1IJV77EI07 UNII
1946826-82-9 SECONDARY_CAS_RN
C4287799 UMLSCUI
3E8 PDB_CHEM_ID
CHEMBL3402762 ChEMBL_ID
25171648 PUBCHEM_CID
DB15133 DRUGBANK_ID
CHEMBL4594292 ChEMBL_ID
C582858 MESH_SUPPLEMENTAL_RECORD_UI
8293 IUPHAR_LIGAND_ID
018627 NDDF
018628 NDDF
1148537007 SNOMEDCT_US
1148545002 SNOMEDCT_US
1148549008 SNOMEDCT_US
4040036 VANDF
4040037 VANDF
2477103 RXNORM
343294 MMSL
39305 MMSL
d09709 MMSL
C000707607 MESH_SUPPLEMENTAL_RECORD_UI
9934 INN_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
TEPMETKO HUMAN PRESCRIPTION DRUG LABEL 1 44087-5000 TABLET 225 mg ORAL NDA 31 sections
TEPMETKO HUMAN PRESCRIPTION DRUG LABEL 1 44087-5000 TABLET 225 mg ORAL NDA 31 sections