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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5424	1100598-32-0

Description:

Molecule	Description
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

Molecule

Description

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:

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

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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:

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

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

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Disease	Relation	SNOMED_ID	DOID
Non-small cell lung cancer	indication	254637007	DOID:3908
Metastatic non-small cell lung cancer	indication

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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 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

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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 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

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Hepatocyte growth factor receptor	Kinase	P08581	MET_HUMAN	INHIBITOR	IC50	8.77	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Ribosyldihydronicotinamide dehydrogenase [quinone]	Enzyme	P16083	NQO2_HUMAN		Kd	6.06	CHEMBL
Interleukin-1 receptor-associated kinase 4	Kinase	Q9NWZ3	IRAK4_HUMAN	INHIBITOR	IC50	6.21	SCIENTIFIC LITERATURE

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External reference:

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ID	Source
018627	NDDF
018628	NDDF
1148537007	SNOMEDCT_US
1148545002	SNOMEDCT_US
1148549008	SNOMEDCT_US
1946826-82-9	SECONDARY_CAS_RN
1IJV77EI07	UNII
2477103	RXNORM
25171648	PUBCHEM_CID
343294	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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

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