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 |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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:
| Source | Code | Description |
|---|---|---|
| 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|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 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 |
Orange Book exclusivity data (new drug applications)
| 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 |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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:
| 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 |