| Pharmaceutical Information |
| Drug Name |
Tepotinib |
| Drug ID |
BADD_D02599 |
| Description |
Tepotinib is a MET tyrosine kinase inhibitor intended to treat a variety of MET-overexpressing solid tumors.[A228058] It was originally developed in partnership between EMD Serono and the University of Texas M.D. Anderson Cancer Center in 2009 and has since been investigated in the treatment of neuroblastoma,[A228053] gastric cancers,[A228033] non-small cell lung cancer, and hepatocellular carcinoma.[A228058] MET is a desirable target in the treatment of certain solid tumors as it appears to play a critical role, both directly and indirectly, in the growth and proliferation of tumors in which it is overexpressed and/or mutated.
Tepotinib was first approved in Japan in March 2020 for the treatment of non-small cell lung cancers (NSCLC) with _MET_ alterations, and was subsequently granted accelerated approval by the US FDA in February 2021, under the brand name Tepmetko, for the treatment of adult patients with metastatic NSCLC and _MET_ exon 14 skipping alterations.[L31443,L31473] It is the first oral MET-targeted tyrosine kinase inhibitor to allow for once-daily dosing,[L31473] an advantage that may aid in easing the pill burden often associated with chemotherapeutic regimens. |
| Indications and Usage |
Tepotinib is indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) who have mesenchymal-epithelial transition (_MET_) exon 14 skipping alterations.[L31443] |
| Marketing Status |
approved; investigational |
| ATC Code |
L01EX21 |
| DrugBank ID |
DB15133
|
| KEGG ID |
D11717
|
| MeSH ID |
C000707607
|
| PubChem ID |
25171648
|
| TTD Drug ID |
D0R8QG
|
| NDC Product Code |
Not Available |
| UNII |
1IJV77EI07
|
| Synonyms |
tepotinib | 3-(1-(3-(5-((1-Methyl-4-piperidinyl)methoxy)-2-pyrimidinyl)benzyl)-6-oxo-1,6-dihydro-3-pyridazinyl)benzonitrile | benzonitrile, 3-(1,6-dihydro-1-((3-(5-((1-methyl-4-piperidinyl)methoxy)-2-pyrimidinyl)phenyl)methyl)-6-oxo-3-pyridazinyl)- | tepmetko |
|
| Chemical Information |
| Molecular Formula |
C29H28N6O2 |
| CAS Registry Number |
1100598-32-0 |
| SMILES |
CN1CCC(CC1)COC2=CN=C(N=C2)C3=CC=CC(=C3)CN4C(=O)C=CC(=N4)C5=CC=CC(=C5)C#N |
| Chemical Structure |
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| ADRs Induced by Drug |
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