Basic Information
ID DDInter2050
Drug Type small molecule
Molecular Formula C29H28N6O2
Molecular Weight 492.583
CAS Number 1100598-32-0
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. In February 2022, tepotinib was approved for use in Europe.[L42200]
ATC Classification L01EX21
IUPAC Name 3-{1-[(3-{5-[(1-methylpiperidin-4-yl)methoxy]pyrimidin-2-yl}phenyl)methyl]-6-oxo-1,6-dihydropyridazin-3-yl}benzonitrile
InChI AHYMHWXQRWRBKT-UHFFFAOYSA-N
Canonical SMILES CN1CCC(COC2=CN=C(N=C2)C2=CC(CN3N=C(C=CC3=O)C3=CC(=CC=C3)C#N)=CC=C2)CC1
Useful Links DrugBank ChemSpider BindingDB Wikipedia ChEMBL ZINC
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