Tepotinib hydrochlorideProduct ingredient for Tepotinib

Name
Tepotinib hydrochloride
Drug Entry
Tepotinib

Tepotinib is a MET tyrosine kinase inhibitor intended to treat a variety of MET-overexpressing solid tumors.6 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,5 gastric cancers,2 non-small cell lung cancer, and hepatocellular carcinoma.6 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.7,9 It is the first oral MET-targeted tyrosine kinase inhibitor to allow for once-daily dosing,9 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.10

Accession Number
DBSALT003143
Structure
Synonyms
Tepotinib hydrochloride / Tepotinib hydrochloride monohydrate
UNII
VY5YX2TQ1F
CAS Number
1946826-82-9
Weight
Average: 547.06
Monoisotopic: 546.2146166
Chemical Formula
C29H31ClN6O3
InChI Key
KZVOMLRKFJUTLK-UHFFFAOYSA-N
InChI
InChI=1S/C29H28N6O2.ClH.H2O/c1-34-12-10-21(11-13-34)20-37-26-17-31-29(32-18-26)25-7-3-5-23(15-25)19-35-28(36)9-8-27(33-35)24-6-2-4-22(14-24)16-30;;/h2-9,14-15,17-18,21H,10-13,19-20H2,1H3;1H;1H2
IUPAC Name
3-{1-[(3-{5-[(1-methylpiperidin-4-yl)methoxy]pyrimidin-2-yl}phenyl)methyl]-6-oxo-1,6-dihydropyridazin-3-yl}benzonitrile hydrate hydrochloride
SMILES
O.Cl.CN1CCC(COC2=CN=C(N=C2)C2=CC(CN3N=C(C=CC3=O)C3=CC(=CC=C3)C#N)=CC=C2)CC1
ChemSpider
68007288
Wikipedia
Tepotinib
Predicted Properties
PropertyValueSource
logP4Chemaxon
pKa (Strongest Basic)9.13Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count7Chemaxon
Hydrogen Donor Count0Chemaxon
Polar Surface Area94.71 Å2Chemaxon
Rotatable Bond Count7Chemaxon
Refractivity154.74 m3·mol-1Chemaxon
Polarizability54.7 Å3Chemaxon
Number of Rings5Chemaxon
Bioavailability1Chemaxon
Rule of FiveNoChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleYesChemaxon