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
- External Links
- Predicted Properties
Property Value Source logP 4 Chemaxon pKa (Strongest Basic) 9.13 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 7 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 94.71 Å2 Chemaxon Rotatable Bond Count 7 Chemaxon Refractivity 154.74 m3·mol-1 Chemaxon Polarizability 54.7 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon