Tivantinib

Chemical compound From Wikipedia, the free encyclopedia

Tivantinib (ARQ197; by Arqule, Inc.) is an experimental small molecule anti-cancer drug. It is a bisindolylmaleimide that binds to the dephosphorylated MET kinase in vitro. (MET is a growth factor receptor.) Tivantinib is being tested clinically as a highly selective MET inhibitor.[1] However, the mechanism of action of tivantinib is still unclear.[citation needed]

Other namesARQ197; ARQ-197
Routes of
administrationOral
ATC code
  • none
Legal status
  • Investigational
Quick facts Clinical data, Other names ...
Tivantinib
Clinical data
Other namesARQ197; ARQ-197
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • Investigational
Identifiers
  • (3R,4R)-3-(5,6-Dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-2,5-pyrrolidinedione
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.231.891 Edit this at Wikidata
Chemical and physical data
FormulaC23H19N3O2
Molar mass369.424 g·mol−1
3D model (JSmol)
  • C1CC2=C3C(=CC=C2)C(=CN3C1)[C@H]4[C@@H](C(=O)NC4=O)C5=CNC6=CC=CC=C65
  • InChI=1S/C23H19N3O2/c27-22-19(16-11-24-18-9-2-1-7-14(16)18)20(23(28)25-22)17-12-26-10-4-6-13-5-3-8-15(17)21(13)26/h1-3,5,7-9,11-12,19-20,24H,4,6,10H2, (H,25,27,28)/t19-,20-/m0/s1
  • Key:UCEQXRCJXIVODC-PMACEKPBSA-N
Close

Tivantinib displays cytotoxic activity via molecular mechanisms that are independent from its ability to bind MET, notably tubulin binding, which likely underlies tivantinib cytotoxicity.[2]

Possible applications include non-small-cell lung carcinoma, hepatocellular carcinoma, and oesophageal cancer.[3]

In 2017, it was announced that a phase III clinical trial for advanced hepatocellular carcinoma had failed to meet the primary endpoint.[4][5]

See also

References

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