Tivantinib

Tivantinib

Clinical data
Synonyms	ARQ197; ARQ-197
Routes of administration	Oral
ATC code	none
Legal status
Legal status	Investigational
Identifiers
IUPAC name (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	905854-02-6
PubChem CID	11494412
ChemSpider	9669218
KEGG	D10173
ChEMBL	CHEMBL2103882
ECHA InfoCard	100.231.891
Chemical and physical data
Formula	C23H19N3O2
Molar mass	369.42 g/mol
3D model (JSmol)	Interactive image
SMILES C1CC2=C3C(=CC=C2)C(=CN3C1)[C@H]4[C@@H](C(=O)NC4=O)C5=CNC6=CC=CC=C65
InChI 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

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.

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]

References

See also

• Template:Intracellular chemotherapeutic agents
• Template:Growth factor receptor modulators