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]

Tivantinib structure.svg
Tivantinib ball-and-stick model.png
Clinical data
Other namesARQ197; ARQ-197
Routes of
ATC code
  • none
Legal status
Legal status
  • Investigational
CAS Number
PubChem CID
CompTox Dashboard (EPA)
ECHA InfoCard100.231.891 Edit this at Wikidata
Chemical and physical data
Molar mass369.42 g/mol g·mol−1
3D model (JSmol)

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]


  1. ^ "ArQule Announces Commencement of Phase 3 Clinical Trial with Tivantinib in Hepatocellular Carcinoma by Partner Kyowa Hakko Kirin in Japan - WSJ.com". online.wsj.com. Retrieved 2014-02-09.
  2. ^ Basilico, C; Pennacchietti, S; Vigna, E; Chiriaco, C; Arena, S; Bardelli, A; Valdembri, D; Serini, G; Michieli, P (2013). "Tivantinib (ARQ197) displays cytotoxic activity that is independent of its ability to bind MET". Clinical Cancer Research. 19 (9): 2381–92. doi:10.1158/1078-0432.CCR-12-3459. PMID 23532890.
  3. ^ H. Spreitzer (24 November 2014). "Neue Wirkstoffe – Tivantinib". Österreichische Apothekerzeitung (in German) (24/2014): 30.
  4. ^ ArQule, Daiichi Sankyo Say Cancer Candidate Tivantinib Fails Phase III Trial. Feb 2017
  5. ^ https://www.arqule.com/pipeline/tivantinib-arq-197/

See alsoEdit