|Other names||ARQ197; ARQ-197|
|Chemical and physical data|
|Molar mass||369.42 g/mol g·mol−1|
|3D model (JSmol)|
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. 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.
- "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.
- 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.
- H. Spreitzer (24 November 2014). "Neue Wirkstoffe – Tivantinib". Österreichische Apothekerzeitung (in German) (24/2014): 30.
- ArQule, Daiichi Sankyo Say Cancer Candidate Tivantinib Fails Phase III Trial. Feb 2017
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