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.
|Other names||ARQ197; ARQ-197|
|CompTox Dashboard (EPA)|
|Chemical and physical data|
|Molar mass||369.42 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.
- "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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