Chemistry:Tivantinib
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| Other names | ARQ197; ARQ-197 |
| Routes of administration | Oral |
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| Formula | C23H19N3O2 |
| Molar mass | 369.424 g·mol−1 |
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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 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
- Template:Intracellular chemotherapeutic agents
- Template:Growth factor receptor modulators
References
- ↑ "ArQule Announces Commencement of Phase 3 Clinical Trial with Tivantinib in Hepatocellular Carcinoma by Partner Kyowa Hakko Kirin in Japan". The Wall Street Journal. 4 February 2014. https://online.wsj.com/article/PR-CO-20140204-906777.html.
- ↑ "Tivantinib (ARQ197) displays cytotoxic activity that is independent of its ability to bind MET". Clinical Cancer Research 19 (9): 2381–92. May 2013. doi:10.1158/1078-0432.CCR-12-3459. PMID 23532890.
- ↑ "Neue Wirkstoffe – Tivantinib" (in German). Österreichische Apothekerzeitung (24/2014): 30. 24 November 2014.
- ↑ "ArQule, Daiichi Sankyo Say Cancer Candidate Tivantinib Fails Phase III Trial". Genetic Engineering & Biotechnology News. February 2017. http://www.genengnews.com/gen-news-highlights/arqule-daiichi-sankyo-say-cancer-candidate-tivantinib-fails-phase-iii-trial/81253902.
- ↑ "Tivantinib (ARQ 197)". ArQule. https://www.arqule.com/pipeline/tivantinib-arq-197/.
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