Tivantinib

Nowadays, Tivantinib is a topic on everyone's lips. Whether due to its relevance in the social sphere, its impact on the economy or its influence on popular culture, Tivantinib has captured the attention of a large number of people around the world. This phenomenon is not surprising, as Tivantinib possesses a number of characteristics that make it worthy of study and interest by academics, experts, and enthusiasts alike. In this article, we will explore in depth some of the most prominent facets of Tivantinib, analyzing its importance today and its potential impact in the future. Through a rigorous and exhaustive analysis, we will seek to shed light on this highly relevant topic and offer a comprehensive vision that allows readers to better understand its scope and significance.

Tivantinib
Clinical data
Other namesARQ197; ARQ-197
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • Investigational
Identifiers
  • (3R,4R)-3-(5,6-Dihydro-4H-pyrroloquinolin-1-yl)-4-(1H-indol-3-yl)-2,5-pyrrolidinedione
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.231.891 Edit this at Wikidata
Chemical and physical data
FormulaC23H19N3O2
Molar mass369.424 g·mol−1
3D model (JSmol)
  • C1CC2=C3C(=CC=C2)C(=CN3C1)4(C(=O)NC4=O)C5=CNC6=CC=CC=C65
  • 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.[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

References

  1. ^ "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. Archived from the original on 22 February 2014.
  2. ^ Basilico C, Pennacchietti S, Vigna E, Chiriaco C, Arena S, Bardelli A, et al. (May 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. ^ Spreitzer H (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". Genetic Engineering & Biotechnology News. February 2017.
  5. ^ "Tivantinib (ARQ 197)". ArQule. Archived from the original on 14 March 2017.
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