Tivantinib: A new promising mesenchymal-epithelial transition factor inhibitor in the treatment of hepatocellular carcinoma

Research output: Contribution to journalArticlepeer-review

Abstract

Tivantinib (ARQ 197) is an orally administered, selective small molecule that inhibits mesenchymal-epithelial transition factor (MET) via a novel, ATPindependent binding mechanism. Preclinical studies demonstrated that tivantinib has a broadspectrum anti-tumor activity, especially in cells expressing high levels of MET. A randomized Phase II study in second-line hepatocellular carcinoma showed statistically significant improvement in time to progression with tivantinib compared to a placebo. Noteworthy, a significant pronounced benefit in time to progression and overall survival was observed in METhigh patients. In addition, MET expression was defined as a negative prognostic factor. The most frequent adverse events were hematologic events. A Phase III study in the MET-high hepatocellular carcinoma is actively recruiting patients. Phase II and III studies in non-small-cell lung cancer and colorectal cancer are ongoing.

Original languageEnglish
Pages (from-to)153-165
Number of pages13
JournalFuture Oncology
Volume9
Issue number2
DOIs
Publication statusPublished - Feb 2013

Keywords

  • hepatocellular carcinoma
  • immunohistochemistry
  • locally advanced/metastatic disease
  • MET expression
  • MET inhibitor
  • second line
  • tivantinib

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

Fingerprint Dive into the research topics of 'Tivantinib: A new promising mesenchymal-epithelial transition factor inhibitor in the treatment of hepatocellular carcinoma'. Together they form a unique fingerprint.

Cite this