Tivantinib (ARQ 197) is an orally administered, selective small molecule that inhibits mesenchymal-epithelial transition factor (MET) via a novel, ATP-independent binding mechanism. Preclinical studies demonstrated that tivantinib has a broad-spectrum 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 MET-high 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.
Tivantinib : a new promising mesenchymal–epithelial transition factor inhibitor in the treatment of hepatocellular carcinoma / L. Rimassa, N. Personeni, M. Simonelli, A. Santoro. - In: FUTURE ONCOLOGY. - ISSN 1479-6694. - 9:2(2013 Feb), pp. 153-165.
|Titolo:||Tivantinib : a new promising mesenchymal–epithelial transition factor inhibitor in the treatment of hepatocellular carcinoma|
PERSONENI, NICOLA (Secondo)
SIMONELLI, MATTEO (Penultimo)
|Parole Chiave:||hepatocellular carcinoma; immunohistochemistry; locally advanced/metastatic disease; MET expression; MET inhibitor; second line; tivantinib|
|Settore Scientifico Disciplinare:||Settore MED/06 - Oncologia Medica|
|Data di pubblicazione:||feb-2013|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.2217/fon.12.188|
|Appare nelle tipologie:||01 - Articolo su periodico|