The summaries are free for public
use. The Chronic Liver Disease
Foundation will continue to add and
archive summaries of articles deemed
relevant to CLDF by the Board of
Trustees and its Advisors.
Abstract Details
Tivantinib: a new promising mesenchymal-epithelial transition factor inhibitor in the treatment of hepatocellular carcinoma
Rimassa L, Personeni N, Simonelli M, Santoro A. Future Oncol. 2013 Feb;9(2):153-65. doi: 10.2217/fon.12.188.
Source
Medical Oncology & Hematology Unit, Humanitas Cancer Center, Istituto Clinico Humanitas, IRCCS. Via Manzoni 56, 20089 Rozzano (Milano), Italy.
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.