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. OI Personeni, Nicola/0000-0002-7995-272X
Tivantinib: a new promising mesenchymal-epithelial transition factor inhibitor in the treatment of hepatocellular carcinoma / Rimassa, L; Personeni, N; Simonelli, M; Santoro, A. - In: FUTURE ONCOLOGY. - ISSN 1479-6694. - 9:2(2013), pp. 153-165. [10.2217/FON.12.188]
Tivantinib: a new promising mesenchymal-epithelial transition factor inhibitor in the treatment of hepatocellular carcinoma
Personeni N;Santoro A
2013-01-01
Abstract
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. OI Personeni, Nicola/0000-0002-7995-272XI documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
