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. [10.2217/fon.12.188]

Tivantinib : a new promising mesenchymal–epithelial transition factor inhibitor in the treatment of hepatocellular carcinoma

N. Personeni
Secondo
;
M. Simonelli
Penultimo
;
2013

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.
hepatocellular carcinoma; immunohistochemistry; locally advanced/metastatic disease; MET expression; MET inhibitor; second line; tivantinib
Settore MED/06 - Oncologia Medica
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/426274
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