title: Tivantinib: a new promising mesenchymal-epithelial transition factor inhibitor in the treatment of hepatocellular carcinoma.
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.
authors: Medical Oncology & Hematology Unit, Humanitas Cancer Center, Istituto Clinico Humanitas, IRCCS. Via Manzoni 56, 20089 Rozzano, Milano, Italy. lorenza.rimassa@cancercenter.humanitas.it
authors: Lorenza
authors: L
authors: Rimassa
authors: Nicola
authors: N
authors: Personeni
authors: Matteo
authors: M
authors: Simonelli
authors: Armando
authors: A
authors: Santoro
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy*; D017321:Clinical Trials, Phase I as Topic; D017322:Clinical Trials, Phase II as Topic; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008113:Liver Neoplasms / Q000188:drug therapy*; D011760:Pyrrolidinones / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D011804:Quinolines / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D016896:Treatment Outcome
chemical_list: C551661:ARQ 197; D000970:Antineoplastic Agents; D011760:Pyrrolidinones; D011804:Quinolines