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This gene drives several tumorigenic processes and is overexpressed in many cancers. Although <jats:italic>c\u2010MYC<\/jats:italic> is a strategic target to restrain cancer processes, no drugs acting as c\u2010MYC inhibitors are available. The novel thienotriazolodiazepine small\u2010molecule bromodomain inhibitor OTX015\/MK\u20108628 has shown potent antiproliferative activity accompanied by <jats:italic>c\u2010MYC<\/jats:italic> downregulation in several tumor types. This study was designed to evaluate the growth inhibitory effect of OTX015 on patient\u2010derived MPM473, MPM487 and MPM60 mesothelioma cell lines and its antitumor activity in three patient\u2010derived xenograft models, MPM473, MPM487 and MPM484, comparing it with cisplatin, gemcitabine and pemetrexed, three agents which are currently used to treat MPM in the clinic. OTX015 caused a significant delay in cell growth both <jats:italic>in vitro<\/jats:italic> and <jats:italic>in vivo<\/jats:italic>. It was the most effective drug in MPM473 xenografts and showed a similar level of activity as the most efficient treatment in the other two MPM models (gemcitabine in MPM487 and cisplatin in MPM484). <jats:italic>In vitro<\/jats:italic> studies showed that OTX015 downregulated c\u2010MYC protein levels in both MPM473 and MPM487 cell lines. Our findings represent the first evidence of promising therapeutic activity of OTX015 in mesothelioma.<\/jats:p>","DOI":"10.1002\/ijc.30412","type":"journal-article","created":{"date-parts":[[2016,9,5]],"date-time":"2016-09-05T03:37:06Z","timestamp":1473046626000},"page":"197-207","source":"Crossref","is-referenced-by-count":38,"title":["Promising <i>in vivo<\/i> efficacy of the BET bromodomain inhibitor OTX015\/MK\u20108628 in malignant pleural mesothelioma xenografts"],"prefix":"10.1002","volume":"140","author":[{"given":"Ramiro","family":"V\u00e1zquez","sequence":"first","affiliation":[{"name":"Laboratory of Cancer Pharmacology IRCCS\u2010Istituto di Ricerche Farmacologiche Mario Negri Milan Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Simonetta Andrea","family":"Licandro","sequence":"additional","affiliation":[{"name":"Laboratory of Cancer Pharmacology IRCCS\u2010Istituto di Ricerche Farmacologiche Mario Negri Milan Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lucile","family":"Astorgues\u2010Xerri","sequence":"additional","affiliation":[{"name":"Oncology Therapeutic Development Clichy France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Emanuele","family":"Lettera","sequence":"additional","affiliation":[{"name":"Laboratory of Cancer Pharmacology IRCCS\u2010Istituto di Ricerche Farmacologiche Mario Negri Milan Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Nicol\u00f2","family":"Panini","sequence":"additional","affiliation":[{"name":"Laboratory of Cancer Pharmacology IRCCS\u2010Istituto di Ricerche Farmacologiche Mario Negri Milan Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Michela","family":"Romano","sequence":"additional","affiliation":[{"name":"Laboratory of Cancer Pharmacology IRCCS\u2010Istituto di Ricerche Farmacologiche Mario Negri Milan Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Eugenio","family":"Erba","sequence":"additional","affiliation":[{"name":"Laboratory of Cancer Pharmacology IRCCS\u2010Istituto di Ricerche Farmacologiche Mario Negri Milan Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Paolo","family":"Ubezio","sequence":"additional","affiliation":[{"name":"Laboratory of Cancer Pharmacology IRCCS\u2010Istituto di Ricerche Farmacologiche Mario Negri Milan Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ezia","family":"Bello","sequence":"additional","affiliation":[{"name":"Laboratory of Cancer Pharmacology IRCCS\u2010Istituto di Ricerche Farmacologiche Mario Negri Milan Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Roberta","family":"Libener","sequence":"additional","affiliation":[{"name":"Cytogenetic and Molecular Pathology Laboratory, Pathology Unit, Oncology SS Antonio e Biagio e Cesare Arrigo General Hospital Alessandria Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sara","family":"Orecchia","sequence":"additional","affiliation":[{"name":"Cytogenetic and Molecular Pathology Laboratory, Pathology Unit, Oncology SS Antonio e Biagio e Cesare Arrigo General Hospital Alessandria Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Federica","family":"Grosso","sequence":"additional","affiliation":[{"name":"Cytogenetic and Molecular Pathology Laboratory, Pathology Unit, Oncology SS Antonio e Biagio e Cesare Arrigo General Hospital Alessandria Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mar\u00eda Eugenia","family":"Riveiro","sequence":"additional","affiliation":[{"name":"Oncology Therapeutic Development Clichy France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Esteban","family":"Cvitkovic","sequence":"additional","affiliation":[{"name":"Oncology Therapeutic Development Clichy France"},{"name":"Oncoethix SA (now Oncoethix GmbH, a wholly owned subsidiary of Merck Sharp &amp; 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