O7.3BET-bromodomain (BRD) inhibitor OTX015: Final results of the dose-finding part of a phase I study in hematologic malignancies

Patrice Herait,Herve Dombret,Catherine Thieblemont,Thierry Facon,Anastasios Stathis,D Cunningham, Antonio Palumbo,Norbert Vey,M Michallet,Christian Recher,Keyvan Rezai,Claude Preudhomme

Annals of Oncology（2015）

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摘要

Background: OTX015 (Oncoethix) is a small molecule that specifically binds to BRDs 2, 3 and 4, thereby inhibiting binding to acetylated histones, resulting in downregulation of several oncogenes driven by super-enhancers. The therapeutic potential of BRD inhibitors has been demonstrated in several preclinical models including hematologic malignancies.

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关键词

inhibitor otx015,hematologic malignancies,brd,bet-bromodomain,dose-finding

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