Phase I Study of Bromodomain Inhibitor OTX015 in Patients with Lymphoma or Multiple Myeloma
By Oncology Therapeutic Development (OTD)This white paper describes the methods and findings of a dose-escalation, open-label, pharmacokinetic, Phase I study of bromodomain inhibitor OTX015 in patients with lymphoma or multiple myeloma.
This first-in-class small molecule inhibitor specifically binds to bromodomain motifs BRD2, BRD3 and BRD4 of bromodomain and extraterminal (BET) proteins, inhibiting them from binding to acetylated histones, which occurs preferentially at super-enhancer regions that control oncogene expression.
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