Umbralisib, a novel PI3K delta and casein kinase-1 epsilon inhibitor, in relapsed or refractory chronic lymphocytic leukaemia and lymphoma: an open-label, phase 1, dose-escalation, first-in-human study

摘要

Background Umbralisib (TGR-1202) is a novel next-generation inhibitor of phosphatidylinositol 3-kinase (PI3K) isoform p110 delta (PI3K delta), which is structurally distinct from other PI3K delta inhibitors and shows improved isoform selectivity. Umbralisib also uniquely inhibits casein kinase-1 epsilon, a major regulator of protein translation. The aim of this first-in-human phase 1 study was to establish the safety and preliminary activity profile of umbralisib in patients with haematological malignancies.