Drug intelligence / Profile preview

umbralisib

Development stage
Phase 3
Lead developer
TG Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Umbralisib is an oral small molecule kinase inhibitor developed for the treatment of certain B-cell malignancies. It selectively inhibits phosphoinositide 3-kinase delta (PI3K-delta), a key enzyme involved in cell survival and proliferation, particularly in hematopoietic cells and malignant lymphoid disorders. Umbralisib also inhibits casein kinase 1 epsilon (CK1-epsilon), which regulates oncoprotein translation and is associated with lymphoma cell growth and survival. The drug was indicated for adults with relapsed or refractory marginal zone lymphoma (MZL) who had received at least one prior anti-CD20-based regimen, as well as for adults with relapsed or refractory follicular lymphoma (FL) after at least three prior lines of systemic therapy. Umbralisib was withdrawn from the U.S. market in June 2022 due to safety concerns[1][2][4][5][6][7][8].

Brand names
Ukoniq
02

Targets

CK1 (Casein kinase 1)PIK3CD (Phosphatidylinositol 3-kinase delta)

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