Abstract
Umbralisib (UKONIQ™) is an oral, first-in-class dual phosphatidylinositol 3-kinase delta (PI3Kδ) and casein kinase 1 epsilon (CK1ε) inhibitor being developed by TG Therapeutics for the treatment of various haematological malignancies. In February 2021, umbralisib received its first approval in the USA for the treatment of adults with relapsed or refractory marginal zone lymphoma (MZL) who have received ≥ 1 prior anti-CD20-based regimen, and relapsed or refractory follicular lymphoma (FL) who have received ≥ 3 prior lines of systemic therapy. Clinical studies in various haematological malignancies, including chronic lymphocytic leukaemia and non-Hodgkin's lymphoma, are underway in multiple countries. This article summarizes the milestones in the development of umbralisib leading to this first approval.
MeSH terms
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Antineoplastic Combined Chemotherapy Protocols / therapeutic use
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Area Under Curve
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Casein Kinase 1 epsilon / antagonists & inhibitors
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Drug Approval
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Drug Interactions
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Hematologic Neoplasms / drug therapy*
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Heterocyclic Compounds, 4 or More Rings / adverse effects
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Heterocyclic Compounds, 4 or More Rings / pharmacokinetics
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Heterocyclic Compounds, 4 or More Rings / pharmacology*
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Heterocyclic Compounds, 4 or More Rings / therapeutic use*
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Humans
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Leukemia, Lymphocytic, Chronic, B-Cell / drug therapy
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Lymphoma, B-Cell, Marginal Zone / drug therapy
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Lymphoma, Follicular / drug therapy
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Lymphoma, Non-Hodgkin / drug therapy
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Metabolic Clearance Rate
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Phosphoinositide-3 Kinase Inhibitors / therapeutic use
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Randomized Controlled Trials as Topic
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United States
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United States Food and Drug Administration
Substances
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Heterocyclic Compounds, 4 or More Rings
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Phosphoinositide-3 Kinase Inhibitors
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umbralisib
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Casein Kinase 1 epsilon