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umbralisib + ibrutinib
- Development stage
- Unknown
- Lead developer
- TG Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Umbralisib + ibrutinib is a combination therapy evaluated in Phase II clinical trials for the treatment of relapsed or refractory diffuse large B-cell lymphoma (DLBCL). This regimen combines umbralisib (TGR-1202), a dual inhibitor of phosphoinositide 3-kinase (PI3K) delta and casein kinase 1 epsilon (CK1ε), with ibrutinib, a covalent inhibitor of Bruton's tyrosine kinase (BTK). By simultaneously targeting multiple components of the B-cell receptor (BCR) signaling pathway, the combination aims to achieve synergistic anti-tumor activity and overcome resistance mechanisms common in aggressive B-cell lymphomas. The development of this combination was supported by TG Therapeutics and Janssen Pharmaceuticals through investigator-initiated trials at the University of Nebraska Medical Center.
- Brand names
- UkoniqImbruvica
- Other names
- umbralisib and ibrutinibTGR-1202 and ibrutinibTGR1202 and ibrutinibTGR 1202 and ibrutinibPI3K-delta inhibitor TGR-1202 + ibrutinib
02
Targets
ITK (Interleukin 2-inducible T-cell kinase)BTK (Bruton tyrosine kinase)CSNK1E (Casein kinase I isoform epsilon)PIK3CD (Phosphatidylinositol 3-kinase delta)
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