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ublituximab + umbralisib + ibrutinib
- Development stage
- Unknown
- Lead developer
- TG Therapeutics
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous, Oral
01
Overview
The combination of ublituximab, umbralisib (TGR-1202), and ibrutinib is a chemotherapy-free triplet regimen developed for the treatment of B-cell malignancies, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL). Ublituximab is a glycoengineered monoclonal antibody targeting CD20 on B-cells, designed to enhance antibody-dependent cell-mediated cytotoxicity. Umbralisib (TGR-1202) is an oral, next-generation phosphoinositide 3‑kinase delta (PI3Kδ) inhibitor with improved safety compared to earlier PI3K inhibitors. Ibrutinib is a first-in-class small molecule inhibitor of Bruton’s tyrosine kinase (BTK), disrupting B-cell receptor signaling. The combination leverages complementary mechanisms to target malignant B-cells through distinct pathways. Clinical studies have shown this regimen to be well-tolerated with promising efficacy in heavily pretreated and high-risk patients[1][6][7][8].
- Brand names
- Imbruvica
- Other names
- ublituximab + TGR-1202 + ibrutinibublituximab + umbralisib + ibrutinib
02
Targets
BTK (Bruton tyrosine kinase)CD20 (B-lymphocyte antigen CD20)CK1 (Casein kinase 1)PIK3CD (Phosphatidylinositol 3-kinase delta)
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