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TG-1701 + ublituximab + umbralisib

Development stage: Unknown
Lead developer: TG Therapeutics
Modality: Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration: Oral, Intravenous

Overview

A combination investigational regimen targeting B-cell malignancies, particularly chronic lymphocytic leukemia (CLL), mantle cell lymphoma (MCL), and Waldenström macroglobulinemia (WM). It consists of: - **TG-1701**: A next-generation, irreversible, covalently binding Bruton tyrosine kinase (BTK) inhibitor, designed for selectivity and improved safety compared to other BTK inhibitors. - **Ublituximab**: A monoclonal antibody that targets CD20 on B-cells, leading to cell depletion via antibody-dependent mechanisms. - **Umbralisib**: A small-molecule inhibitor of phosphoinositide 3-kinase delta (PI3Kδ). This triple regimen is tested to exploit dual and triple pathway blockade in the B-cell receptor signaling axis, aiming for deeper and more durable responses in B-cell lymphoproliferative disorders, especially in patients naïve to BTK inhibitors. TG-1701 is administered orally, and ublituximab and umbralisib are administered intravenously[1][3][5].

Brand names: Briumvi (ublituximab)
Other names: U2 (sometimes refers to the combination of ublituximab + umbralisib)

Targets

CSNK1E (Casein kinase I isoform epsilon)CD20 (B-lymphocyte antigen CD20)BTK (Bruton tyrosine kinase)PIK3CD (Phosphatidylinositol 3-kinase delta)

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