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umbralisib + brentuximab vedotin
- Development stage
- Phase 1
- Lead developer
- TG Therapeutics
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Umbralisib (TGR-1202) is an orally active small molecule inhibitor that selectively targets phosphoinositide 3-kinase delta (PI3Kδ) and casein kinase 1 epsilon (CK1ε). It is developed primarily for the treatment of hematologic malignancies such as chronic lymphocytic leukemia (CLL), non-Hodgkin’s lymphoma, and other related cancers. Umbralisib works by inhibiting PI3Kδ signaling pathways involved in tumor cell growth and survival[1][4]. Brentuximab vedotin is an antibody-drug conjugate consisting of a CD30-directed monoclonal antibody linked to the microtubule-disrupting agent monomethyl auristatin E. It is used mainly for treating CD30-positive lymphomas such as Hodgkin lymphoma and systemic anaplastic large cell lymphoma. The combination of umbralisib with brentuximab vedotin represents a multi-modal approach targeting both intracellular signaling pathways critical for cancer cell survival and delivering cytotoxic agents directly to malignant cells.
- Other names
- umbralisib + AdcetrisTGR-1202 + BV
02
Targets
CD30 (CD30 antigen)CSNK1E (Casein kinase I isoform epsilon)PIK3CD (Phosphatidylinositol 3-kinase delta)
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