Umbralisib is a kinase inhibitor used to treat rare forms of refractory lymphoma. Marginal zone lymphoma is a rare, slowly progressing type of non-Hodgkin lymphoma initially treated with rituximab (an anti-CD20 drug), either alone or in combination with chemotherapy.
- Mechanism
- Curator reviewed · 5 references
The PI3K pathway is a deregulated in malignancies, leading to the overexpression of p110 isoforms (p110α, p110β, p110δ, p110γ) that induces malignant transformation in cells. Umbralisib inhibits several protein kinases, including PI3Kδ and casein kinase CK1ε. PI3Kδ is expressed in both healthy cells and malignant B-cells. CK1ε is believed to be involved in the pathogenesis of malignant cells, including lymphomas. This results in reduced progression of relapsed or refractory lymphoma. In biochemical assays, umbralisib inhibited a mutated form of ABL1. In vitro, umbralisib inhibits malignant cell proliferation, CXCL12-mediated cell adhesion, and CCL19-mediated cell migration.
- Primary indication
- Umbralisib does not have any approved therapeutic indications.Curator reviewed
- Formula / weight
- C31H24F3N5O3 · 571.56 g/mol (avg)
- First approval
- United States, 2021
- Code names
- RP-5264 · TGR-1202
Resolves to
IUVCFHHAEHNCFT-INIZCTEOSA-NSMILESCC(C)OC1=C(F)C=C(C=C1)C1=NN([C@@H](C)C2=C(C3=CC=CC(F)=C3)C(=O)C3=CC(F)=CC=C3O2)C2=C1C(N)=NC=N2What you can answer from here — as of September 23, 2026
Which drugs share a target with Umbralisib, and which of those have an active Phase 3 trial?
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