Umbralisib
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Umbralisib is a kinase inhibitor used to treat rare forms of refractory lymphoma.
Umbralisib is a kinase inhibitor used to treat rare forms of refractory lymphoma.
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.
Umbralisib does not have any approved therapeutic indications.
每项发明一条，涵盖美国、欧洲、PCT 与中国的同族专利。
