Umbralisib (Mechanism of Action)

In this article, we will discuss Umbralisib (Mechanism of Action). So, let’s get started.

Mechanism of Action

Umbralisib inhibits multiple kinases. In biochemical and cell-based assays, umbralisib inhibited PI3Kδ and casein kinase CK1ε. PI3Kδ is expressed in normal and malignant B-cells; CK1ε has been implicated in the pathogenesis of cancer cells, including lymphoid malignancies. Umbralisib also inhibited a mutated form of ABL1 in biochemical assays. Umbralisib inhibited cell proliferation, CXCL12-mediated cell adhesion, and CCL19-mediated cell migration in lymphoma cell lines in studies conducted in vitro.

Pharmacodynamics

Exposure-Response Relationships

An exposure-response relationship between umbralisib and overall response rate was observed in patients with FL. The time course of pharmacodynamic response is unknown.

A relationship between higher umbralisib steady state exposures and higher incidence of adverse reactions, including diarrhea (any grade) and elevated AST/ALT (any grade and Grade ≥ 3), was observed.

Cardiac Electrophysiology

The effect of umbralisib on QT interval has not been fully characterized.

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