Anticancer Drugs Oncology Pharmacology Physiotherapy Umbralisib

Umbralisib (Mechanism of Action)

In this article we will discuss 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.


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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