dezapelisib (Incyte)

Dezapelisib (INCB040093) is an orally bioavailable, potent, and selective small molecule inhibitor of the delta isoform of phosphoinositide 3-kinase (PI3Kδ), developed by Incyte. PI3Kδ is a lipid kinase primarily expressed in hematopoietic cells and is a critical mediator of B-cell receptor signaling, which is frequently dysregulated in various hematologic malignancies. By selectively targeting the delta isoform, dezapelisib aims to disrupt the signaling pathways that drive the proliferation, migration, and survival of malignant B cells while potentially reducing the off-target toxicities associated with pan-PI3K inhibition. The compound has been investigated in Phase 1 and Phase 2 clinical trials for the treatment of relapsed or refractory B-cell malignancies, including follicular lymphoma, chronic lymphocytic leukemia (CLL), and Hodgkin lymphoma. It has been studied both as a monotherapy and in combination with other targeted therapies, such as the JAK1 inhibitor itacitinib. Although it demonstrated clinical activity, Incyte has largely transitioned its PI3Kδ inhibitor development efforts toward its next-generation candidate, parsaclisib.

Other names

dezaelisibdezapelisibum