ABSTRACT
Idelalisib is a novel, highly selective, small-molecule, tyrosine kinase inhibitor with potent activity against phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PI3Kδ). Given the highly selective inhibition of this compound, studies have shown that idelalisib is able to achieve significantly increased apoptotic activity in B-cell acute lymphoblastic leukemia (B-ALL) and chronic lymphocytic leukemia (CLL) cell lines, without significant increase in apoptosis among normal T and natural killer cells. Recent studies have suggested potential clinical benefit with idelalisib as either a single agent or in combination with established chemotherapeutic compounds including bendamustine and rituximab in relapsed/refractory CLL. This review will focus on the preclinical pharmacology, pharmacokinetics and clinical utility of idelalisib in the treatment of various indolent forms of non-Hodgkin's lymphoma.
