title: Idelalisib for the treatment of indolent non-Hodgkin's lymphoma.
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.
authors.affiliation: Department of Internal Medicine, University of Colorado School of Medicine, Aurora, Colorado, USA.
authors.forename: J P
authors.initials: JP
authors.lastname: Lopez
authors.affiliation: Division of Medical Oncology, Department of Medicine, Developmental Therapeutics Program, University of Colorado School of Medicine, Aurora, Colorado, USA. antonio.jimeno@ucdenver.edu.
authors.forename: A
authors.initials: A
authors.lastname: Jimeno
mesh_terms: D000818:Animals; D058543:Class Ia Phosphatidylinositol 3-Kinase / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D017321:Clinical Trials, Phase I as Topic; D017322:Clinical Trials, Phase II as Topic; D017326:Clinical Trials, Phase III as Topic; D006801:Humans; D008228:Lymphoma, Non-Hodgkin / Q000188:drug therapy*; D011687:Purines / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D052999:Quinazolinones / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*
chemical_list: D011687:Purines; D052999:Quinazolinones; D058543:Class Ia Phosphatidylinositol 3-Kinase; C552946:idelalisib
keywords: Idelalisib; Indolent non-Hodgkin's lymphoma; Non-Hodgkin's lymphoma; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PI3Kδ) inhibitor; Tyrosine kinase inhibitor; iNHL