Idelalisib for the treatment of non-Hodgkin lymphoma

Expert Opin Pharmacother. 2016;17(2):265-74. doi: 10.1517/14656566.2016.1135130. Epub 2016 Jan 28.

Abstract

Introduction: B-cell Non-Hodgkin lymphomas (B-NHLs) include a number of disease subtypes, each defined by the tempo of disease progression and the identity of the cancerous cell. Idelalisib is a potent, selective inhibitor of the delta isoform of phosphatidylinositol-3-kinase (PI3K), a lipid kinase whose over-activity in B-NHL drives disease progression. Idelalisib has demonstrated activity in indolent B-NHL (iB-NHL) and is approved for use as monotherapy in patients with follicular lymphoma and small lymphocytic lymphoma and in combination with rituximab in patients with chronic lymphocytic leukemia.

Areas covered: Herein we review the development and pharmacology of idelalisib, its safety and efficacy in clinical studies of iB-NHL, and its potential for inclusion in future applications in iB-NHL and in combination with other therapies.

Expert opinion: Idelalisib adds to the growing arsenal of iB-NHL pharmacotherapeutics and to the progression of the field toward precision agents with good efficacy and reduced toxicities. Nevertheless, idelalisib carries important risks that require careful patient counseling and monitoring. The appropriate sequencing of idelalisib with other proven treatment options in addition to its potential for combination with established or novel drugs will be borne out in ongoing and planned investigations.

Keywords: B-cell; Idelalisib; indolent; lymphoma.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Clinical Trials, Phase I as Topic
  • Clinical Trials, Phase II as Topic
  • Clinical Trials, Phase III as Topic
  • Humans
  • Lymphoma, B-Cell / drug therapy*
  • Phosphoinositide-3 Kinase Inhibitors*
  • Purines / administration & dosage
  • Purines / pharmacology
  • Purines / therapeutic use*
  • Quinazolinones / administration & dosage
  • Quinazolinones / pharmacology
  • Quinazolinones / therapeutic use*
  • Randomized Controlled Trials as Topic
  • Rituximab / administration & dosage

Substances

  • Antineoplastic Agents
  • Phosphoinositide-3 Kinase Inhibitors
  • Purines
  • Quinazolinones
  • Rituximab
  • idelalisib