PI3K inhibitors are finally coming of age.


Type
Article
Change log
Abstract

Overactive phosphoinositide 3-kinase (PI3K) in cancer and immune dysregulation has spurred extensive efforts to develop therapeutic PI3K inhibitors. Although progress has been hampered by issues such as poor drug tolerance and drug resistance, several PI3K inhibitors have now received regulatory approval - the PI3Kα isoform-selective inhibitor alpelisib for the treatment of breast cancer and inhibitors mainly aimed at the leukocyte-enriched PI3Kδ in B cell malignancies. In addition to targeting cancer cell-intrinsic PI3K activity, emerging evidence highlights the potential of PI3K inhibitors in cancer immunotherapy. This Review summarizes key discoveries that aid the clinical translation of PI3Kα and PI3Kδ inhibitors, highlighting lessons learnt and future opportunities.

Description
Keywords
Animals, Humans, Immune System Diseases, Immunotherapy, Neoplasms, Phosphatidylinositol 3-Kinases, Phosphoinositide-3 Kinase Inhibitors
Journal Title
Nat Rev Drug Discov
Conference Name
Journal ISSN
1474-1776
1474-1784
Volume Title
20
Publisher
Springer Science and Business Media LLC
Rights
All rights reserved
Sponsorship
Medical Research Council (MR/M012328/1)
Wellcome Trust (200925/Z/16/Z)
Cancer Research UK (via University College London (UCL)) (548494)
Biotechnology and Biological Sciences Research Council (BB/M013278/1)