TY - JOUR
T1 - PI3K inhibitors are finally coming of age
AU - Vanhaesebroeck, Bart
AU - Perry, Matthew W.D.
AU - Brown, Jennifer R.
AU - André, Fabrice
AU - Okkenhaug, Klaus
N1 - Publisher Copyright:
© 2021, Springer Nature Limited.
PY - 2021/10/1
Y1 - 2021/10/1
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=85107858936&partnerID=8YFLogxK
U2 - 10.1038/s41573-021-00209-1
DO - 10.1038/s41573-021-00209-1
M3 - Review article
C2 - 34127844
AN - SCOPUS:85107858936
SN - 1474-1776
VL - 20
SP - 741
EP - 769
JO - Nature Reviews Drug Discovery
JF - Nature Reviews Drug Discovery
IS - 10
ER -