[HTML][HTML] Drugging PI3K in cancer: refining targets and therapeutic strategies
Highlights•PI3K is an important target for innovative anticancer drug development and
precision medicine.•Over 30 small molecule PI3K inhibitors are currently in clinical trial
testing.•These drugs include dual PI3K/mTOR, pan-Class I PI3K and isoform-selective PI3K
inhibitors.•The PI3Kδ inhibitor idelalisib has received FDA approval for the treatment of B-
cell malignancies.•Drug resistance, patient selection and development of targeted
combinations remain challenges.The phosphatidylinositol-3 kinase (PI3K) pathway is one of …
precision medicine.•Over 30 small molecule PI3K inhibitors are currently in clinical trial
testing.•These drugs include dual PI3K/mTOR, pan-Class I PI3K and isoform-selective PI3K
inhibitors.•The PI3Kδ inhibitor idelalisib has received FDA approval for the treatment of B-
cell malignancies.•Drug resistance, patient selection and development of targeted
combinations remain challenges.The phosphatidylinositol-3 kinase (PI3K) pathway is one of …