The phosphatidylinositol-3-kinases (PI3Ks) play a critical role in cellular metabolism and proliferation, as well as in the development of cancer. Several mutations in the genes coding for PI3Ks have been identified in a large proportion of tumours at different rates, depending on the tumour type. Therapies targeting PI3Ks have been developed in the last years and initially used in hematological malignancies. In medical oncology, a number of trials have tried to prove the efficacy of these compounds, but most of them have been confronted with very important toxicities and only a modest benefit in progression-free survival. Recent trials using more selective treatments have shown good efficacy with an acceptable toxicity profile. The aim of this article is to review the current knowledge about PI3K inhibitors, their potential use in medical oncology and their toxicities.

(BELG J MED ONCOL 2021;15(3):96-103)