PI3K targeting in breast cancer: the end of the beginning?
Mené sur 168 patientes atteintes d'un cancer du sein ER+ HER2- résistant à un traitement par inhibiteur d'aromatase, cet essai randomisé international de phase II évalue l'efficacité, du point de vue de la survie sans progression, et la toxicité de l'ajout du pictilisib, un inhibiteur de PI3K, au fulvestrant
Activation of the phosphatidylinositol 3-kinase (PI3K)-protein kinase B (AKT)-mTOR pathway is thought to play a major role in hormone resistance. PIK3CA mutation is the most common somatic mutation observed in oestrogen receptor-positive breast cancer, with an incidence of PIK3CA mutation of up to 40% in the largest studies. Preclinical models using well established luminal breast cell lines, such as MCF7 and T47D, have shown that hormone resistance is largely linked to PI3K pathway activation and could be reversed by PI3K, AKT, or mTOR inhibitors.
The Lancet Oncology , commentaire, 2015