Improving the armamentarium of PI3K inhibitors with isoform-selective agents: A new light in the darkness

Abstract

Excitement and drug-development efforts aimed at targetable genetic aberrations in the PI3K/AKT/ mTOR pathway have declined due to the limited clinical performance of these inhibitors as monotherapies. New, more isoform-selective treatments, such as taselisib, promise to both expand the therapeutic window and increase efficacy.