Phosphoinositide 3-kinase inhibitor

This signal pathway regulates cellular functions such as growth and survival.

PI3K inhibitors block the PI3K/AKT/mTOR pathway and thus slow down cancer growth.

[5][6] After PI3K inhibitors had been under investigation as anti-cancer drugs for several years,[7][8][9][10] the first one to be approved for treatment in clinical practice was idelalisib in 2014.

[13] Class 1 PI3Ks have a catalytic subunit known as p110, with four types (isoforms) – p110 alpha (PIK3CA), p110 beta (PIK3CB), p110 gamma (PIK3CG) and p110 delta (PIK3CD).

Inhibiting different p110 isoforms can have different effects,[15] e.g. PTEN-negative tumors may be more sensitive to PIK3CB inhibitors.

Overview of phosphoinositide 3-kinase (PI3K) inhibitors and their interaction with the PI3K/AKT/mTOR pathway . There are pan-class I PI3K inhibitors such as copanlisib , isoform-specific PI3K inhibitors such as idelalisib , and dual PI3K/ mTOR inhibitors such as dactolisib . Note that fimepinostat and rigosertib inhibit the PI3K/AKT/mTOR pathway, but not PI3K itself. [ 1 ]