mTOR Inhibitors Mechanism of Action
Everolimus, Temsirolimus, Ridaforilimus Inhibits protein synthesis and cell growth
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  1. Mutations of PIK3CA activate PI3 kinase without growth factor stimulation or ligand-independent HER2 activation.
  2. PTEN acts as a negative regulator of PI3K pathway activity. Loss of PTEN protein or function results in unchecked activity of this pathway and cell growth in the absence of stimulation from upstream growth factors, such as EGFR, heregulin, IGF-1, and HGF.
  3. Mutations in KRAS lead to activation of MAPK and increased protein synthesis through mTOR as well as other enzymes (e.g., p90 ribosomal S6 kinase), thereby limiting the effectiveness of mTOR inhibitors.

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Green squares, sensitivity markers. Red squares, resistance markers