AFINITOR^® Mechanism of Action

How AFINITOR (everolimus) tablets work

The intracellular kinase mTOR plays key roles upstream and downstream of many different pathways important in renal cell carcinoma.

Unlike other therapies that primarily inhibit tumor angiogenesis, AFINITOR is proven to directly inhibit mTOR. This results in:

• Reduced tumor cell growth and proliferation
• Decreased tumor angiogenesis
• Inhibited cell metabolism

• AFINITOR is a signal transduction inhibitor targeting mTOR (mammalian target of rapamycin)
• mTOR is a serine-threonine kinase playing a central role in the regulation of cell growth, proliferation and survival
• The regulation of mTOR complex 1 (mTORC1) signaling is intricate, being modulated by mitogens, growth factors, energy and nutrient availability
• mTORC1 is an essential regulator of global protein synthesis downstream on the PI3K/AKT pathway, which is dysregulated in the many human cancers
• Consistent with the known activity of mTORC1, its inhibition by AFINITOR has been shown to reduce cell proliferation, glycolysis and angiogenesis in solid tumors in vivo, both through direct antitumor cell activity and inhibition of the tumor stromal compartment

Next: mTOR Inhibitors