FDA Approves Novartis's Afinitor

Afinitor (everolimus) is a cancer medication that interferes with the growth of cancer cells and slows their spread in the body.

Afinitor also lowers your body's immune system. The immune system helps your body fight infections. The immune system can also fight or "reject" a transplanted organ such as a liver or kidney. This is because the immune system treats the new organ as an invader.

Afinitor is used to treat advanced kidney cancer. Afinitor is usually given after sorafenib (Nexavar) or sunitinib (Sutent) have been tried without successful treatment of symptoms.

Afinitor is an inhibitor of mTOR (mammalian target of rapamycin), a serine-threonine kinase, downstream of the PI3K/AKT pathway. The mTOR pathway is dysregulated in several human cancers. Everolimus binds to an intracellular protein, FKBP-12, resulting in an inhibitory complex formation and inhibition of mTOR kinase activity. Inhibition of mTOR by everolimus has been shown to reduce cell proliferation, angiogenesis, and glucose uptake in in vitro and/or in vivo studies.

Afinitor is specifically indicated for the treatment of advanced renal cell carcinoma after failure of treatment with sunitinib or sorafenib.

Afinitor is supplied as a 5 mg or 10 mg tablet designed for oral administration. The recommended initial dose of the drug is 10 mg, to be taken once daily at the same time every day, either with or without food. Afinitor tablets should be swallowed whole with a glass of water; they should not be chewed or crushed.

Afinitor is a once-daily, oral inhibitor of mTOR (mammalian target of rapamycin) indicated for the treatment of patients with advanced renal cell carcinoma after failure of treatment with sunitinib or sorafenib. The active ingredient in Afinitor, everolimus, specifically blocks the activity of mTOR, an intracellular regulator important in tumor progression. Unlike other therapies that primarily inhibit tumor angiogenesis, Afinitor targets both tumor cells and blood vessel cells. Afinitor specifically blocks mTOR in 2 places, resulting in 3 distinct effects:

Reduced tumor cell growth and proliferation

Reduced cell metabolism

Reduced tumor angiogenesis