This is an international site for AFINITOR® (everolimus) and is intended for Health Care Professionals outside the U.S. The information on the site is not country-specific, and may contain information that is outside the approved indications in the country in which you are located. Please contact your local Novartis representative for the latest information specific to your country

I am a healthcare professional outside of the US I am a US Resident I am a patient outside of the US

AFINITOR® (everolimus) Logo | AFINITOR.com
AFINITOR is a once-daily oral inhibitor of mTOR (mammalian target of rapamycin) for patients with advanced renal cell carcinoma (RCC) whose disease has progressed on or after treatment with VEGF-targeted therapy
Afinitor now approved in the EU!
Afinitor International Website  |  For Healthcare Professionals Outside the U.S.  |  US Residents
Mechanism of Action
mTOR Inhibitors

• Cell Proliferation

• Angiogenesis

• Cell Metabolism


Stay informed on the latest information, including news related to AFINITOR and other updates.

Register for Afinitor Updates
Afinitor Approved Countries

Angiogenesis

mTOR activation promotes angiogenesis

mTOR plays a key role in angiogenesis — the formation of new blood vessels that provide oxygen and nutrients to growing tumour cells.1-3 Specifically, mTOR controls the production of proteins that play a role in mediating the expression of a wide variety of genes whose products play a role in angiogenesis as well as in cell metabolism, proliferation, motility, adhesion and survival.1-3

In many cancers, angiogenesis is deregulated. Angiogenesis deregulation has been shown to correlate with increased mortality in a number of tumor types, including cervical cancer, breast cancer, non-small-cell lung cancer, ovarian cancer, head and neck cancer and gastrointestinal stromal tumors.3 In addition, loss of the von Hippel-Lindau (VHL) protein is a primary cause of many cases of advanced renal cell carcinoma.4,5

Recently, activated mTOR has been shown in vitro and in animal models to up-regulate production of a key inducer of lymphangiogenesis (VEGF-C).6 In cancer, lymphangiogenesis has been shown to play a causal role in lymph node metastasis. Inhibition of mTOR has been shown to significantly suppress lymph node metastasis in animal models.6

Next: Cell Metabolism

References
1. Pouysségur J, Dayan F, Mazure N. Hypoxia signalling in cancer and approaches to enforce tumour regression. Nature. 2006;441:437-443.
2. Faivre S, Kroemer G, Raymond E. Current development of mTOR inhibitors as anticancer agents. Nat Rev Drug Disc. 2006;5:671-688.
3. Semenza GL. Targeting HIF-1 for cancer therapy. Nat Rev Cancer. 2003;3:721-731.
4. Ohh M, Kaelin WG. VHL and kidney cancer. Methods Mol Biol. 2003;222:167-183.
5. Hammel PR, Vilgrain V, Terris B, et al. Pancreatic involvement in von Hippel-Lindau disease. Gastroenterology. 2000;119:1087-1095.
6. Kobayashi S, Kishimoto T, Kamata S, Otsuka M, Miyazaki M, Ishikura H. Rapamycin, a specific inhibitor of the mammalian target of rapamycin, suppresses lymphangiogenesis and lymphatic metastasis. Cancer Sci. 2007;98:726-733.