Biologic Effect
Afinitor inhibits mTOR—an important factor driving aRCC progression with multiple biologic effects1-7
See the multiple biologic effects of Afinitor in this video.
Mammalian target of rapamycin (mTOR) is an important factor driving the proliferation, growth, and metabolism of advanced renal cell carcinoma (aRCC) tumor cells. This makes mTOR an important target in the treatment of aRCC.1-7
Afinitor has a dual targeted mechanism that inhibits mTOR in both tumor and blood vessel cells.8-10 This yields a reduction in:
- Cell growth and cell proliferation
- Cell metabolism
- Angiogenesis*
*Inhibition of mTOR by Afinitor has been shown to reduce cell proliferation, angiogenesis, and glucose uptake in in vitro and/or in vivo studies.
Get more detail about how Afinitor inhibits mTOR in aRCC on TargetmTOR.com.
Important Safety Information
Oral Ulceration: Oral ulcerations (ie, mouth ulcers, stomatitis, and oral mucositis) are the most frequently occurring adverse event and occurred in 44% of advanced RCC patients and were mostly Grade 1 or 2. In such cases, topical treatments are recommended, but alcohol- or peroxide-containing mouthwashes should be avoided. Antifungal agents should not be used unless fungal infection has been diagnosed.
Renal Failure: Cases of renal failure (including acute renal failure), some with a fatal outcome, have been observed in patients treated with AFINITOR.
Laboratory Tests and Monitoring: Elevations of serum creatinine, proteinuria, glucose, lipids, and triglycerides, as well as reductions of hemoglobin, lymphocytes, neutrophils, and platelets have been reported. Renal function, blood glucose, lipids, and hematologic parameters should be evaluated prior to treatment and periodically thereafter. When possible, optimal glucose and lipid control should be achieved before starting a patient on AFINITOR.
Please see additional Important Safety Information at the bottom of this page.
Please see full Prescribing Information.
References
1. Rini BI, Atkins MB. Resistance to targeted therapy in renal-cell carcinoma. Lancet Oncol. 2009;10:992-1000. 2. Yuan R, Kay A, Berg W, Lebwohl D. J Hematol Oncol. 2009;2:45. 3. Zacchia M, Vilasi A, Capasso A, et al. J Nephrol. 2011;24:155-164. 4. Hudes GR. Cancer. 2009;115:2313-2320. 5. Kapoor A, Figlin RA. Cancer. 2009;115:3618-3630. 6. Pantuck AJ, Seligson DB, Klatte T, et al. Cancer. 2007;109:2257-2267. 7. Schmidinger M, Bellmunt J. Cancer Treat Rev. 2010;36:416-424. 8. Wullschleger S, Loewith R, Hall MN. Cell. 2006;124:471-484. 9. Dancey JE. Expert Opin Investig Drugs. 2005;14:313-328. 10. Hartford CM, Ratain MJ. Clin Pharmacol Ther. 2007;82:381-388.
ADVANCED RENAL CELL CARCINOMA (aRCC)
AFINITOR is indicated for the treatment of patients with advanced renal cell carcinoma after failure of treatment with sunitinib or sorafenib.
Important Safety Information
There have been reports of non-infectious pneumonitis, infections and kidney failure (including acute renal failure) in patients taking AFINITOR, some with fatal outcomes. Oral ulceration is the most frequently occurring adverse event and occurred in 44% of AFINITOR-treated patients. Most were Grade 1 or 2. Elevations of serum creatinine, proteinuria, glucose, lipids, and triglycerides and reductions of hemoglobin, lymphocytes, neutrophils, and platelets have also been reported.
Please see additional
