Encyclopedia of Cancer

Living Edition
| Editors: Manfred Schwab

Everolimus

  • Daniel C. Cho
Living reference work entry
DOI: https://doi.org/10.1007/978-3-642-27841-9_2040-2

Synonyms

Definition

Everolimus is an orally administered inhibitor of mammalian target of rapamycin (mTOR). This agent has significant activity in renal cell carcinoma (RCC) and is approved by the Food and Drug Administration (FDA) for treatment of patients with RCC who have failed treatment with sorafenib or sunitinib.

Characteristics

Everolimus (RAD001, Afinitor®) is an ester of the immunosuppressant rapamycin which binds with high affinity to FK506-binding protein 12 (FKBP12), forming a complex that inhibits the kinase activity of mTOR. mTOR is a highly conserved serine/threonine kinase which is activated downstream of Akt (protein kinase B; Akt signal transduction pathway) and regulates cell growth and metabolism in response to environmental factors (Fig. 1). Once activated, mTOR executes its biologic functions as a critical component of two distinct complexes, TORC1 and TORC2, which have differential...

Keywords

Renal Cell Carcinoma Cell Renal Cell Carcinoma Clear Cell Renal Cell Carcinoma Advanced Renal Cell Carcinoma Everolimus Group 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
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References

  1. Amato RJ, Jac J, Giessinger S, Saxena S, Willis JP (2009) A phase 2 study with a daily regimen of the oral mTOR inhibitor RAD001 (Everolimus) in patients with metastatic clear cell RCC. Cancer 115:2438–2445CrossRefPubMedGoogle Scholar
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  3. Meric-Bernstam F, Gonzalez-Angulo AM (2009) Targeting the mTOR signaling network for cancer therapy. J Clin Oncol 27:2278–2287CrossRefPubMedPubMedCentralGoogle Scholar
  4. Motzer RJ, Escudier B, Oudard S, Hutson TE, Porta C, Bracarda S, Grunwald V, Thompson JA, Figlin RA, Hollaender N, Urbanowitz G, Berg WJ, Kay A, Lebwohl D, Ravaud A (2008) Efficacy of everolimus in advanced renal cell carcinoma: a double-blind, randomized, placebo-controlled phase III trial. Lancet 372:449–456CrossRefPubMedGoogle Scholar
  5. Toschi A, Lee E, Gadir N, Ohh M, Foster DA (2008) Differential dependence of hypoxia-inducible factors 1 alpha and 2 alpha on TORC1 and TORC2. J Biol Chem 283:34495–34499CrossRefPubMedPubMedCentralGoogle Scholar

See Also

  1. (2012) Adjuvant. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer Berlin Heidelberg, p 75. doi:10.1007/978-3-642-16483-5_107Google Scholar
  2. (2012) Cell cycle. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 737. doi:10.1007/978-3-642-16483-5_994Google Scholar
  3. (2012) Ornithine decarboxylase. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer Berlin Heidelberg, p 2656. doi:10.1007/978-3-642-16483-5_4259Google Scholar
  4. (2012) Renal cancer. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer Berlin Heidelberg, pp 3225–3226. doi: 10.1007/978-3-642-16483-5_6575Google Scholar
  5. (2012) Sunitinib. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer Berlin Heidelberg, p 3562. doi:10.1007/978-3-642-16483-5_5575Google Scholar
  6. (2012) Translation. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer Berlin Heidelberg, p 3770. doi:10.1007/978-3-642-16483-5_5936Google Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 2014

Authors and Affiliations

  1. 1.Beth Israel Deaconess Medical CenterBostonUSA