Encyclopedia of Cancer

Living Edition
| Editors: Manfred Schwab

Temsirolimus

  • Janet E. Dancey
Living reference work entry
DOI: https://doi.org/10.1007/978-3-642-27841-9_5724-2

Synonyms

Definition

Temsirolimus is a small molecule inhibitor of mammalian target of rapamycin (mTOR) kinase. Aberrant intracellular signaling through mTOR is associated with the cancer cell proliferation. Inhibition of this pathway by temsirolimus results in antiproliferative effects that may result in improved survival in patients with cancer.

Characteristics

Temsirolimus is a soluble 42-[2,2-bis (hydroxymethyl)]-propionic ester of the macrocyclic lactone rapamycin (also known as sirolimus). Temsirolimus, sirolimus, and other members of this class of agents inhibit the proliferation of normal and malignant cells by inhibiting the activity of mTOR, an intracellular serine-threonine kinase within the phosphoinositide 3-kinase (PI3K)/Akt signal transduction pathway. Temsirolimus, like sirolimus, reacts with the ubiquitous intracellular FK506-binding protein 12 (FKBP12) to inhibit mTOR function.

Mechanism of Action

Activation of the phosphoinositide 3-kinase...

Keywords

Renal Cell Carcinoma Mantle Cell Lymphoma Tuberous Sclerosis Macrocyclic Lactone Cowden Syndrome 
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. Cully M, You H, Levine AJ et al (2006) Beyond PTEN mutations: the PI3K pathway as an integrator of multiple inputs during tumorigenesis. Nat Rev Cancer 6(3):184–192CrossRefPubMedGoogle Scholar
  2. Faivre S, Kroemer G, Raymond E (2006) Current development of mTOR inhibitors as anticancer agents. Nat Rev Drug Discov 5(8):671–688CrossRefPubMedGoogle Scholar
  3. Hudes G, Carducci M, Tomczak P, et al: Temsirolimus, interferon alfa, or both for advanced renal-cell carcinoma. N Engl J Med 356:2271-81, 2007.CrossRefPubMedGoogle Scholar
  4. Hess G, Herbrecht R, Romaguera J, et al: Phase III study to evaluate temsirolimus compared with investigator's choice therapy for the treatment of relapsed or refractory mantle cell lymphoma. J Clin Oncol 27:3822-9, 2009.CrossRefPubMedGoogle Scholar
  5. Samuels Y, Ericson K (2006) Oncogenic PI3K and its role in cancer. Curr Opin Oncol 18(1):77–82CrossRefPubMedGoogle Scholar
  6. Thomas GV (2006) mTOR and cancer: reason for dancing at the crossroads? Curr Opin Genet Dev 16(1):78–84CrossRefPubMedGoogle Scholar

See Also

  1. (2012) Endothelial cells. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer Berlin Heidelberg, p. 1251. doi: 10.1007/978-3-642-16483-5_1896Google Scholar
  2. (2012) Pericyte. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer Berlin Heidelberg, pp 2814-2815. doi: 10.1007/978-3-642-16483-5_4448Google Scholar
  3. (2012) Small cell lung carcinoma. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer Berlin Heidelberg, p. 3448. doi: 10.1007/978-3-642-16483-5_5368Google Scholar
  4. (2012) Stomatitis. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer Berlin Heidelberg, p. 3535. doi: 0.1007/978-3-642-16483-5_5522Google Scholar
  5. (2012) Tuberous sclerosis syndrome. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer Berlin Heidelberg, p. 3792. doi: 10.1007/978-3-642-16483-5_6010Google Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 2014

Authors and Affiliations

  1. 1.Division of Cancer Treatment and DiagnosisNational Cancer InstituteRockvilleUSA