About: Temsirolimus     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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rdf:type
http://linked.open...gbank/description
  • Temsirolimus is an intravenous drug for the treatment of renal cell carcinoma (RCC), developed by Wyeth Pharmaceuticals and approved by the FDA in late May 2007, and was also approved by the European Medicines Agency (EMEA) on November 2007. It is a derivative of sirolimus and is sold as Torisel. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Wyeth Pharmaceuticals Inc. Torisel® (temsirolimus) injection prescribing information. Philadelphia, PA: 2010 Sep. # Boni J, Leister C, Burns J, Cincotta M, Hug B, Moore L: Pharmacokinetic profile of temsirolimus with concomitant administration of cytochrome p450-inducing medications. J Clin Pharmacol. 2007 Nov;47(11):1430-9. Epub 2007 Oct 3. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17913896 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • Temsirolimus exhibits a bi-exponential decline in whole blood concentrations and the mean half-lives of temsirolimus and sirolimus were 17.3 hr and 54.6 hr, respectively. (en)
http://linked.open...ugbank/indication
  • For the treatment of renal cell carcinoma (RCC). Also investigated for use/treatment in breast cancer, lymphoma (unspecified), rheumatoid arthritis, and multiple myeloma. (en)
sameAs
Title
  • Temsirolimus (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Temsirolimus is an inhibitor of mTOR (mammalian target of rapamycin). Temsirolimus binds to an intracellular protein (FKBP-12), and the protein-drug complex inhibits the activity of mTOR that controls cell division. Inhibition of mTOR activity resulted in a G1 growth arrest in treated tumor cells. When mTOR was inhibited, its ability to phosphorylate p70S6k and S6 ribosomal protein, which are downstream of mTOR in the PI3 kinase/AKT pathway was blocked. In in vitro studies using renal cell carcinoma cell lines, temsirolimus inhibited the activity of mTOR and resulted in reduced levels of the hypoxia-inducible factors HIF-1 and HIF-2 alpha, and the vascular endothelial growth factor. (en)
http://linked.open...drugbank/packager
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • Excreted predominantly in feces (76%), 4.6% of drug and metabolites recovered in urine. 17% of drug was not recovered by either route following a 14-day sample collection. (en)
http://linked.open.../drugbank/synonym
  • Torisel (en)
  • CCI 779 (en)
  • 42-[3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoate]rapamycin (en)
http://linked.open...drugbank/toxicity
  • Temsirolimus has been administered to patients with cancer in phase 1 and 2 trials with repeated intravenous doses as high as 220 mg/m2. The risk of several serious adverse events, including thrombosis, bowel perforation, interstitial lung disease (ILD), seizure, and psychosis, is increased with doses of temsirolimus greater than 25 mg. (en)
http://linked.open...umeOfDistribution
  • 172 L in whole blood of cancer patients; both temsirolimus and sirolimus are extensive distributed partitioned into formed blood elements (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...nk/proteinBinding
  • 87% bound to plasma proteins <i>in vitro</i> at a concentration of 100 ng/ml (en)
http://linked.open...ynthesisReference
  • Kwang-Chung Lee, Ting-Huei Lee, Yen-Shih Tung, Chia-Chen Kao, Tzu-Ai Lee, "Process for preparation of temsirolimus." U.S. Patent US20100249415, issued September 30, 2010. (en)
http://linked.open...y/mesh/hasConcept
foaf:page
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...noisotopic-Weight
http://linked.open...y/drugbank/SMILES
http://linked.open.../Water-Solubility
http://linked.open...ogy/drugbank/logP
http://linked.open...ogy/drugbank/logS
http://linked.open...l/drug/hasATCCode
http://linked.open...nd-Acceptor-Count
http://linked.open...-Bond-Donor-Count
http://linked.open...drugbank/InChIKey
http://linked.open...urface-Area--PSA-
http://linked.open...nk/Polarizability
http://linked.open...bank/Refractivity
http://linked.open...atable-Bond-Count
http://linked.open...ugbank/absorption
  • Infused intravenous over 30 - 60 minutes. C<sub>max</sub> is typically observed at the end of infusion (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 162635-04-3 (en)
http://linked.open...rugbank/clearance
  • 16.2 L/h (22%) (en)
http://linked.open...gbank/containedIn
http://linked.open...k/Bioavailability
http://linked.open...bank/Ghose-Filter
http://linked.open...nk/MDDR-Like-Rule
http://linked.open...k/Number-of-Rings
http://linked.open...siological-Charge
http://linked.open...bank/Rule-of-Five
http://linked.open...tional-IUPAC-Name
http://linked.open...strongest-acidic-
http://linked.open...-strongest-basic-
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