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Temsirolimus

产品号 DB06287 公司名称 DrugBank
CAS号 162635-04-3 公司网站 http://www.ualberta.ca/
分子式 C56H87NO16 电 话 (780) 492-3111
分子量 1030.28708 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 4426

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产品别名

标题
Temsirolimus
IUPAC标准名
(1R,2R,4S)-4-[(2R)-2-[(1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-2,3,10,14,20-pentaoxo-11,36-dioxa-4-azatricyclo[30.3.1.0^{4,9}]hexatriaconta-16,24,26,28-tetraen-12-yl]propyl]-2-methoxycyclohexyl 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate
IUPAC传统名
torisel
商标名
Torisel
别名
CCI-779
temsirolimus

产品登记号

PubChem SID 99443243
CAS号 162635-04-3
PubChem CID 23724530

产品性质

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved; investigational
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.
Indication For the treatment of renal cell carcinoma (RCC). Also investigated for use/treatment in breast cancer, lymphoma (unspecified), rheumatoid arthritis, and multiple myeloma.
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.
Affected Organisms
Humans and other mammals
Biotransformation Primarily metabolized by cytochrome P450 3A4 in the human liver. Sirolimus, an equally potent metabolite, is the primary metabolite in humans following IV infusion. Other metabolic pathways observed in in vitro temsirolimus metabolism studies include hydroxylation, reduction and demethylation.
Absorption Infused intravenous over 30 - 60 minutes. Cmax is typically observed at the end of infusion
Half Life 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.
Protein Binding 87% bound to plasma proteins in vitro at a concentration of 100 ng/ml
Elimination 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.
Distribution 172 L in whole blood of cancer patients; both temsirolimus and sirolimus are extensive distributed partitioned into formed blood elements
Clearance 16.2 L/h (22%)
References
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]
External Links
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RxList
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参考文献

  • 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