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QuickView for Temsirolimus (compound)


PubChem
Name: temsirolimus
PubChem Compound ID: 5469176
Molecular formula: C56H87NO16
Molecular weight: 1030.29 g/mol
Synonyms:
NSC683864
DrugBank
Identification
Name: temsirolimus
Name (isomeric): DB06287
Drug Type: small molecule
Synonyms:
CCI-779
Brand: Torisel
Category: Antineoplastic Agents, Protein Kinase Inhibitors
CAS number: 162635-04-3
Pharmacology
Indication: For the treatment of renal cell carcinoma (RCC). Also investigated for use/treatment in breast cancer, lymphoma (unspecified), rheumatoid arthritis, and multiple myeloma.
Mechanism of Action:
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 phosphoryla...
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Absorption: Infused intravenous over 30 - 60 minutes. Cmax is typically observed at the end of infusion
Protein binding: 87% bound to plasma proteins in vitro at a concentration of 100 ng/ml
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.
Route of 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.
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.
Clearance: 16.2 L/h (22%)
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
Interactions
Drug interaction:
TipranavirTipranavir may affect the efficacy/toxicity of Temsirolimus.
NefazodoneNefazodone may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
RitonavirRitonavir may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
RifampinRifampin may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
PhenobarbitalPhenobarbital may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
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