Substance
ID:1071
Names and Identifiers
Synonyms
Estramustinum [INN-Latin]Estramustina [INN-Spanish]Estramustin Sodium PhosphateEstramustine Sodium PhosphateEstramustine
Brand Name
EstracytEmcyt
IUPAC name
14-hydroxy-15-methyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-2(7),3,5-trien-5-yl N,N-bis(2-chloroethyl)carbamate
IUPAC Traditional name
estramustine
Registration numbers
CAS Number
Properties
Physical Property
Hydrophobicity(logP)
5.7
Molecule Details
Drug Groups
approved
Description
A nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties. [PubChem]
Indication
For the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostate
Pharmacology
Estramustine is an antineoplastic agent indicated in the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostate. Estramustine is a combination of estradiol with nitrogen mustard. In vivo, the nitrogen-mustard moiety becomes active and participates in alkylation of DNA or other cellular components.. This causes DNA damage in rapidly dividing cancerous cells leading to cell death and ideally, tumor shrinkage.
Affected Organisms
Humans and other mammals
Half Life
20 hours
Elimination
The metabolic urinary patterns of the estradiol moiety of estramustine phosphate and estradiol itself are very similar, although the metabolites derived from estramustine phosphate are excreted at a slower rate.
External Links
Molecular Spectra
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References
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