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QuickView for Estramustine (compound)


PubChem
Name: Estramustine
PubChem Compound ID: 18140
Description: A nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties.
Molecular formula: C23H31Cl2NO3
Molecular weight: 440.403 g/mol
Synonyms:
17.Beta.-Estradiol {3-[bis(2-chloroethyl)carbamate]}; Estradiol 3-(bis(2-chloroethyl)carbamate); Estra-1,3,5(10)-triene-3,17-diol (17.beta.)-, 3-[bis(2-chloroethyl)carbamate]; Estramustina [INN-Spanish]; Estra-1,3,5(10)-triene-3,17-diol (17beta)-, 3-(bis(2-chloroethyl)carbamate) (9CI); Estramustinum [INN-Latin]; Emcyt; Estra-1,3,5(10)-triene-3,17-diol, 3-(bis(2-chloroethyl)carbamate), (17beta)-; Estracyt; EINECS 221-076-3.
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DrugBank
Identification
Name: Estramustine
Name (isomeric): DB01196
Drug Type: small molecule
Description: A nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties.
Synonyms:
Estramustina [INN-Spanish]; Estramustinum [INN-Latin]; Estramustine Sodium Phosphate; Estramustin Sodium Phosphate
Brand: Estracyt, Emcyt
Category: Radiation-Protective Agents, Antineoplastic Agents, Hormonal, Antineoplastic Agents, Antineoplastic Agents, Alkylating
CAS number: 2998-57-4
Pharmacology
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...
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Mechanism of Action:
Estramustine is a derivative of estradiol with a nitrogen mustard moiety. This gives it alkylating properties. In vivo, the nitrogen mustard component is active and can alklyate DNA and other cellular components (such as tubulin components) of rapidly dividing cells. This causes DNA strandbreaks or misscoding events. This leads to apoptosis and cel...
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Route of 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.
Half Life: 20 hours
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Take on an empty stomach.
Do not take with milk or milk products.
Drug interaction:
TrastuzumabTrastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
ClodronateClodronate may increase the levels of estramustine.
Calcium AcetateCalcium salts such as calcium acetate may decrease the absorption of estramustine. Interactions can be minimized by administering estramustine on an empty stomach, at least 1 hour before or 2 hours after the dose of an oral calcium supplement. Do not coadminister estramustine with food or milk. Monitor for decreased therapeutic effects of estramustine if administered with oral calcium supplements, food or milk.

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