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Estramustine


ACCESSION NB: DB01196 (APRD00625)


TYPE: small molecule


GROUP: approved


DESCRIPTION:
A nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties. [PubChem]

VOLUME OF DISTRIBUTION: Not Available

CATEGORIES:
Antineoplastic Agents Antineoplastic Agents, Hormonal Radiation-Protective Agents Antineoplastic Agents, Alkylating

ABSORPTION: Not Available

INDICATION:
For the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostate

PHARMACODYNAMICS:
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.

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 cell death. Also, due to the drugs estrogen component, it can bind more selectively to active estrogen receptors.

PROTEIN BINDING:
Not Available

TOXICITY:
Not Available

AFECTED ORGANISMS:
Humans and other mammals