Estramustine is an antineoplastic agent used for the management of metastatic and/or progressive prostate cancer in palliative setting. A nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties.
- Mechanism
- Curator reviewed
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.
- Primary indication
- For the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostateCurator reviewed · 1 structured indication
- Formula / weight
- C23H31Cl2NO3 · 440.403 g/mol (avg)
- First approval
- Canada, 2003 · United States, 1992
- Code names
- RO 22-2296/000
Resolves to
FRPJXPJMRWBBIH-RBRWEJTLSA-NSMILES[H][C@@]12CC[C@H](O)[C@@]1(C)CC[C@]1([H])C3=CC=C(OC(=O)N(CCCl)CCCl)C=C3CC[C@@]21[H]What you can answer from here — as of September 30, 2026
Which drugs share a target with Estramustine, and which of those have an active Phase 3 trial?
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