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Estramustine is an oral prostate cancer drug that combines an oestrogen with an alkylating agent, approved in the United States in 1981 for metastatic disease and later combined with taxanes, though its clotting risk has pushed it out of routine use.
Estramustine phosphate was designed to deliver a nitrogen mustard to oestrogen-receptor-bearing prostate cancer cells, but it turned out to work mostly by disrupting microtubules. The FDA approved it in 1981 for palliative treatment of metastatic or progressive prostate cancer. In the 1990s and 2000s it was combined with docetaxel and other taxanes with higher response rates than the taxane alone, but venous thromboembolism and the equal survival of docetaxel alone in the TAX 327 era left it out of standard regimens. It remains licensed in the United States and Europe.
Carries a nornitrogen mustard on an oestradiol backbone; in the body it acts mainly as an antimicrotubule agent that binds microtubule-associated proteins, with oestrogenic effects that also lower testosterone. Connects to Tubulin (microtubules).
1.Estramustine slips into a pocket on Tubulin (microtubules).
Background: ADC sequencing, Antigen escape (antigen loss, lineage switch), BCG-unresponsive, Castration-resistant prostate cancer (CRPC), Circulating tumour DNA (ctDNA). Also on OnCo: Resistance: how tumours escape each drug class · Lines of therapy.
| Region | Year | Indication |
|---|---|---|
| US | 1981 | Palliative treatment of metastatic or progressive prostate cancer |
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Query for this drug: (TITLE:"Estramustine" OR ABSTRACT:"Estramustine" OR TITLE:"Emcyt" OR ABSTRACT:"Emcyt" OR TITLE:"Estramustine phosphate" OR ABSTRACT:"Estramustine phosphate") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Estramustine, not a curated reading list.
Shares Tubulin (microtubules), Cytotoxic chemotherapy and the tag chembl-universe.
Shares Cytotoxic chemotherapy and the tag chembl-universe.
Shares Cytotoxic chemotherapy and the tag chembl-universe.
Shares Cytotoxic chemotherapy and the tag chembl-universe.
Shares Cytotoxic chemotherapy and the tag chembl-universe.
Shares Prostate cancer and the tag chembl-universe.
Shares Cytotoxic chemotherapy and the tag chembl-universe.
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