Estramustine
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.
Overview
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).
- AmivantamabApproved
- CamizestrantApproved
- Comprehensive genomic profilingStandard of care
- Liquid biopsy (ctDNA)Standard of care
- LorlatinibApproved
- MRD / molecular residual disease testingEstablished
- ADC payload neutralisersPhase 1
- BGB-16673Phase 3
- Bispecific ADCPhase 3
- BRUIN CLL-321Positive
- CaDAnCe-304Recruiting
- CIRCULATE-Japan (GALAXY / VEGA / ALTAIR)Active
- A clone report from blood at every treatment cycle
- A fast route to the matched drug when it is licensed for another cancer
- A multi-cancer platform trial of adaptive (dose-holiday) therapy
- A national rapid research autopsy network for end-stage cancer
- A standard evolvability score for every tumour
- A standing platform trial that assigns treatment by how the tumour escaped
Background: ADC sequencing, Antigen escape (antigen loss, lineage switch), BCG-unresponsive, Castration-resistant prostate cancer (CRPC), Circulating tumour DNA (ctDNA). Also on OnCo: Resistance atlas · Lines of therapy.
Approvals
| Region | Year | Indication |
|---|---|---|
| US | 1981 | Palliative treatment of metastatic or progressive prostate cancer |
Trials
topTrials recruiting now
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Latest papers
topQuery 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.
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