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doxorubicin + estramustine
- Development stage
- Unknown
- Lead developer
- The University of New Mexico
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
A combination regimen of the anthracycline chemotherapy agent doxorubicin and the chemohormonal agent estramustine used investigationally for metastatic, hormone-refractory (castration-resistant) prostate cancer. Doxorubicin intercalates DNA, inhibits topoisomerase II, and generates reactive oxygen species, leading to DNA damage and apoptosis. Estramustine is an estrogen–nitrogen mustard conjugate that binds microtubule-associated proteins and tubulin, disrupting microtubule dynamics, and also exerts antiandrogenic/estrogenic effects; it can sensitize prostate cancer cells to cytotoxic agents. Clinical phase I–II studies evaluated daily oral estramustine phosphate with weekly or q3‑week intravenous doxorubicin in men with hormone-refractory metastatic prostate cancer, showing partial responses and PSA declines with expected toxicities. This combination is not an approved fixed-dose product and has been studied as a protocol-defined regimen rather than a marketed co-formulation.
- Other names
- doxorubicin plus estramustinedoxorubicin and estramustinedoxorubicin + estramustine phosphate
02
Targets
DNATUBB (Tubulin (alpha and beta subunits))TOP2A (DNA topoisomerase II)
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