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docetaxel + estramustine
- Development stage
- Discontinued
- Lead developer
- Sanofi
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
A combination regimen of the taxane chemotherapy docetaxel and the estrogen-derived antineoplastic agent estramustine phosphate used primarily in advanced or metastatic prostate cancer resistant to androgen deprivation. Docetaxel stabilizes microtubules, inhibiting depolymerization and mitosis, leading to apoptosis. Estramustine phosphate, a prodrug of estramustine, binds microtubule-associated proteins and tubulin, disrupting microtubule dynamics and exerting anti-mitotic and anti-androgenic effects; it may also enhance docetaxel activity. Early phase trials in androgen-independent/hormone-refractory prostate cancer demonstrated PSA responses and clinical activity, leading to broader evaluation of taxane-based regimens in this setting.
- Brand names
- TaxotereEmcyt
- Other names
- docetaxel and estramustine phosphate
02
Targets
TUBB (Tubulin (alpha and beta subunits))APC (Activated protein C)ABCB1 (P-glycoprotein)
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