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estramustine + vinorelbine
- Development stage
- Unknown
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
A multi-agent chemotherapy regimen combining the microtubule-interfering agents estramustine and vinorelbine, investigated primarily for androgen-independent/hormone-refractory metastatic prostate cancer. Estramustine is an estradiol–nitrogen mustard conjugate that disrupts microtubule dynamics and binds microtubule-associated proteins, exerting antimitotic effects; vinorelbine is a semisynthetic Vinca alkaloid that inhibits microtubule polymerization, leading to mitotic arrest and apoptosis. Phase I/II studies reported the combination to be generally tolerable with modest activity, including prostate-specific antigen (PSA) declines in a subset of patients, using both oral and intravenous vinorelbine schedules alongside oral estramustine.[2][1]
- Other names
- vinorelbine + estramustine
02
Targets
TUBB (Tubulin (alpha and beta subunits))
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