Drug intelligence / Profile preview

estramustine + vinorelbine

Development stage
Phase 2
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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