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epirubicin + estramustine phosphate + celecoxib
- Development stage
- Unknown
- Lead developer
- United States Department of Veterans Affairs
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
A multi-agent antineoplastic regimen combining the anthracycline epirubicin, the estrogen-derived antimicrotubule agent estramustine phosphate, and the selective COX-2 inhibitor celecoxib. The combination has been studied primarily in hormone-resistant/metastatic castration-resistant prostate cancer, including as second-line therapy following taxane-based regimens. Epirubicin intercalates DNA and stabilizes topoisomerase II-DNA cleavable complexes to inhibit DNA replication and transcription. Estramustine phosphate disrupts microtubule assembly and dynamics, impairing mitosis. Celecoxib selectively inhibits cyclooxygenase-2, reducing prostaglandin-mediated tumor growth and angiogenesis; it has been explored for potential synergy with cytotoxics and effects on tumor microenvironment and cancer stemness. This combination has been evaluated in phase II settings to assess PSA responses, radiographic responses, toxicity, survival, and quality of life in advanced prostate cancer.
- Other names
- epirubicin/estramustine phosphate/celecoxib
02
Targets
PTGS2 (Prostaglandin-Endoperoxide Synthase 2)DNATUBB (Tubulin (alpha and beta subunits))TOP2A (DNA topoisomerase II)
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