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zibotentan + docetaxel
- Development stage
- Discontinued
- Lead developer
- AstraZeneca
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
**Zibotentan + docetaxel** is a combination therapy studied in metastatic castration-resistant prostate cancer (mCRPC). Zibotentan (ZD4054) is an oral specific endothelin A receptor antagonist, while docetaxel is a cytotoxic taxane chemotherapeutic agent that stabilizes microtubules and disrupts cell division. The rationale for this combination was based on the hypothesis that targeting both tumor biology (via blockade of endothelin A receptor involved in tumor invasion, angiogenesis, and inhibition of apoptosis) and providing cytotoxic therapy might improve clinical outcomes. Phase I, II, and large phase III clinical trials evaluated efficacy and safety; results demonstrated no significant improvement in overall survival or progression endpoints compared to docetaxel plus placebo. The most commonly reported adverse effects included edema, diarrhea, alopecia, and nausea[1][5].
- Brand names
- Taxotere + zibotentan
- Other names
- zibotentan + docetaxelZD4054 + docetaxelzibotentan and docetaxeldocetaxel and zibotentanTaxotere + zibotentan
02
Targets
EDNRA (Endothelin receptor type A)TUBB (Tubulin (alpha and beta subunits))
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