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docetaxel + ketoconazole
- Development stage
- Unknown
- Lead developer
- Sanofi
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Docetaxel + ketoconazole is a combination therapy investigated primarily for the treatment of advanced or metastatic castration-resistant prostate cancer. Docetaxel is a taxane-class chemotherapeutic agent that inhibits microtubule depolymerization, thereby disrupting cell division and inducing apoptosis in cancer cells. Ketoconazole, an antifungal agent, also acts as a second-line hormonal therapy in prostate cancer by inhibiting steroidogenesis through cytochrome P450 enzyme (CYP17A1) inhibition. The combination has been studied due to potential synergistic antitumor effects and pharmacokinetic interactions; ketoconazole can increase docetaxel exposure by inhibiting its metabolism via CYP3A4. Clinical studies have shown significant antitumor activity with this regimen, though dose-limiting toxicities such as neutropenia and fatigue have been observed[1][2][3].
- Brand names
- TaxotereNizoral
- Other names
- Docetaxel and Ketoconazole
02
Targets
TUBB (Tubulin (alpha and beta subunits))CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)CYP3A4 (Cytochrome P450 3A4)
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