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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › CYTOTOXIC ANTIBIOTICS AND RELATED SUBSTANCES › Other cytotoxic antibiotics
utidelone
L01DC05
Forms & Strengths
- Lyophilized powder for injection: 20 mg
- Lyophilized powder for injection: 50 mg
Adult Dosing
- Advanced or metastatic breast cancer: 30-40 mg/m² intravenously once daily on days 1 to 5 of a 21-day cycle
- Typically administered in combination with capecitabine for refractory metastatic breast cancer
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of advanced or metastatic breast cancer, particularly in patients who have failed anthracycline and taxane therapies
Mechanism of Action
- Epothilone analog (microtubule stabilizer)
- Binds to tubulin, promotes microtubule polymerization, and stabilizes microtubules against depolymerization
- Induces cell cycle arrest at the G2/M phase and triggers apoptosis in cancer cells
Contraindications
- Hypersensitivity to utidelone or other epothilones
- Severe baseline neutropenia (e.g., ANC < 1.5 x 10^9/L) or severe baseline thrombocytopenia
- Severe hepatic impairment
Adverse Reactions
- Peripheral neuropathy (sensory and motor)
- Myelosuppression (neutropenia, leukopenia, anemia, thrombocytopenia)
- Fatigue and asthenia
- Gastrointestinal disturbances (nausea, vomiting, diarrhea, stomatitis)
- Elevated liver transaminases and bilirubin
Drug Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) may increase utidelone exposure and toxicity
- Strong CYP3A4 inducers (e.g., rifampin, carbamazepine) may decrease utidelone efficacy
- Concomitant use with other neurotoxic or myelosuppressive agents may exacerbate adverse effects
Curated Content: Needs Vetting Before Put to Clinical Use