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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › OTHER ANTINEOPLASTIC AGENTS › Other antineoplastic agents
amsacrine
L01XX01
Forms & Strengths
- Intravenous solution: 50 mg/mL (requires reconstitution/dilution)
Adult Dosing
- Acute leukemia: 90-120 mg/m²/day IV for 1-5 days every 3-4 weeks
- Refractory malignancies: 75-100 mg/m²/day IV for 3 consecutive days every 3 weeks
Pediatric Dosing
- Safety and efficacy in pediatric patients not well established; clinical trial dosing typically extrapolated from adult regimens (e.g., 75-100 mg/m²/day for 3 days)
Indications
- Acute lymphoblastic leukemia (ALL) in adults
- Acute myeloid leukemia (AML) in adults
- Refractory malignant lymphomas
Mechanism of Action
- Amsacrine is an acridine derivative antineoplastic agent that intercalates between DNA base pairs and inhibits topoisomerase II, leading to DNA single- and double-strand breaks and cell death
Contraindications
- Hypersensitivity to amsacrine or related acridine derivatives
- Severe preexisting myelosuppression not secondary to disease
- Severe hepatic impairment
- Severe electrolyte disturbances (hypokalemia, hypomagnesemia) due to arrhythmia risk
Adverse Reactions
- Severe myelosuppression (leukopenia, thrombocytopenia, anemia)
- Severe cardiac arrhythmias (ventricular tachycardia, torsades de pointes associated with hypokalemia)
- Stomatitis and mucositis
- Nausea, vomiting, and diarrhea
- Transient abnormal liver function tests
- Alopecia
- Local phlebitis or tissue necrosis upon extravasation
Drug Interactions
- QT-prolonging drugs (increased risk of severe ventricular arrhythmias)
- Other myelosuppressive chemotherapeutic agents (additive bone marrow suppression)
- Potent CYP450 inhibitors/inducers (potential pharmacokinetic alterations)
- Live virus vaccines (risk of disseminated infection)
Curated Content: Needs Vetting Before Put to Clinical Use