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eflornithine

L01XX79

Forms & Strengths

Intravenous infusion: 192 mg/mL in 100 mL vials (as eflornithine hydrochloride monohydrate)

Adult Dosing

High-risk neuroblastoma: 750 mg/m² intravenously over 1 hour twice daily (approximately 12 hours apart) from day 1 through day 5 of a 14-day cycle for up to 39 cycles
Pre-medication with antipyretics and antihistamines is recommended prior to infusion

Pediatric Dosing

Pediatric patients (≥ 1 year of age) with high-risk neuroblastoma: 750 mg/m² intravenously over 1 hour twice daily from day 1 through day 5 of a 14-day cycle for up to 39 cycles
Dosing is based on body surface area (BSA)

Indications

Reduction of the risk of relapse in pediatric and adult patients with high-risk neuroblastoma who have demonstrated at least a partial response to prior multi-agent, multimodality therapy

Mechanism of Action

Irreversible inhibitor of ornithine decarboxylase (ODC), the rate-limiting enzyme in the biosynthesis of polyamines
Depletion of polyamines inhibits DNA and RNA synthesis, resulting in decreased cellular proliferation and induction of apoptosis in rapidly dividing neuroblastoma cells

Contraindications

History of severe hypersensitivity to eflornithine or any of its components

Adverse Reactions

Ototoxicity (hearing loss, tinnitus)
Infusion-related reactions (chills, pyrexia, flushing, hypertension)
Diarrhea and abdominal pain
Vomiting and nausea
Headache and dizziness
Bone marrow suppression (anemia, neutropenia, thrombocytopenia)
Elevated liver enzymes

Drug Interactions

No formal clinical drug-drug interaction studies have been conducted
Potential for additive ototoxicity when co-administered with other ototoxic agents (e.g., aminoglycosides, loop diuretics, platinum-based chemotherapy)
Potential for additive myelosuppression with other bone marrow-suppressive therapies

Curated Content: Needs Vetting Before Put to Clinical Use