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eribulin

L01XX41

Forms & Strengths

Intravenous solution: 0.5 mg/mL (as eribulin mesylate) in 2 mL single-dose vials

Adult Dosing

Metastatic breast cancer: 1.4 mg/m2 IV over 2 to 5 minutes on Days 1 and 8 of a 21-day cycle
Liposarcoma: 1.4 mg/m2 IV over 2 to 5 minutes on Days 1 and 8 of a 21-day cycle
Renal impairment (CrCl 15-49 mL/min): 1.1 mg/m2 IV on Days 1 and 8 of a 21-day cycle
Hepatic impairment (mild/moderate, Child-Pugh A or B): 1.1 mg/m2 or 0.7 mg/m2 respectively, IV on Days 1 and 8 of a 21-day cycle

Pediatric Dosing

Safety and efficacy in pediatric patients have not been established

Indications

Treatment of patients with metastatic breast cancer who have previously received at least two chemotherapeutic regimens for metastatic disease (must have included an anthracycline and a taxane)
Treatment of patients with unresectable or metastatic liposarcoma who have received a prior anthracycline-containing regimen

Mechanism of Action

Non-taxane microtubule dynamics inhibitor
Binds to the plus ends of microtubules to sequester tubulin into non-productive aggregates
Exerts a distinct antimicrotubule mechanism causing cell cycle arrest at the G2/M phase, disruption of mitotic spindles, and apoptotic cell death

Contraindications

Hypersensitivity to eribulin or any of its excipients
Severe hepatic impairment (insufficient data)

Adverse Reactions

Neutropenia, leukopenia, anemia, thrombocytopenia
Fatigue, asthenia
Peripheral neuropathy (sensory and motor)
Nausea, constipation, diarrhea, vomiting
Alopecia, decreased appetite, dyspnea
QT prolongation

Drug Interactions

Strong CYP3A4 inhibitors: monitor for increased toxicity (though eribulin is minimally metabolized by CYP3A4)
Strong CYP3A4 inducers: may decrease eribulin exposure
QT-prolonging drugs: concurrent use may increase the risk of torsades de pointes

Curated Content: Needs Vetting Before Put to Clinical Use