Halaven
Metastatic breast cancer — in patients who have previously received at least two chemotherapeutic regimens for metastatic disease (prior therapy should include an anthracycline and a taxane); Unresectable or metastatic liposarcoma — in patients who have received a prior anthracycline-containing regimen.
1.4 mg/m² IV over 2-5 minutes on Days 1 and 8 of a 21-day cycle
Do NOT administer on Day 1 if: ANC <1,000/mm³, platelets <75,000/mm³, or Grade 3-4 non-hematologic toxicity
Dose reductions: 1.1 mg/m², then 0.7 mg/m²
Hepatic impairment (Child-Pugh A): 1.1 mg/m²; (Child-Pugh B): 0.7 mg/m²
Injection: 1 mg/2 mL (0.5 mg/mL) solution in single-dose vials
None listed.
- Neutropenia: Grade 3-4 in 57%. Febrile neutropenia in 5%. Fatal neutropenic sepsis reported. Monitor CBC before each dose.
- Peripheral Neuropathy: In 35% (Grade 3-4: 8%). Monitor for signs of neuropathy. Delay or reduce dose for Grade 3-4.
- QT Prolongation: QTcF prolongation >60 ms in 4.4%. Monitor ECGs, especially in patients with CHF, bradyarrhythmias, or electrolyte imbalance.
- Embryo-Fetal Toxicity
Neutropenia (82%), fatigue (54%), alopecia (45%), nausea (35%), constipation (25%), peripheral neuropathy (35%), anemia (20%), asthenia (22%), weight decrease (21%), pyrexia (12%)
Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.
Eribulin is a non-taxane microtubule dynamics inhibitor derived from halichondrin B (a marine sponge natural product). Unlike taxanes (which stabilize microtubules) or vinca alkaloids (which destabilize microtubules at both ends), eribulin inhibits microtubule growth by binding specifically to the plus ends of microtubules without affecting shortening. This unique mechanism leads to irreversible mitotic blockade, disruption of mitotic spindles, and apoptosis after prolonged mitotic arrest. Eribulin also has anti-metastatic effects by promoting epithelial-mesenchymal transition reversal and tumor vasculature remodeling.
Half-life: approximately 40 hours. Clearance: 1.16 L/h/m². Vd: 43-114 L/m². Protein binding: 49-65%. Minimal metabolism (no significant CYP involvement); excreted primarily unchanged in feces (82%). No dose adjustment for mild-moderate renal impairment.
Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.
- EMBRACE — Eribulin vs. physician's choice in pretreated metastatic breast cancer. Phase III, n=762.