Halaven Eribulin Mesilate Injection

1. Indications and Usage
Breast Cancer:
Indicated for the treatment of patients with locally recurrent or metastatic breast cancer who have previously received at least two chemotherapeutic regimens for the treatment of metastatic disease. Prior therapy should have included an anthracycline and a taxane.
Liposarcoma:
Indicated for the treatment of patients with unresectable or metastatic liposarcoma who have received a prior anthracycline-containing regimen.
2. Dosage and Administration
Route of Administration:
For Intravenous (IV) Infusion ONLY.
Recommended Dosage (Breast Cancer):
Dose: 1.2 mg/m².
Schedule: Administered as a 2-minute IV infusion on Days 1 and 8 of a 21-day cycle.
Recommended Dosage (Liposarcoma):
Dose: 1.4 mg/m².
Schedule: Administered as a 2-minute IV infusion on Days 1 and 8 of a 21-day cycle.
Administration Instructions:
Dilute in 50 mL or 100 mL of 0.9% Sodium Chloride Injection.
Do not dilute with Dextrose solutions.
Do not use filters during administration (the drug may adsorb to PVDF/nylon filters).
Dose Adjustments:
Reduce dose for neutropenia (ANC < 1,000/mm³), thrombocytopenia (Platelets < 50,000/mm³), or Grade 3/4 non-hematologic toxicity.
Reduce dose for Grade 2 or greater peripheral neuropathy.
3. Mechanism of Action
Microtubule Dynamics Inhibitor:
Eribulin is a macrocyclic ketone analog of halichondrin B. It binds to the vinca domain of tubulin.
Anti-Cancer Effect:
Unlike vinca alkaloids, eribulin does not significantly inhibit microtubule depolymerization. Instead, it inhibits the growth phase of microtubules. This leads to cell cycle arrest at the G2/M phase and induces apoptosis in cancer cells. It also reverses epithelial-to-mesenchymal transition (EMT) and induces remodeling of the tumor microenvironment.
4. Safety and Warnings
Neutropenia and Sepsis:
Neutropenia is common and can be severe. Monitor absolute neutrophil count (ANC) prior to each dose. Withhold or reduce dose if ANC < 1,000/mm³ or if febrile neutropenia occurs.
Peripheral Neuropathy:
Can cause sensory and motor neuropathy. Monitor patients regularly; dose interruption or reduction is required based on severity.
Embryo-Fetal Toxicity:
Can cause fetal harm. Females of reproductive potential must use effective contraception during treatment and for at least 3 months after the final dose.
Long QT Syndrome:
Eribulin may prolong the QT interval. Use with caution in patients with a history of QT prolongation or those taking medications known to prolong QT.
5. Adverse Reactions
Most Common (Incidence ≥25%):
Neutropenia, fatigue, nausea, peripheral neuropathy, alopecia, constipation, vomiting, and anemia.
6. Drug Interactions
CYP450 System:
Eribulin is not a significant substrate or inhibitor of CYP450 enzymes.
P-gp Inhibitors:
Eribulin is a P-gp substrate. Concomitant use with strong P-gp inhibitors (e.g., ketoconazole) may increase eribulin exposure, though clinical significance is currently unknown.
7. Pharmaceutical Information
Chemical Composition:
Active Ingredient: Eribulin mesilate.
Appearance: Clear, colorless liquid.
Storage: Store vials refrigerated at 2°C to 8°C (36°F to 46°F). Do not freeze. Store in the original carton to protect from light.