Halaven

Erebulin mesylate (Halaven) instructions
Common name: Eribulin mesylate
Trade name: Halaven
Full names: Eribulin mesylate, Eribulin, Halaven, eribulin mesylate

Indications:
①Metastatic breast cancer (patients who have previously received at least two chemotherapy treatments for metastatic disease); ②Unresectable or metastatic liposarcoma (patients who have previously received anthracyclines)

Usage and dosage:
Metastatic breast cancer
Inject 1.4 mg intravenously over 2-5 minutes on days 1 and 8 of a 21-day cycle /m²
Liposarcoma
1.4 mg IV over 2-5 minutes on days 1 and 8 of a 21-day cycle /m²

Adverse reactions:
> 10%
Neutropenia (82%)
Anemia (58%)
Weakness/fatigue (54%)
Alopecia (45%)
Peripheral neuropathy (35%)
Nausea (35 %)
Constipation (25%)
Arthralgia/myalgia (22%)
Fever (21%)
Weight loss (21%)
Anorexia (20%)
Headache (19%)
Vomiting (18%)
Diarrhea (18%)
Back pain (16%)
Trouble breathing (16%)
Cough (14%)
Bone pain (12%)
Extremity pain (11%)
Urine Road infections (10%)

1-10%
Increased tearing
Indigestion
Abdominal pain
Stomatitis
Xerostomia
URI
Hypokalemia
Muscle Cramps/weakness
Disturbance of taste
Dizziness
Insomnia
Depression
Skin rash

Postmarketing reports
Gastrointestinal disorders: Pancreatitis
Blood and lymphatic disorders: Lymphopenia
Hepatobiliary disorders: Hepatotoxicity
Immune system disorders: Drug hypersensitivity
Infections and infections: Pneumonia, sepsis/neutropenia
Metabolic and nutritional disorders: Hypomagnesemia, dehydration
Respiratory, thoracic, and mediastinal disorders: Interstitial lung disease
Skin and subcutaneous tissue disorders: Pruritus, Stevens-Johnson syndrome, toxic epidermal necrosis

Contraindications:
Unknown

Precautions:
Monitor for peripheral neuropathy before each dose
Report for severe neutropenia; monitor complete blood count before each dose; increase monitoring frequency in patients who develop Grade 3 or 4 cytopenias; Delay treatment and reduce subsequent doses in patients with febrile neutropenia or grade 4 neutropenia lasting more than 7 days
If ANC <1,000/m³, platelets <75,000 /m³ or Grade 3-4 non-hematologic toxicity, please delay dosing and/or reduce dose
Caution CHF, cardiac arrhythmias, and congenital long QT syndrome (monitor for QT prolongation); correct hypokalemia or hypomagnesemia before dosing
With other drugs that prolong the QT interval Drugs (such as Class Ia or III antiarrhythmic drugs, thiopyridazine, erythromycin) may cause additive effects when used together
Based on animal studies and their mechanism of action, when used with a female partner of reproductive potential in pregnant women or men, it may cause harm to the fetus
/p>

Storage:
Store undiluted eribulin in a syringe at room temperature for up to 4 hours or refrigerated (40°F or /4°C) for up to 24 hours
Store diluted eribulin at room temperature Keep lin solution for up to 4 hours, or store refrigerated (40°F or /4°C) for up to 24 hours

Mechanism of Action:
Halaven (eribulin mesylate) is a non-taxane inhibitor of microtubule dynamics. It is a synthetic analogue of rutin B, a product isolated from the marine sponge Squirrel Cage. Eribulin inhibits the growth phase of microtubules without affecting their shortening phase and sequesters tubulin into nonproductive aggregates. Eribulin acts through a tubulin-based antimitotic mechanism, causing G2/M cell cycle arrest, mitotic spindle disruption, and ultimately apoptotic cell death after prolonged blockage of mitosis.

Efficacy and Safety:
The FDA's approval of Halaven is based on an open-label, randomized, multicenter trial of 762 patients with metastatic breast cancer who received at least two chemotherapy regimens and experienced disease progression within six months of their last chemotherapy regimen. Subjects were randomized to receive Halaven (n=508) or monotherapy selected prior to randomization (n=254). Randomization was stratified by geographic region, HER2/neu status, and previous capecitabine exposure. Halaven was administered at a dose of 1.4 mg/m2 on days 1 and 8 of the 21-day cycle. Patients treated with Halaven received a median of 5 cycles of treatment. Treatment in the control group consisted of 97% chemotherapy and 3% hormonal therapy. The primary efficacy outcome was overall survival. A statistically significant improvement in overall survival was observed between the Halaven and placebo groups: 274 of 508 subjects died in the Halaven group compared with 148 of 254 subjects in the control group (p=0.041). An updated, unplanned survival analysis was performed when 77% of events were observed and consistent with the primary analysis (386 vs. 203 deaths, respectively). According to RECIST criteria, the objective response rate in the Halaven arm was 11%, and the median duration of response was 4.2 months. 203 people died respectively). According to RECIST criteria, the objective response rate in the Halaven arm was 11%, and the median duration of response was 4.2 months. 203 people died respectively). According to RECIST criteria, the objective response rate in the Halaven arm was 11%, and the median duration of response was 4.2 months.