Eribulina
Eribulina Uses, Dosage, Side Effects, Food Interaction and all others data.
Eribulina inhibits the growth phase of microtubules without affecting the shortening phase and sequesters tubulin into nonproductive aggregates. Eribulina exerts its effects via a tubulin-based antimitotic mechanism leading to G2/M cell-cycle block, disruption of mitotic spindles, and, ultimately, apoptotic cell death after prolonged mitotic blockage.
Linear
Trade Name | Eribulina |
Availability | Prescription only |
Generic | Eribulin |
Eribulin Other Names | Eribulin, Eribulina |
Related Drugs | Arimidex, Ibrance, Femara, Xeloda, Herceptin, Lynparza, palbociclib, Halaven |
Type | |
Formula | C40H59NO11 |
Weight | Average: 729.908 Monoisotopic: 729.408811724 |
Protein binding | 49 to 65%. |
Groups | Approved, Investigational |
Therapeutic Class | Targeted Cancer Therapy |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Eribulina Mesylate is used for the treatment of patients with 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 in either the adjuvant or metastatic setting.
Pediatric Use: The safety and effectiveness of Eribulina in pediatric patients below the age of 18 years have not been established.
Geriatric Use: Study 1 did not include sufficient numbers of subjects aged 65 years and older to determine whether they respond differently from younger subjects. Of the 827 subjects who received the recommended dose and schedule of Eribulina in clinical studies, 15% (121/827) were 65 and older, and 2% (17/827) patients were 75 and older. No overall differences in safety were observed between these subjects and younger subjects.
Hepatic Impairment: A lower starting dose is recommended for patients with mild (Child-Pugh A) and moderate (Child-Pugh B) hepatic impairment. Patients with severe hepatic impairment (Child-Pugh C) were not studied.
Renal Impairment: A lower starting dose is recommended for patients with moderate (CrCl 30-50 mL/min) renal impairment. Patients with severe (CrCl < 30 mL/min) renal impairment were not studied.
Eribulina is also used to associated treatment for these conditions: Metastatic Liposarcoma, Refractory, metastatic Breast cancer, Unresectable Liposarcoma
How Eribulina works
Eribulina inhibits the growth phase of microtubules without affecting the shortening phase and sequesters tubulin into nonproductive aggregates. Eribulina exerts its effects via a tubulin-based antimitotic mechanism leading to G2/M cell-cycle block, disruption of mitotic spindles, and, ultimately, apoptotic cell death after prolonged mitotic blockage. [FDA]
Dosage
Eribulina dosage
The recommended dose of Eribulina Mesylate is 1.4 mg/m2 administered intravenously over 2 to 5 minutes on Days 1 and 8 of a 21-day cycle.
The recommended dose of Eribulina Mesylate in patients with mild hepatic impairment (Child-Pugh A) is 1.1 mg/m2 administered intravenously over 2 to 5 minutes on Days 1 and 8 of a 21-day cycle.
The recommended dose of Eribulina Mesylate in patients with moderate hepatic impairment (Child-Pugh B) is 0.7 mg/m2 administered intravenously over 2 to 5 minutes on Days 1 and 8 of a 21-day cycle.
The recommended dose of Eribulina Mesylate in patients with moderate renal impairment (creatinine clearance of 30-50 mL/min) is 1.1 mg/m2 administered intravenously over 2 to 5 minutes on Days 1 and 8 of a 21-day cycle.
Side Effects
The most common adverse reactions (incidence ≥25%) were neutropenia, anemia, asthenia/fatigue, alopecia, peripheral neuropathy, nausea, and constipation.
Toxicity
Peripheral neuropathy was the most common toxicity leading to discontinuation of eribulin (5 percent). [Richard Pazdur, M.D., director of the FDA's Division of Oncology Drug Products.] Single doses of 0.75 mg/kg were lethal to rats and two doses of 0.075 mg/kg were lethal to dogs. The no-observed-adverse-effect level (NOAEL) in rats and dogs were 0.015 and 0.0045 mg/kg/day, respectively.
Precaution
Neutropenia: Monitor peripheral blood cell counts and adjust dose as appropriate.
Peripheral Neuropathy: Monitor for signs of neuropathy. Manage with dose delay and adjustment.
Use in Pregnancy: Fetal harm can occur when administered to a pregnant woman.
QT Prolongation: Monitor for prolonged QT intervals in patients with congestive heart failure, bradyarrhythmias, drugs known to prolong the QT interval, and electrolyte abnormalities. Avoid in patients with congenital long QT syndrome.
Interaction
Effects of Other Drugs on Eribulina Mesylate: No drug-drug interactions are expected with CYP3A4 inhibitors or P-gp inhibitors. The effect of ketoconazole, a strong inhibitor of cytochrome P450 3A4 (CYP3A4) and a P-gp inhibitor, on the pharmacokinetics (PK) of eribulin was studied in an open-label, two-treatment, two-sequence, two-way crossover trial in 12 patients with advanced solid tumors. The mean dose-normalized AUC values were similar when eribulin was administered with or without ketoconazole (ratio of the mean AUC: 0.97; 90% CI: 0.83, 1.12).
Effect of Eribulina Mesylate on Other Drugs: Eribulina does not inhibit CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1 or CYP3A4 enzymes or induce CYP1A2, CYP2C9, CYP2C19 or CYP3A4 enzymes at relevant clinical concentrations. Eribulina is not expected to alter the plasma concentrations of drugs that are substrates of these enzymes
Food Interaction
No interactions found.Eribulina Drug Interaction
Moderate: paclitaxel protein-bound, doxorubicin, prochlorperazine, tramadolUnknown: everolimus, ubiquinone, warfarin, medroxyprogesterone, ethanol, levothyroxine, fulvestrant, emollients topical, palbociclib, bioflavonoids, levothyroxine, multivitamin, cyanocobalamin, ascorbic acid, cholecalciferol, cetirizine
Eribulina Disease Interaction
Major: infectionsModerate: cytopenias, hepatic impairment, peripheral neuropathy, QT prolongation, renal impairment
Volume of Distribution
43 L/m2 to 114 L/m2
Half Life
about 40 hours
Clearance
1.16 L/hr/m2 to 2.42 L/hr/m2 (dose range of 0.25 mg/m2 to 4.0 mg/m2). [FDA]
Elimination Route
Eribulina is eliminated primarily in feces unchanged.
Pregnancy & Breastfeeding use
Pregnancy Category D. There are no adequate and well-controlled studies with Eribulina Mesylate in pregnant women. It is not known whether Eribulina Mesylate is excreted into human milk. No studies in humans or animals were conducted to determine if Eribulina Mesylate is excreted into milk. Because many drugs are excreted into human milk and because of the potential for serious adverse reactions in human milk-fed infants from Eribulina Mesylate, a decision should be made whether to discontinue nursing or to discontinue Eribulina Mesylate taking into account the importance of the drug to the mother.
Acute Overdose
Overdosage of Eribulina has been reported at approximately 4 times the recommended dose, which resulted in Grade 3 neutropenia lasting seven days and a Grade 3 hypersensitivity reaction lasting one day. There is no known antidote for Eribulina overdose.
Storage Condition
Store at 25°C; excursions permitted to 15°-30°C. Do not freeze. Store the vials in their original cartons.
Innovators Monograph
You find simplified version here Eribulina
Eribulina contains Eribulin see full prescribing information from innovator Eribulina Monograph, Eribulina MSDS, Eribulina FDA label