Eribulin Mesylate

Drug overview for ERIBULIN MESYLATE (eribulin mesylate):

Generic name: ERIBULIN MESYLATE (ER-i-BUE-lin)
Drug class: Halochondrin B Analogs, Microtubule Inhibitor
Therapeutic class:

Eribulin mesylate, a synthetic analog of halichondrin B and nontaxane microtubule dynamics inhibitor, is an antineoplastic agent.

No enhanced Uses information available for this drug.

DRUG IMAGES

ERIBULIN MESYLATE 1 MG/2 ML VL

The following indications for ERIBULIN MESYLATE (eribulin mesylate) have been approved by the FDA:

Indications:
None.

Professional Synonyms:
None.

The following dosing information is available for ERIBULIN MESYLATE (eribulin mesylate):

Dosing
Administration
Dosing Information
Generic

Eribulin is commercially available as eribulin mesylate; dosage of eribulin mesylate is expressed in terms of the mesylate salt.

Dosage of eribulin mesylate is based on the patient's body surface area.

For the treatment of metastatic breast cancer in patients who have received at least 2 prior chemotherapeutic regimens (including an anthracycline and a taxane), the recommended dosage of eribulin mesylate in adults is 1.4 mg/m2 administered IV over 2-5 minutes on days 1 and 8 of a 21-day treatment cycle. Patients should have an absolute neutrophil count (ANC) of at least 1000/mm3 and a platelet count of at least 75,000/mm3 prior to each dose.

In addition, any nonhematologic toxicities should have resolved to grade 2 in severity or less before a dose is administered. Dose delays and reductions are required in patients who experience severe hematologic and/or nonhematologic toxicities during therapy. (See Dosage and Administration: Dosage Modification for Toxicity.)

In the principal efficacy study, eribulin was continued until disease progression, intolerable toxicity, or patient withdrawal for other reasons occurred; patients received a median of 5 cycles (range: 1-23 cycles) of therapy with the drug.

The dose of eribulin mesylate on day 1 or day 8 of the treatment cycle should be withheld if ANC counts are less than 1000/mm3, platelet counts are less than 75,000/mm3, or grade 3 or 4 nonhematologic toxicities are present. The dose on day 8 may be delayed for a maximum of 1 week for these toxicities. If toxicities resolve or improve to grade 2 in severity or less by day 15, eribulin therapy may be resumed at a reduced dosage (see Table 1) and the next treatment cycle should be initiated no sooner than 2 weeks later.

If toxicities do not resolve or improve to grade 2 or less within this 1-week time period, the dose should be omitted.

Table 1. Recommended Dosage Reductions for Hematologic and Nonhematologic Toxicities

Permanently Reduce Dosage in Recommended Dosage on Days 1 and 8 Patients Initially Dosed with 1.4 of 21-Day Cycle mg/m2 for Any of the Following Toxicities: ANC <500/mm3 for >7 days 1.1 mg/m2 ANC <1000/mm3 with fever or 1.1

mg/m2 infection Platelets <25,000/mm3 1.1 mg/m2 Platelets <50,000/mm3 requiring 1.1 mg/m2 transfusion Nonhematologic grade 3 or 4 1.1

mg/m2 toxicities Omission or delay of day 8 dose in 1.1 mg/m2 previous cycle for toxicity If any of the above events occurs while receiving 1.1 mg/m2, reduce dosage to 0.7

mg/m2. If any of the above events occurs while receiving 0.7 mg/m2, discontinue therapy.

Eribulin mesylate is administered IV, either as an injection or short infusion, over 2-5 minutes. The drug should be given only by IV administration. In clinical trials, the drug was given IV over 1-60 minutes+ either directly or diluted in 0.9%

sodium chloride injection to a concentration of 0.01-0.1 mg/mL; the infusion time was independent of whether the injection was diluted or undiluted.

Good peripheral venous access or a patent central line should be ensured prior to administration. The injection does not appear to be a vesicant or irritant; if extravasation occurs, there is no specific antidote and treatment should be symptomatic. Eribulin mesylate injection is commercially available as a ready-to-use solution containing 0.5

mg of eribulin mesylate per mL in single-use vials. The appropriate dose of the drug should be withdrawn from the vial and administered either undiluted or diluted with 100 mL of 0.9% sodium chloride injection.

The manufacturer states that eribulin injection should not be diluted or administered with dextrose solutions; the injection also should not be administered in the same IV line with other drugs. Undiluted solutions of eribulin may be stored in the syringe for up to 4 hours at room temperature or up to 24 hours under refrigeration (4degreesC). Diluted solutions also may be stored for up to 4 hours at room temperature or up to 24 hours under refrigeration.

Any unused portions of the vial should be discarded. Procedures for proper handling and disposal of antineoplastic drugs should be followed when preparing or administering eribulin. For additional information on proper procedures for handling antineoplastic agents, see the ASHP Guidelines on Handling Hazardous Drugs at https://www.ahfsdruginformation.com.

Unopened vials of eribulin mesylate injection should be stored in their original cartons at 25degreesC, but may be exposed to temperatures ranging from 15-30degreesC. Freezing of the vials should be avoided.

No dosing information available.

No generic dosing information available.

The following precautions are available for ERIBULIN MESYLATE (eribulin mesylate):

Pediatric
Pregnant
Lactation
Geriatric

Safety and effectiveness of eribulin in pediatric patients younger than 18 years of age have not been established.

Contraindicated

None

Severe Precaution

None

Management or Monitoring Precaution

None

Category D. (See Fetal/Neonatal Morbidity and Mortality under Cautions: Warnings/Precautions.)

Not known whether eribulin mesylate is distributed into human milk. Because of the potential for serious adverse reactions to eribulin in nursing infants, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.

Contraindicated
Absolute contraindication. (Human data usually available to support recommendations.) This drug should not be given to breast feeding mothers.

Drug Name	Excretion Potential	Effect on Infant	Notes
Eribulin	Unknown. It is unknown whether the drug is excreted in human breast milk.	It is not known whether this drug has an adverse effect on the nursing infant. (No data or inconclusive human data)	Avoid breastfeeding during tx and for 2 weeks after last dose

The EMBRACE study did not include sufficient numbers of patients 65 years of age and older to determine whether geriatric patients respond differently to eribulin than younger patients. Among 827 patients who received eribulin in clinical studies, 121 (15%) were 65 years of age or older and 17 (2%) were 75 years of age or older. No overall differences in safety were observed in these patients compared with those younger than 65 years of age.