eribulin

Absorption: IV administration results in complete bioavailability.

Distribution: Unknown.

Metabolism/Excretion: Minimal metabolism, mostly excreted unchanged in feces (82%) and less in urine (9%).

Half-Life: 40 hr.

Time/Action Profile ⬆ ⬇

(effects on blood counts)

ROUTE	ONSET	PEAK	DURATION
IV	within days	7–14 days	up to 2 wk

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Severe hepatic impairment;
Severe renal impairment (CCr <15 mL/min);
Congenital long QT syndrome;
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

HF, bradyarrhythmias, concurrent use of drugs known to prolong the QT interval (including Class Ia and III antiarrhythmics), or electrolyte abnormalities (↑ risk of arrhythmias);
Moderate renal impairment;
Mild or moderate hepatic impairment;
Rep: Women of reproductive potential and men with female partners of reproductive potential;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: peripheral edema, QT interval prolongation

Derm: alopecia, stevens-johnson syndrome, toxic epidermal necrolysis, rash

EENT: ↑lacrimation

F and E: hypokalemia

GI: anorexia, constipation, nausea, abdominal pain, abnormal taste, diarrhea, dry mouth, dyspepsia, mucositis, PANCREATITIS, vomiting

GU: urinary tract infection

Hemat: anemia, neutropenia

MS: arthralgia, myalgia

Neuro: fatigue, weakness, depression, dizziness, headache, insomnia, peripheral neuropathy

Resp: cough, dyspnea, upper respiratory tract infection

Misc: fever

Interactions ⬆ ⬇

Drug-drug:

↑risk of bone marrow depression with other antineoplastics or radiation therapy.
↓antibody response and ↑ risk of adverse reactions with live-virus vaccines.

Route/Dosage ⬆ ⬇

IV (Adults ): 1.4 mg/m² on days 1 and 8 of a 21-day cycle.

Renal Impairment

IV (Adults ): CCr 15–49 mL/min: 1.1 mg/m² on days 1 and 8 of a 21-day cycle.

Hepatic Impairment

IV (Adults ): Mild hepatic impairment: 1.1 mg/m² on days 1 and 8 of a 21-day cycle Moderate hepatic impairment: 0.7 mg/m² on days 1 and 8 of a 21-day cycle.

Availability ⬆ ⬇

(Generic available)

Solution for injection: 0.5 mg/mL

Assessment ⬆ ⬇

Assess for peripheral motor and sensory neuropathy (numbness, tingling, burning in hands or feet).
Monitor ECG periodically as indicated.

Lab Test Considerations:

Monitor CBC prior to each dose; ↑ frequency of monitoring in patients who develop Grade 3 or 4 cytopenias.
- Monitor electrolytes periodically during therapy.

Implementation ⬆ ⬇

Do not confuse eribulin with epirubicin.
Correct hypokalemia or hypomagnesemia prior to initiating therapy.

IV Administration:

Do not administer on Day 1 or Day 8 if: ANC <1000/mm³, platelets <75,000/mm³, or Grade 3 or 4 nonhematological toxicities occur.
Day 8 dose may be delayed for a maximum of 1 wk: If toxicities do not resolve or improve to ≤Grade 2 severity by Day 15, omit dose.
- If toxicities resolve or improve to ≤Grade 2 by Day 15, administer eribulin at a reduced dose and initiate next cycle no sooner than 2 wk later.
- If a dose has been delayed for toxicity and toxicities have recovered to Grade 2 severity or less, resume eribulin at a reduced dose of 1.1 mg/m².
- Permanently reduce 1.4 mg/m² eribulin dose to 1.1 mg/m² if: ANC <500/mm³ for >7 days, ANC <1000/mm³ either fever or infection, platelets <25,000/mm³, platelets <50,000/mm³ requiring transfusion, nonhematologic Grade 3 or 4 toxicities, or omission or delay of Day 8 eribulin dose in previous cycle for toxicity.
- Permanently reduce 1.4 mg/m² eribulin dose to 0.7 mg/m² if: occurrence of any event requiring permanent dose reduction while receiving 1.1 mg/m² dose.
- If occurrence of any event requiring permanent dose reduction while receiving 0.7 mg/m²: discontinue eribulin.
Diluent: Administer undiluted or dilute in 100 mL of 0.9% NaCl. Store undiluted in syringe or diluted eribulin for up to 4 hr at room temperature or for up to 24 hr under refrigeration. Discard unused portion of vial.
Rate: Infuse over 2–5 min on Days 1 and 8 of a 21-day cycle.
Y-Site Incompatibility: Do not dilute in or administer through an IV line containing solutions with dextrose or other medications.

Patient/Family Teaching ⬆ ⬇

Advise patient to notify health care professional if fever of ≥100.5°F or other signs or symptoms of infection (chills, cough, burning or pain on urination) or rash occur.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
Advise patient not to receive vaccinations without consulting health care professional.
Rep: May cause fetal harm. Advise females of reproductive potential to use effective contraception during and for at least 2 wk after last dose of therapy. Advise males with female partners of reproductive potential to use effective contraception for 3.5 mo after final dose. Instruct females of reproductive potential to notify health care professional immediately if pregnancy is planned and to avoid breastfeeding during therapy. May cause male infertility.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇