Intravenous Locally advanced breast cancer, Metastatic breast cancer
Adult: Doses are expressed in terms of eribulin mesilate (each 1.4 mg eribulin mesilate is equivalent to 1.23 mg eribulin base). In patients who have progressed after at least 1 chemotherapy regimen, which included an anthracycline and a taxane in either adjuvant or metastatic setting: 1.4 mg/m2 to be given over 2-5 minutes on Days 1 and 8 of a 21-day cycle. Dose reduction, interruption, or discontinuation may be required according to individual safety or tolerability (refer to detailed product guideline).
Adult: Doses are expressed in terms of eribulin mesilate (each 1.4 mg eribulin mesilate is equivalent to 1.23 mg eribulin base). In patients who have previously received an anthracycline-containing therapy: 1.4 mg/m2 to be given over 2-5 minutes on Days 1 and 8 of a 21-day cycle. Dose reduction, interruption, or discontinuation may be required according to individual safety or tolerability (refer to detailed product guideline).
Renal Impairment
CrCl (mL/min)
Dosage
15-49
As eribulin mesilate: 1.1 mg/m2 (equivalent to 0.97 mg/m2 eribulin base) to be given over 2-5 minutes on Days 1 and 8 of a 21-day cycle. Dosing recommendations may vary between countries (refer to specific product guidelines).
Hepatic Impairment
Mild (Child-Pugh class A): As erbulin mesilate: 1.1 mg/m2 (equivalent to 0.97 mg/m2 eribulin base) to be given over 2-5 minutes on Days 1 and 8 of a 21-day cycle. Moderate (Child-Pugh class B): As erbulin mesilate: 0.7 mg/m2 (equivalent to 0.62 mg/m2 eribulin base) to be given over 2-5 minutes on Days 1 and 8 of a 21-day cycle. Severe (Child-Pugh class C): Dose reduction may be required.
Reconstitution
May dilute in 100 mL of NaCl 0.9% inj.
Incompatibility
Solutions containing dextrose.
Contraindications
Congenital long QT syndrome. Pregnancy and lactation.
Special Precautions
Patient with predisposition to QT prolongation (e.g. CHF, bradyarrhythmia, electrolyte disturbances). Available products may have vial strength and dosing expressed as either eribulin mesilate or eribulin base; refer to individual product guideline for detailed information. Renal and hepatic impairment.
Adverse Reactions
Significant: Bone marrow suppression (e.g. severe neutropenia, leucopenia, anaemia, thrombocytopenia), peripheral neuropathy, QT prolongation. Cardiac disorders: Tachycardia. Ear and labyrinth disorders: Vertigo, tinnitus. Eye disorders: Increased lacrimation, conjunctivitis. Gastrointestinal disorders: Nausea, constipation, diarrhoea, vomiting, abdominal pain, stomatitis, dyspepsia, dysgeusia, dry mouth, GERD, abdominal distension, oral candidiasis, oral herpes. General disorders and administration site conditions: Fatigue, lethargy, pyrexia, mucosal inflammation, peripheral oedema, pain, chills. Investigations: Increased AST, ALT or gamma-glutamyl transferase; decreased weight. Metabolism and nutrition disorders: Decreased appetite, hypokalaemia, hypomagnesaemia, dehydration, hypocalcaemia, hyperglycaemia, hypophosphataemia, hyperbilirubinaemia. Musculoskeletal and connective tissue disorders: Arthralgia, myalgia, back pain, pain in extremity, bone pain, muscle spasms, musculoskeletal pain, muscular weakness. Nervous system disorders: Headache, dizziness, hypoaesthesia, neurotoxicity. Psychiatric disorders: Insomnia, depression. Renal and urinary disorders: Dysuria, UTI. Respiratory, thoracic and mediastinal disorders: Dyspnoea, cough, oropharyngeal pain, epistaxis, rhinorrhoea, pneumonia, upper respiratory tract infection, nasopharyngitis, rhinitis, pulmonary embolism. Skin and subcutaneous tissue disorders: Alopecia, rash, pruritus, nail disorder, night sweats, dry skin, erythema, hyperhidrosis, palmar-plantar erythrodysaesthesia. Vascular disorders: Hot flush. Potentially Fatal: Febrile neutropenia, neutropenic sepsis, sepsis and septic shock.
This drug may cause tiredness or dizziness, if affected, do not drive or operate machinery.
Monitoring Parameters
Obtain CBC with differential and evaluate for signs of peripheral neuropathy prior to each dose. Monitor renal function, LFTs, electrolytes (including K and Mg); ECG in patients with predisposition to QT prolongation.
Drug Interactions
May increase risk of QT prolongation with drugs that prolong QT interval (e.g. antiarrhythmics).
Action
Description: Mechanism of Action: Eribulin, a microtubule dynamics inhibitor, is a synthetic analogue of halichondrin B. It inhibits the growth phase of microtubules via tubulin-based antimitotic mechanism which leads to G2/M cell-cycle block, disruption of mitotic spindle formation and subsequent apoptotic cell death. Pharmacokinetics: Distribution: Rapidly distributed. Volume of distribution: 43-114 L/m2. Plasma protein binding: 49-65%. Metabolism: Negligible. Excretion: Mainly via faeces (approx 82%, approx 88% as unchanged drug); urine (9%, approx 91% as unchanged drug). Elimination half-life: Approx 40 hours.
Chemical Structure
Eribulin Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 11354606, Eribulin. https://pubchem.ncbi.nlm.nih.gov/compound/11354606. Accessed July 28, 2022.
Storage
Store below 25°C. Do not freeze. This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
L01XX41 - eribulin ; Belongs to the class of other antineoplastic agents. Used in the treatment of cancer.
References
Anon. Eribulin (Briggs Drugs in Pregnancy and Lactation). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 19/07/2022.Anon. Eribulin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/06/2022.Buckingham R (ed). Eribulin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/06/2022.Halaven 0.44 mg/mL Solution for Injection (Eisai Europe Limited). MHRA. https://products.mhra.gov.uk. Accessed 01/06/2022.Halaven 0.5 mg/mL Solution for Injection (Eisai Malaysia Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 01/06/2022.Halaven Injection (Eisai Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 01/06/2022.Joint Formulary Committee. Eribulin. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/06/2022.
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