Eribulin Mesylate
- Atc Codes:L01XX41
- CAS Codes:253128-41-5
- PHARMGKB ID:253128-41-5
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
North America
USA: Halaven.
Drug combinations
Chemistry
Eribulin Mesylate: C~40~H~59~NO~11~ CH~4~O~3~S. Mw: 826.0 (729.9 for free base). 11,15:18,21:24,28-Triepoxy-7,9-ethano-12,15-methano-9H,15H-furo[3,2-i]furo[2′,3′:5,6]pyrano[4,3-b][1,4]dioxacyclopentacosin-5(4H)-one, 2-[(2S)-3-amino-2-hydroxypropyl]hexacosahydro-3-methoxy-26-methyl-20,27-bis(methylene)-, (2R,3R,3aS,7R,8aS,9S,10aR,11S,12R,13aR,13bS,15S,18S,21S,24S,26R,28R,29aS)-, methanesulfonate (salt). CAS-253128-41-5.
Pharmacologic Category
Other Antineoplastic Agents. Microtubule Dynamics Inhibitor. Analog of Halichondrin B (a product isolated from the marine sponge Halichondria okadai). (ATC-Code: L01XX41).
Mechanism of action
Eribulin inhibits the growth phase of microtubules without affecting the shortening phase, and sequesters tubulin into nonproductive aggregates. It 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.
Therapeutic use
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.
Pregnancy and lactiation implications
Fetal harm can occur when administered to a pregnant woman. Discontinue drug or nursing, taking into consideration importance of drug to mother.
Unlabeled use
Contraindications
None known to date.
Warnings and precautions
Severe neutropenia occurs (monitor peripheral blood cell counts and adjust dose as appropriate). Peripheral neuropathy is the most common toxicity leading to discontinuation of treatment (monitor for signs of neuropathy and manage with dose delay or adjustment). QT prolongation has been observed (ECG monitor for prolonged QT intervals in patients with congestive heart failure, bradyarrhythmias, drugs known to prolong the QT interval, and electrolyte abnormalities, and avoid in patients with congenital long QT syndrome).