Eribulin Mesylate is a synthetic analogue of halichondrin B and an antineoplastic active pharmaceutical ingredient (API). It is a microtubule dynamics inhibitor that binds to tubulin and suppresses microtubule growth, resulting in inhibition of cancer-cell proliferation.
Eribulin Mesylate is the mesylate salt of eribulin and is used in pharmaceutical formulations for the treatment of certain advanced or metastatic cancers.
Eribulin Mesylate is a synthetic small-molecule anticancer drug substance. It is structurally related to the natural marine-product compound halichondrin B and retains the pharmacologically active portion of that molecule.
The molecular formula of Eribulin Mesylate is C₄₀H₅₉NO₁₁·CH₄O₃S, and its molecular weight is approximately 826.00 g/mol. The CAS Registry Number is 441045-96-5.
Eribulin binds to tubulin and inhibits microtubule polymerization. Unlike taxanes, which primarily stabilize microtubules, eribulin suppresses microtubule growth without affecting depolymerization.
This results in:
Eribulin Mesylate is primarily associated with:
The FDA-approved product HALAVEN (eribulin mesylate) is indicated for specific patients with metastatic breast cancer and unresectable or metastatic liposarcoma.
Eribulin Mesylate is a synthetic small-molecule oncology API. Pharmaceutical-grade material requires appropriate control of identity, assay, related substances, water content, residual solvents and other applicable quality attributes.
Because Eribulin Mesylate is a complex synthetic molecule, its impurity profile and stereochemical integrity are particularly important during pharmaceutical manufacturing and quality control.
Eribulin Mesylate API intended for pharmaceutical manufacturing should comply with the applicable approved specification and relevant regulatory requirements.
Typical quality-control parameters may include:
A qualified supplier should provide appropriate Certificate of Analysis (CoA), specification sheet, SDS/MSDS, batch traceability and applicable regulatory documentation.
Eribulin Mesylate should be stored in a tightly closed container, protected from moisture, light and excessive heat, according to the approved specification and stability requirements.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 2.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 20 ppm |
| pH (1% Solution) | 2.0 – 4.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |
| Melting Point | 150°C – 154°C |