Eribulin Mesylate
- CAS No.
- 441045-17-6
- Chemical Name:
- Eribulin Mesylate
- Synonyms
- Halaven;Eribulin Mesilate;E7389 mesylate;B1939 mesylate;Ibrine mesylate;Ezebrine mesylate;Eribulin Mesylate;Irebulin mesylate;ER-086526 mesylate;Eribulin Mesylate (E7389)
- CBNumber:
- CB32563308
- Molecular Formula:
- C41H63NO14S
- Molecular Weight:
- 826.01
- MOL File:
- 441045-17-6.mol
- Modify Date:
- 2024/7/2 8:55:06
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P280-P301+P312-P302+P352-P305+P351+P338 |
Eribulin Mesylate Chemical Properties,Uses,Production
Uses
Eribulin Mesylate is a synthetic analog of the marine natural product halichondrin B.
Definition
ChEBI: Eribulin mesylate is a methanesulfonate salt obtained by reaction of eribulin with one equivalent of methanesulfonic acid. A fully synthetic macrocyclic ketone analogue of marine sponge natural products. Inhibits growth phase of microtubules via tubulin-based antimitotic mechanism, which leads to G2/M cell-cycle block, disruption of mitotic spindles, and, ultimately, apoptotic cell death after prolonged mitotic blockage. It has a role as an antineoplastic agent and a microtubule-destabilising agent. It contains an eribulin(1+).
Clinical Use
Eribulin is a highly potent cytotoxic agent approved in the U.S. for the treatment of metastatic breast cancer for patients who have received at least two previous chemotherapeutic regimens. Eribulin was discovered and developed by Eisai and it is currently undergoing clinical evaluation for the treatment of sarcoma (PhIII) and non-small cell lung cancer which shows progression after platinumbased chemotherapy and for the treatment of prostate cancer (PhII). Early stage clinical trials are also underway to evaluate eribulin’s efficacy against a number of additional cancers. Eribulin is a structural analog of the marine natural product halichondrin B. Its mechanism of action involves the disruption of mitotic spindle formation and inhibition of tubulin polymerization which results in the induction of cell cycle blockade in the G2/M phase and apoptosis.
Clinical Use
Eribulin mesylate, a nontaxane, completely synthetic microtubule inhibitor, has recently been approved by the U.S. Food and Drug Administration as third-line treatment of metastatic breast cancer refractory to anthracyclines and taxanes.
Side effects
Eribulin Mesylate (Halaven) may cause serious side effects including:hives; difficulty breathing; swelling of your face, lips, tongue, or throat; chest pain; severe dizziness; fast or pounding heartbeats, numbness, tingling, or burning pain in your hands or feet; pain or burning when you urinate; confusion; uneven heart rate; extreme thirst; increased urination; leg discomfort; muscle weakness; limp feeling; fever; chill; painful mouth sores; pain when swallowing; cough; trouble breathing; pale skin; easy bruising; sore throat; skin pain followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.
Toxicology
Peripheral neuropathy was the most common toxicity leading to discontinuation of eribulin (5 percent). Single doses of 0.75 mg/kg were lethal to rats and two doses of 0.075 mg/kg were lethal to dogs. The no-observed-adverse-effect level (NOAEL) in rats and dogs were 0.015 and 0.0045 mg/kg/day, respectively.
Mode of action
Eribulin Mesylate is the mesylate salt of a synthetic analogue of halichondrin B, a substance derived from a marine sponge (Lissodendoryx sp.) with antineoplastic activity. Eribulin binds to the vinca domain of tubulin and inhibits the polymerization of tubulin and the assembly of microtubules, resulting in inhibition of mitotic spindle assembly, induction of cell cycle arrest at G2/M phase, and, potentially, tumor regression.
References
Eribulin mesylate: a novel halichondrin B analogue for the treatment of metastatic breast cancer DOI: 10.2146/ajhp110237
From micrograms to grams: scale-up synthesis of eribulin mesylate DOI: 10.1039/c3np70051h
Eribulin mesylate: mechanism of action of a unique microtubule-targeting agent DOI: 10.1158/1078-0432.CCR-14-3252
Eribulin Mesylate Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| BTC pharm India | +918790379245 | AndhraPradesh, India | 1269 | 58 | Inquiry |
| Aspen Biopharma Labs Pvt Ltd | +91-9248058660 +91-9248058662 | Telangana, India | 234 | 58 | Inquiry |
| Pharma Affiliates | 172-5066494 | Haryana, India | 6761 | 58 | Inquiry |
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6522 | 58 | Inquiry |
| Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
| AFINE CHEMICALS LIMITED | +86-0571-85134551 | China | 15395 | 58 | Inquiry |
| ChemExpress | +86-021-58950125 +86-021-58950125; | China | 598 | 58 | Inquiry |
| Hebei Yanxi Chemical Co., Ltd. | +8617531190177 | China | 5873 | 58 | Inquiry |
| Changzhou Rokechem Technology Co., Ltd. | 18758118018 | China | 255 | 58 | Inquiry |
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