eribulinmesilate - CAS 441045-17-6
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C41H63NO14S
Molecular Weight:
826.008
COA:
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Targets:
Microtubule/Tubulin
Description:
Eribulinmesilate can inhibit experimental metastasis of breast cancer cells by reversing phenotype from epithelial-mesenchymal transition (EMT) to mesenchymal-epithelial transition (MET) states.
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Brife Description:
breast cancer
Synonyms:
Halaven
MSDS:
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Application:
the treatmnet of breast cancer
InChIKey:
QAMYWGZHLCQOOJ-LWLFVNJASA-N
InChI:
InChI=1S/C40H59NO11.CH4O3S/c1-19-11-24-5-7-28-20(2)12-26(45-28)9-10-40-17-33-36(51-40)37-38(50-33)39(52-40)35-29(49-37)8-6-25(47-35)13-22(42)14-27-31(16-30(46-24)21(19)3)48-32(34(27)44-4)15-23(43)18-41;1-5(2,3)4/h19,23-39,43H,2-3,5-18,41H2,1,4H3;1H3,(H,2,3,4)/t19-,23+,24+,25-,26+,27+,28+,29+,30-,31+,32-,33-,34-,35-,36-,37+,38-,39-,40+;/m1./s1
Canonical SMILES:
CC1CC2CCC3C(=C)CC(O3)CCC45CC6C(O4)C7C(O6)C(O5)C8C(O7)CCC(O8)CC(=O)CC9C(CC(C1=C)O2)OC(C9OC)CC(CN)O.CS(=O)(=O)O
Current Developer:
Eisai
1.Phase II clinical study of eribulin monotherapy in Japanese patients with metastatic breast cancer who had well-defined taxane resistance.
Inoue K1, Saito T2, Okubo K3, Kimizuka K4, Yamada H5, Sakurai T6, Ishizuna K7, Hata S8, Kai T9, Kurosumi M10. Breast Cancer Res Treat. 2016 Apr 28. [Epub ahead of print]
No clinical evidence on the efficacy and safety of eribulin monotherapy has been obtained by a prospective clinical study in patients with metastatic breast cancer (MBC) who had well-defined taxane resistance. The present Phase II, multicenter, single-arm, open-label study aimed to obtain the evidence. Japanese female patients, aged 33-74 years who had the metastasis of taxane-resistant and histopathologically confirmed breast cancer, received eribulin mesylate 1.4 mg/m2 (equivalent to eribulin 1.23 mg/m2 [expressed as free base]) as a 2- to 5-min intravenous infusion on days 1 and 8 of each 21-day cycle. The primary endpoint was the clinical benefit rate (CBR) [complete response (CR), partial response (PR), and long-term stable disease (LSD) ≥24 weeks]. A total of 51 patients underwent chemotherapy cycles (median 4; range 1-42 cycles). The CBR was 39.2 % (CR 2.0 %; PR 23.5 %; and LSD 13.7 %), and the rate of progressive disease was 49.0 %.
2.Phase II clinical study of eribulin monotherapy in Japanese patients with metastatic breast cancer who had well-defined taxane resistance.
Inoue K1, Saito T2, Okubo K3, Kimizuka K4, Yamada H5, Sakurai T6, Ishizuna K7, Hata S8, Kai T9, Kurosumi M10. Breast Cancer Res Treat. 2016 Apr 28. [Epub ahead of print]
No clinical evidence on the efficacy and safety of eribulin monotherapy has been obtained by a prospective clinical study in patients with metastatic breast cancer (MBC) who had well-defined taxane resistance. The present Phase II, multicenter, single-arm, open-label study aimed to obtain the evidence. Japanese female patients, aged 33-74 years who had the metastasis of taxane-resistant and histopathologically confirmed breast cancer, received eribulin mesylate 1.4 mg/m2 (equivalent to eribulin 1.23 mg/m2 [expressed as free base]) as a 2- to 5-min intravenous infusion on days 1 and 8 of each 21-day cycle. The primary endpoint was the clinical benefit rate (CBR) [complete response (CR), partial response (PR), and long-term stable disease (LSD) ≥24 weeks]. A total of 51 patients underwent chemotherapy cycles (median 4; range 1-42 cycles). The CBR was 39.2 % (CR 2.0 %; PR 23.5 %; and LSD 13.7 %), and the rate of progressive disease was 49.0 %.
3.Antimitotic and Non-mitotic Effects of Eribulin Mesilate in Soft Tissue Sarcoma.
Kawano S1, Asano M1, Adachi Y1, Matsui J2. Anticancer Res. 2016 Apr;36(4):1553-61.
BACKGROUND: Eribulin mesilate (eribulin), a first-in-class halichondrin B-based microtubule dynamics inhibitor, has been shown to promote vascular remodeling and reversal of epithelial-mesenchymal transition (EMT) apart from its antimitotic activity in breast cancer models.
4.Results of the Belgian expanded access program of eribulin in the treatment of metastatic breast cancer closely mirror those of the pivotal phase III trial.
Aftimos P1, Polastro L2, Ameye L3, Jungels C2, Vakili J2, Paesmans M3, van den Eerenbeemt J2, Buttice A2, Gombos A2, de Valeriola D2, Gil T2, Piccart-Gebhart M2, Awada A2. Eur J Cancer. 2016 Apr 20;60:117-124. doi: 10.1016/j.ejca.2016.03.010. [Epub ahead of print]
BACKGROUND: Eribulin is a non-taxane microtubule dynamics inhibitor that showed a survival benefit versus treatment of physician's choice in a phase III trial enrolling patients with metastatic breast cancer (MBC).
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CAS 441045-17-6 eribulinmesilate

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