1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Microtubule/Tubulin

Eribulin mesylate (Synonyms: B1939 mesylate; E7389 mesylate; ER-086526 mesylate)

Cat. No.: HY-13442A
Handling Instructions

Eribulin Mesylate (E7389 Mesylate), a synthetic analogue of halichondrin B in phase III clinical trials for breast cancer, binds to tubulin and microtubules.

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Eribulin mesylate Chemical Structure

Eribulin mesylate Chemical Structure

CAS No. : 441045-17-6

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Description

Eribulin Mesylate (E7389 Mesylate), a synthetic analogue of halichondrin B in phase III clinical trials for breast cancer, binds to tubulin and microtubules. Target: Microtubule/Tubulin Eribulin suppressed centromere dynamics at concentrations that arrest mitosis. At 60 nmol/L eribulin (2 x mitotic IC(50)), the relaxation rate was suppressed 21%, the time spent paused increased 67%, and dynamicity decreased 35% (but without reduction in mean centromere separation), indicating that eribulin decreased normal microtubule-dependent spindle tension at the kinetochores, preventing the signal for mitotic checkpoint passage [1]. [(3)H]eribulin binds soluble tubulin at a single site; however, this binding is complex with an overall K(d) of 46 microM, but also showing a real or apparent very high affinity (K(d) = 0.4 microM) for a subset of 25% of the tubulin. Eribulin also binds microtubules with a maximum stoichiometry of 14.7 +/- 1.3 molecules per microtubule (K(d) = 3.5 microM), strongly suggesting the presence of a relatively high-affinity binding site at microtubule ends. At 100 nM, the concentration that inhibits microtubule plus end growth by 50%, we found that one molecule of eribulin is bound per two microtubules, indicating that the binding of a single eribulin molecule at a microtubule end can potently inhibit its growth. Eribulin does not suppress dynamic instability at microtubule minus ends [2]. Eribulin's in vivo superiority derives from its ability to induce irreversible mitotic blockade, which appears related to persistent drug retention and sustained Bcl-2 phosphorylation [3].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT03207672 Eisai Co., Ltd.|Eisai Inc. Solid Tumor September 1, 2017 Phase 1
NCT01945710 Eisai Limited|Eisai Inc. Solid Tumors December 2012 Phase 1
NCT00069264 Eisai Inc. Advanced Solid Tumors September 2003 Phase 1
NCT00097721 Eisai Inc. Breast Neoplasms September 2004 Phase 2
NCT00326950 Eisai Co., Ltd.|Eisai Inc. Cancer June 2006 Phase 1
NCT00268905 Eisai Inc. Cancer October 2006 Phase 1
NCT00706095 Eisai Inc. Cancer February 2008 Phase 1
NCT00100932 Eisai Inc. Non-Small-Cell Lung Carcinoma December 2004 Phase 2
NCT01418677 Eisai Inc. Unspecified Adult Solid Tumor, Protocol Specific October 2011 Phase 1
NCT01126736 Eisai Inc.|Quintiles, Inc. Non Small Cell Lung Cancer March 2010 Phase 1|Phase 2
NCT00246090 Eisai Inc.|Eisai Limited Breast Cancer October 2005 Phase 2
NCT00069277 Eisai Inc. Cancer August 2003 Phase 1
NCT00413192 Eisai Inc. Soft Tissue Sarcoma January 2007 Phase 2
NCT00278993 Eisai Inc. Prostate Cancer January 2006 Phase 2
NCT00388726 Eisai Inc.|Eisai Limited Breast Cancer October 2006 Phase 3
NCT01432886 Eisai Co., Ltd.|Eisai Inc. Breast Cancer October 2011 Phase 1
NCT02225470 Eisai Co., Ltd.|Eisai Inc. HER2-Negative Breast Cancer|Triple Negative Breast Cancer|Breast Cancer|Cancer of Breast|Breast Tumors September 2013 Phase 3
NCT01126749 Eisai Inc.|PharmaBio Development Inc. Bladder Cancer April 2010 Phase 1|Phase 2
NCT02082626 University of Oklahoma Pediatric Cancer|Solid Tumors|Lymphoma February 1, 2014 Phase 1
NCT01669252 SOLTI Breast Cancer Research Group|Eisai Inc. Breast Cancer August 2012 Phase 2
NCT02640508 Virginia G. Kaklamani|Eisai Inc.|The University of Texas Health Science Center at San Antonio Cancer|Solid Tumor May 2016 Phase 2
NCT03222856 MedSIR Breast Cancer October 1, 2017 Phase 2
NCT01596751 Hope Rugo, MD|Susan G. Komen Breast Cancer Foundation|Plexxikon|University of California, San Francisco Metastatic Breast Cancer July 2012 Phase 1|Phase 2
NCT02481050 Eisai Inc. Breast Cancer June 16, 2015 Phase 2
NCT01328249 Eisai Inc. Her2normal March 2, 2011 Phase 2
NCT02864030 Oncologia Medica dell'Ospedale Fatebenefratelli|Mario Negri Institute for Pharmacological Research Metastatic Breast Cancer|Toxicity|Neurotoxicity|Drug Toxicity|Adverse Drug Event May 2014 Phase 4
NCT02404506 Swiss Group for Clinical Cancer Research Breast Cancer|Adenocarcinoma August 2015 Phase 2
NCT00908908 Eisai Inc. Advanced Solid Tumors March 2009 Phase 1
NCT03002493 Eisai Limited|Eisai Inc. Tumor December 2009 Phase 1
NCT01458249 Eisai Co., Ltd.|Eisai Inc. Soft Tissue Sarcoma November 2011 Phase 2
NCT03027245 Eisai GmbH|Eisai Inc. Locally Advanced or Metastatic Breast Cancer August 2016
NCT02318589 Tom Badgett|University of Kentucky Solid Tumor August 2015 Phase 1
NCT01000376 Eisai Limited|Eisai Inc. Cancer February 2009 Phase 1
NCT03202316 M.D. Anderson Cancer Center|Genentech, Inc. Malignant Neoplasm of Breast August 2017 Phase 2
NCT00334893 National Cancer Institute (NCI) Fallopian Tube Cancer|Primary Peritoneal Cavity Cancer|Recurrent Ovarian Epithelial Cancer April 2006 Phase 2
NCT01439282 Eisai Inc. Estrogen Receptor Positive Tumor|Breast Cancer August 2011 Phase 2
NCT02723877 PIQUR Therapeutics AG|Hospital Universitario Ramon y Cajal|Hospital Universitari Vall d'Hebron Research Institute|Institut Català d'Oncologia|Churchill Hospital|Barts Cancer Institute|Fundación Instituto Valenciano de Oncología Metastatic Breast Cancer April 2016 Phase 1|Phase 2
NCT00337077 National Cancer Institute (NCI) Adenocarcinoma of the Prostate|Hormone-refractory Prostate Cancer|Recurrent Prostate Cancer|Stage IV Prostate Cancer November 2006 Phase 2
NCT02753595 Eisai Inc.|Halozyme Therapeutics Metastatic Breast Cancer July 13, 2016 Phase 1|Phase 2
NCT02596503 University of Colorado, Denver|University of Kentucky Relapsed Solid Tumors|Refractory Solid Tumors October 2015 Phase 1
NCT02097238 National Cancer Institute (NCI) Recurrent Osteosarcoma August 2014 Phase 2
NCT02513472 Eisai Inc.|Merck Sharp & Dohme Corp. Breast Cancer August 28, 2015 Phase 1|Phase 2
NCT01554371 University of California, San Francisco|Eisai Inc. Malignant Solid Tumour|Breast Cancer Nos Metastatic Recurrent|Neuropathy March 2012 Phase 1|Phase 2
NCT01676818 University of Southern California|National Cancer Institute (NCI) Recurrent Cervical Cancer|Stage IIIA Cervical Cancer|Stage IIIB Cervical Cancer|Stage IVA Cervical Cancer|Stage IVB Cervical Cancer August 9, 2012 Phase 2
NCT02581839 Case Comprehensive Cancer Center Metastatic Breast Cancer|Brain Metastases November 17, 2015 Phase 2
NCT02014337 Corcept Therapeutics Breast Cancer|Ovarian Epithelial Cancer Recurrent|Sarcoma|Non-small Cell Lung Cancer|Carcinoma, Transitional Cell|Prostate Cancer|Prostatic Neoplasms January 2014 Phase 1
NCT01613768 University of Washington|National Cancer Institute (NCI) Recurrent Salivary Gland Cancer|Stage IVA Salivary Gland Cancer|Stage IVB Salivary Gland Cancer|Stage IVC Salivary Gland Cancer May 8, 2012 Phase 2
NCT01463891 Eisai Co., Ltd.|Eisai Inc. Inoperable or Recurrent Breast Cancer July 2011
NCT01961544 Eisai Korea Inc.|Eisai Inc. Breast Neoplasms|Breast Cancer June 2013 Phase 4
NCT02396433 The University of Texas Health Science Center at San Antonio Cancer of the Breast April 2015 Phase 1|Phase 2
NCT01142661 Eisai Inc. Breast Cancer August 2010
NCT01388647 Vector Oncology|Eisai Inc. HER-2 Positive Breast Cancer August 2011 Phase 1|Phase 2
NCT02171260 Eisai Inc. Pediatrics|Solid Tumors July 2014 Phase 1
NCT01795586 H. Lee Moffitt Cancer Center and Research Institute|Eisai Inc. Breast Cancer February 6, 2013 Phase 1
NCT02338037 City of Hope Medical Center|National Cancer Institute (NCI)|Eisai Inc. Metastatic Malignant Neoplasm in the Adult Brain|Primary Brain Tumor May 19, 2015
NCT01106248 Eisai Limited|Eisai Inc. Advanced Solid Tumor March 2009 Phase 1
NCT00965523 Eisai Co., Ltd.|Eisai Inc. Breast Cancer January 2008 Phase 2
NCT01827787 Dana-Farber Cancer Institute Breast Cancer June 2013 Phase 2
NCT01912963 Dana-Farber Cancer Institute|Eisai Inc.|Genentech, Inc. HER-2 Positive Breast Cancer August 2013 Phase 2
NCT00337129 National Cancer Institute (NCI) Head and Neck Cancer May 2006 Phase 2
NCT01104155 Eisai Inc. Non-small Cell Lung Cancer February 22, 2010 Phase 2
NCT03032614 The University of Texas Health Science Center at San Antonio Breast Cancer Stage IV|Ovarian Cancer|BRCA1 Mutation|BRCA2 Mutation July 31, 2017 Phase 2
NCT01908101 University of Washington|National Cancer Institute (NCI) Recurrent Breast Carcinoma|Stage IV Breast Cancer January 8, 2014 Phase 2
NCT01705691 NSABP Foundation Inc|Eisai Inc. Breast Cancer|HER2-negative Breast Cancer September 2012 Phase 2
NCT00383760 National Cancer Institute (NCI) Adenocarcinoma of the Pancreas|Pancreatic Cancer|Recurrent Pancreatic Cancer|Stage II Pancreatic Cancer|Stage III Pancreatic Cancer|Stage IV Pancreatic Cancer August 2006 Phase 2
NCT03051659 Dana-Farber Cancer Institute|Merck Sharp & Dohme Corp. Breast Cancer March 22, 2017 Phase 2
NCT02681523 Imperial College London Breast Cancer October 2015 Phase 2
NCT00879086 Eisai Inc. Breast Cancer March 2009 Phase 2
NCT00047034 National Cancer Institute (NCI) Unspecified Adult Solid Tumor, Protocol Specific August 2002 Phase 1
NCT01527487 SCRI Development Innovations, LLC|Eisai Inc. HER2 Negative Breast Cancer June 2012 Phase 2
NCT02623972 Dana-Farber Cancer Institute|Eisai Inc. Inflammatory Breast Cancer|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast December 2015 Phase 2
NCT00365157 National Cancer Institute (NCI) Metastatic Urothelial Carcinoma|Recurrent Urothelial Carcinoma of the Renal Pelvis and Ureter|Stage III Bladder Cancer|Stage III Urethral Cancer|Stage IV Bladder Cancer|Stage IV Urethral Cancer October 23, 2006 Phase 1|Phase 2
NCT02178241 National Cancer Institute (NCI) Metastatic Ureteral Neoplasm|Metastatic Urethral Neoplasm|Stage III Bladder Urothelial Carcinoma|Stage III Ureter Cancer|Stage III Urethral Cancer|Stage IV Bladder Urothelial Carcinoma|Stage IV Ureter Cancer|Stage IV Urethral Cancer|Ureter Urothelial Carcinoma|Urethral Urothelial Carcinoma December 11, 2014 Phase 2
NCT01534455 German Breast Group Metastatic Breast Cancer February 2012 Phase 2
NCT02175446 Consorzio Oncotech|Clinical Research Technology S.r.l. Metastatic Breast Cancer|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast September 2014 Phase 2
NCT02616848 Istituti Ospitalieri di Cremona Triple Negative Breast Cancer November 2015 Phase 1
NCT01585870 Bayer|Onyx Therapeutics, Inc. Neoplasms July 2012 Phase 1
NCT01401959 SCRI Development Innovations, LLC|Eisai Inc. Metastatic Breast Cancer September 23, 2011 Phase 2
NCT02824575 Montefiore Medical Center|Deciphera Pharmaceuticals LLC|Albert Einstein College of Medicine, Inc. Breast Cancer|Breast Adenocarcinoma|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast|Recurrent Breast Carcinoma|Stage IV Breast Cancer July 2016 Phase 1
NCT01498588 Emory University|Eisai Inc. Breast Neoplasms|Breast Cancer|Breast Tumors|Cancer of the Breast|Neoplasms, Breast|Tumors, Breast November 2011 Phase 2
NCT01268150 Eisai Inc. Locally Recurrent|Metastatic Breast Cancer ( HER2 Negative) February 2011 Phase 2
NCT01269346 Eisai Inc. Breast Cancer December 2010 Phase 2
NCT00410553 National Cancer Institute (NCI) Adult Solid Neoplasm|Recurrent Ovarian Carcinoma|Recurrent Uterine Corpus Carcinoma|Stage III Ovarian Cancer|Stage III Uterine Corpus Cancer|Stage IV Ovarian Cancer|Stage IV Uterine Corpus Cancer November 14, 2006 Phase 1
NCT02120469 City of Hope Medical Center|National Cancer Institute (NCI) Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor-negative|Stage IV Breast Cancer|Triple-negative Breast Carcinoma October 1, 2014 Phase 1
NCT02263495 Asan Medical Center|Eisai Inc.|Dong-A ST Co., Ltd.|Samyang Biopharmaceuticals Corporation Metastatic Breast Cancer November 2014 Phase 2
NCT01427933 Eli Lilly and Company Breast Cancer November 2011 Phase 2
NCT02551263 Translational Research Informatics Center, Kobe, Hyogo, Japan|Kyoto Breast Cancer Research Network Breast Cancer July 2015
NCT01941407 ARCAGY/ GINECO GROUP Metastatic Breast Cancer November 2013 Phase 2
NCT01323530 Eisai Limited|Eisai Inc. Metastatic Breast Cancer January 2010 Phase 1|Phase 2
NCT02061085 MedSIR Breast Neoplasm|Metastasis July 2013 Phase 2
NCT01327885 Eisai Inc. Soft Tissue Sarcoma March 2011 Phase 3
NCT01240421 Eisai Inc. Metastatic Breast Cancer March 2011
NCT02037529 Academic and Community Cancer Research United Metastatic Breast Cancer|Locally Recurrent Breast Cancer March 2014 Phase 3
NCT03058406 Eisai Co., Ltd.|Eisai Inc. Sarcoma, Soft Tissue March 1, 2016
NCT00400829 National Cancer Institute (NCI) Recurrent Non-small Cell Lung Cancer|Stage IIIB Non-small Cell Lung Cancer|Stage IV Non-small Cell Lung Cancer November 2006 Phase 2
NCT01372579 Northwestern University|Eisai Inc. Estrogen Receptor-negative Breast Cancer|HER2-negative Breast Cancer|Male Breast Cancer|Progesterone Receptor-negative Breast Cancer|Stage IA Breast Cancer|Stage IB Breast Cancer|Stage II Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Triple-negative Breast Cancer August 2011 Phase 2
NCT01593020 M.D. Anderson Cancer Center|Eisai Inc. Breast Cancer August 2012 Phase 2
NCT02215876 Sidney Kimmel Comprehensive Cancer Center Breast Cancer September 2014 Phase 2
NCT02393287 Institut Cancerologie de l'Ouest Metastatic Breast Cancer November 2014
NCT00415324 National Cancer Institute (NCI) Unspecified Adult Solid Tumor, Protocol Specific December 2006 Phase 1
NCT02841722 Centre Georges Francois Leclerc Breast Cancer December 3, 2015
NCT01454934 Eisai Inc. Non-Small Cell Lung Cancer (NSCLC) September 2011 Phase 3
NCT00337103 Eisai Inc. Metastatic Breast Cancer June 2006 Phase 3
NCT02035813 Prof. W. Janni|University of Ulm HER2-negative Und Hormone-receptor Positive Metastatic Breast Cancer|HER2-negative Circulating Tumor Cells|Postmenopausal Female Patients January 2014 Phase 2
NCT02555657 Merck Sharp & Dohme Corp. Metastatic Triple Negative Breast Cancer October 13, 2015 Phase 3
NCT02000596 Katherine Tkaczuk|Genentech, Inc.|University of Maryland Metastatic Breast Cancer January 2014 Phase 2
NCT02574455 Immunomedics, Inc. Breast Cancer March 31, 2017 Phase 3
NCT02492711 MacroGenics HER-2 Positive Breast Cancer|Metastatic Neoplasm July 2015 Phase 3
NCT02514681 Japan Breast Cancer Research Group|Chugai Pharmaceutical HER2-positive Locally Advanced or Metastatic Breast Cancer October 2015 Phase 3
NCT02419495 M.D. Anderson Cancer Center|Karyopharm Therapeutics Inc Advanced Cancers June 26, 2015 Phase 1
NCT02915744 Nektar Therapeutics Metastasis|Breast Cancer November 2016 Phase 3
NCT01698281 AEterna Zentaris Breast Cancer December 2012 Phase 2
NCT02299999 UNICANCER|Fondation ARC|AstraZeneca Metastatic Breast Cancer April 7, 2014 Phase 2
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References
M.Wt

826.0

Formula

C₄₁H₆₃NO₁₄S

CAS No.

441045-17-6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Eribulin mesylate
Cat. No.:
HY-13442A
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