Eribulin

drug
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Also known as B-1939E-7389 FREE BASEER-086526EribulinaEribuline

Summary

Eribulin (CHEMBL1683590) is an approved small-molecule antineoplastic agent (ATC L01XX41) targeting TUBB; indicated across 15 conditions including neoplasm and breast carcinoma; with CIViC clinical evidence for 1 variant-indication association (e.g. CDK2 CYTOPLASMIC EXPRESSION in triple-receptor negative breast cancer).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L01XX41
  • Targets: 1 (TUBB)
  • Indications: 15 conditions
  • Clinical trials: 107
  • Precision-oncology evidence (CIViC): 1 variant–indication association
  • Chemistry: 729.9 Da · C40H59NO11

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1683590
NameEribulin
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID11354606
ChEBICHEBI:63587
ATCL01XX41
Molecular formulaC40H59NO11
Molecular weight729.9
InChIKeyUFNVPOGXISZXJD-JBQZKEIOSA-N

SMILES: C[C@@H]1C[C@@H]2CC[C@H]3C(=C)C[C@@H](O3)CC[C@]45C[C@@H]6[C@H](O4)[C@H]7[C@@H](O6)[C@@H](O5)[C@@H]8[C@@H](O7)CC[C@@H](O8)CC(=O)C[C@H]9[C@H](C[C@H](C1=C)O2)O[C@@H]([C@@H]9OC)C[C@@H](CN)O

IUPAC name: (1S,3S,6S,9S,12S,14R,16R,18S,20R,21R,22S,26R,29S,31R,32S,33R,35R,36S)-20-[(2S)-3-amino-2-hydroxypropyl]-21-methoxy-14-methyl-8,15-dimethylidene-2,19,30,34,37,39,40,41-octaoxanonacyclo[24.9.2.13,32.13,33.16,9.112,16.018,22.029,36.031,35]hentetracontan-24-one

ChEBI definition: 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

Pharmacological roles (ChEBI): antineoplastic agent, microtubule-destabilising agent.

Also known as: B-1939, E-7389 FREE BASE, ER-086526, Eribulin, Eribulina, Eribuline, eribulin, ERIBULIN

Parent form; salt/anhydrous children: CHEMBL1683544, CHEMBL3526882

Patent coverage: 2,319 distinct patent families (5,581 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
TUBBtubulin beta class IInhibition8.23P07437

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 1 target gene(s): TUBB.

Top Reactome pathways

24 total, by targets touching each:

PathwayTargetsGenes
Cell Cycle1TUBB
Disease1TUBB
Innate Immune System1TUBB
Immune System1TUBB
Organelle biogenesis and maintenance1TUBB
Regulation of PLK1 Activity at G2/M Transition1TUBB
Loss of Nlp from mitotic centrosomes1TUBB
Recruitment of mitotic centrosome proteins and complexes1TUBB
Loss of proteins required for interphase microtubule organization from the centrosome1TUBB
Centrosome maturation1TUBB
Recruitment of NuMA to mitotic centrosomes1TUBB
Mitotic G2-G2/M phases1TUBB
Cilium Assembly1TUBB
Anchoring of the basal body to the plasma membrane1TUBB
Infectious disease1TUBB
Neutrophil degranulation1TUBB
Mitotic Prometaphase1TUBB
M Phase1TUBB
G2/M Transition1TUBB
Cell Cycle, Mitotic1TUBB
AURKA Activation by TPX21TUBB
Potential therapeutics for SARS1TUBB
SARS-CoV Infections1TUBB
Viral Infection Pathways1TUBB

Dominant GO biological processes

GO termTargets
microtubule cytoskeleton organization1
mitotic cell cycle1
microtubule-based process1
cytoskeleton-dependent intracellular transport1
natural killer cell mediated cytotoxicity1
regulation of synapse organization1
spindle assembly1
cell division1
odontoblast differentiation1
cytoskeleton organization1

Indications & clinical

Indications

15 indications (2 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
neoplasm4MONDO:0005070EFO:0000616
breast carcinoma3MONDO:0004989EFO:0000305
non-small cell lung carcinoma3MONDO:0005233EFO:0003060
sarcoma3MONDO:0005089EFO:0000691
breast neoplasm3MONDO:0021100MONDO:0007254
triple-negative breast carcinoma3MONDO:0005494EFO:0005537
angiosarcoma2MONDO:0016982EFO:0003968
inflammatory breast carcinoma2MONDO:0006804EFO:1000984
hereditary breast ovarian cancer syndrome2MONDO:0003582Orphanet:145
epithelioid hemangioendothelioma2MONDO:0015523MONDO:0015523
solitary fibrous tumor2MONDO:0016238MONDO:0016238
ovarian carcinoma1MONDO:0005140EFO:0001075
metastatic melanoma1MONDO:0005191EFO:0002617
fallopian tube carcinoma1MONDO:0006206EFO:1000251

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 107.

Phase distribution

PhaseTrials
PHASE251
PHASE328
PHASE111
PHASE1/PHASE210
Not specified6
EARLY_PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT02344472PHASE3ACTIVE_NOT_RECRUITINGDetect V / CHEVENDO (Chemo vs. Endo)
NCT03734029PHASE3ACTIVE_NOT_RECRUITINGTrastuzumab Deruxtecan (DS-8201a) Versus Investigator’s Choice for HER2-low Breast Cancer That Has Spread or Cannot be Surgically Removed [DESTINY-Breast04]
NCT05063786PHASE3ACTIVE_NOT_RECRUITINGTrastuzumab + Alpelisib +/- Fulvestrant vs Trastuzumab + CT in Patients With PIK3CA Mutated Previously Treated HER2+ Advanced BrEasT Cancer (ALPHABET)
NCT05104866PHASE3ACTIVE_NOT_RECRUITINGA Phase-3, Open-Label, Randomized Study of Dato-DXd Versus Investigator’s Choice of Chemotherapy (ICC) in Participants With Inoperable or Metastatic HR-Positive, HER2-Negative Breast Cancer Who Have Been Treated With One or Two Prior Lines of Systemic Chemotherapy (TROPION-Breast01)
NCT05814354PHASE3RECRUITINGSHR-A1811 Versus Investigator’s Chemotherapy in Recurrent/Metastatic Breast Cancer Clinical Trial
NCT06081959PHASE3RECRUITINGStudy of SKB264 for Locally Advanced, Recurrent or Metastatic HR+/HER2- Breast Cancer
NCT06263231PHASE3ACTIVE_NOT_RECRUITINGA Study to Investigate Efficacy & Safety of Intratumoral INT230-6 Compared to US Standard of Care in Adults With Soft Tissue Sarcomas (INVINCIBLE-3)
NCT06268652PHASE3RECRUITINGPatient Derived Organoid-guided Personalized Treatment Versus Treatment of Physician’s Choice in Breast Cancer
NCT06279364PHASE3RECRUITINGA Study of SKB264 Versus Investigator’s Choice Chemotherapy in Patients With Unresectable Recurrent or Metastatic Triple-Negative Breast Cancer
NCT06343948PHASE3ACTIVE_NOT_RECRUITINGA Study Comparing BL-B01D1 With Chemotherapy of Physician’s Choice in Patients With Unresectable Locally Advanced, Recurrent, or Metastatic HR+HER2- Breast Cancer(PANKU-Breast01)
NCT06382142PHASE3ACTIVE_NOT_RECRUITINGA Study Comparing BL-B01D1 With Chemotherapy of Physician’s Choice in Patients With Unresectable Locally Advanced or Metastatic Triple-Negative Breast Cancer(PANKU-Breast02)
NCT06383767PHASE3RECRUITINGA Phase III Study of ESG401 for Locally Advanced or Metastatic HR+/HER2- Breast Cancer
NCT06435429PHASE3RECRUITINGA Study Comparing the Efficacy and Safety of Zanidatamab to Trastuzumab, Each in Combination With Physician’s Choice Chemotherapy, for the Treatment of Participants With Metastatic HER2-positive Breast Cancer
NCT06519370PHASE3ACTIVE_NOT_RECRUITINGFDA018-ADC vs Investigator’s Choice Chemotherapy to Treat Locally Advanced, Recurrent or Metastatic Triple-negative Breast Cancer
NCT06889688PHASE3RECRUITINGPhase III Trial of Camrelizumab+Apatinib+Eribulin vs. Physician’s Choice Chemotherapy in Advanced Triple-Negative Breast Cancer
NCT06957886PHASE3RECRUITINGA Study of BL-M07D1 Versus Investigator’s Choice of Chemotherapy in Patients With HER2-low Recurrent/Metastatic Breast Cancer
NCT07088263PHASE3RECRUITINGAdaptive Chemotherapy for the Treatment of Advanced Breast Cancer
NCT07173751PHASE3RECRUITINGROSETTA Breast-01: The Effects and Safety of Pumitamig in Patients With Triple-Negative Breast Cancer
NCT07461454PHASE3RECRUITINGYL202 Versus Treatment of Physician’s Choice in Patients With HR+/HER2- Breast Cancer
NCT01454934PHASE3COMPLETEDA Randomized, Open-label, Multicenter, Phase 3 Study to Compare the Efficacy and Safety of Eribulin With Treatment of Physician’s Choice in Subjects With Advanced Non-Small Cell Lung Cancer
NCT02514681PHASE3COMPLETEDA Phase III Trial of Pertuzumab Retreatment in Previously Pertuzumab Treated Her2-Positive Advanced Breast Cancer
NCT02555657PHASE3COMPLETEDStudy of Single Agent Pembrolizumab (MK-3475) Versus Single Agent Chemotherapy for Metastatic Triple Negative Breast Cancer (MK-3475-119/KEYNOTE-119)
NCT02574455PHASE3COMPLETEDTrial of Sacituzumab Govitecan in Participants With Refractory/Relapsed Metastatic Triple-Negative Breast Cancer (TNBC)
NCT02915744PHASE3COMPLETEDA Study of Etirinotecan Pegol (NKTR-102) Versus Treatment of Physician’s Choice (TPC) in Patients With Metastatic Breast Cancer Who Have Stable Brain Metastases and Have Been Previously Treated With an Anthracycline, a Taxane, and Capecitabine
NCT03264547PHASE3COMPLETEDA Study to Compare Eribulin Mesylate + Pertuzumab + Trastuzumab With Paclitaxel or Docetaxel + Pertuzumab + Trastuzumab
NCT03786094PHASE3TERMINATEDPivotal Study in HER2 Negative, Locally Recurrent or Metastatic Breast Cancer
NCT03901339PHASE3COMPLETEDStudy of Sacituzumab Govitecan-hziy Versus Treatment of Physician’s Choice in Participants With HR+/HER2- Metastatic Breast Cancer
NCT05134194PHASE3TERMINATEDA Study of Camrelizumab in Combination With Chemotherapy Regimen Comparative Chemotherapy Regimen for Metastatic Triple-negative Breast Cancer
NCT02299999PHASE2ACTIVE_NOT_RECRUITINGSAFIR02_Breast - Efficacy of Genome Analysis as a Therapeutic Decision Tool for Patients With Metastatic Breast Cancer
NCT02623972PHASE2ACTIVE_NOT_RECRUITINGA Phase 2 Study of Eribulin Followed by AC as Preoperative Therapy for HER2-negative Inflammatory Breast Cancer
NCT03202316PHASE2ACTIVE_NOT_RECRUITINGAtezolizumab, Cobimetinib, and Eribulin in Treating Patients With Chemotherapy Resistant Metastatic Inflammatory Breast Cancer
NCT03331250PHASE2ACTIVE_NOT_RECRUITINGEribulin in Angiosarcoma and Epithelioid Hemangioendothelioma (EHE)
NCT04986579PHASE2RECRUITINGScalp Cooling in MBC
NCT05458674PHASE2RECRUITINGTucatinib+Trastuzumab+Eribulin in HER2+ MBC
NCT05570253PHASE2RECRUITINGA Study of SDX-7320 in Combination With Eribulin for People With Breast Cancer
NCT05810870PHASE2ACTIVE_NOT_RECRUITINGPIK3CA/PTEN-altered Advanced Breast Cancer Treated With MEN1611 Monotherapy or in Combination With Eribulin
NCT05824975PHASE1/PHASE2RECRUITINGA Study to Evaluate the Safety and Therapeutic Activity of GI-102 As a Single Agent and in Combination with Conventional Anti-cancer Drugs, Pembrolizumab or Trastuzumab Deruxtecan(T-DXd) in Patients with Advanced Solid Tumors (KEYNOTE-G08)
NCT06102824PHASE2RECRUITINGOrganoid-based Functional Precision Therapy for Advanced Breast Cancer
NCT06202313PHASE2NOT_YET_RECRUITINGStudy of Cadonilimab (AK104) Plus Eribulin vs. Eribulin Monotherapy for Recurrent or Metastatic Triple-negative Breast Cancer
NCT06308939PHASE2NOT_YET_RECRUITINGEribulin Combined With Sintilimab as First-line Treatment for Unresectable Locally Advanced or Metastatic HER2-negative Breast Cancer:A Multicenter, Single-arm,Phase II Clinical Trial

Clinical evidence (CIViC)

Variant × indication × effect (1 predictive associations from 1 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
CDK2 CYTOPLASMIC EXPRESSIONTriple-receptor Negative Breast CancerSensitivity/ResponseEribulin + CarboplatinCIViC BEID2969

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

18 molecules share ≥1 primary target. Top 18 by shared-target count:

MoleculeSourceStatusShared targets
PODOFILOXChEMBL + PubChemPhase 4 (approved)TUBB
VINBLASTINEChEMBL + PubChemPhase 4 (approved)TUBB
COLCHICINEChEMBLPhase 4 (approved)TUBB
DOCETAXELChEMBLPhase 4 (approved)TUBB
LEVOFLOXACINChEMBLPhase 4 (approved)TUBB
NOSCAPINEChEMBLPhase 4 (approved)TUBB
PACLITAXELChEMBLPhase 4 (approved)TUBB
TIRBANIBULINChEMBLPhase 4 (approved)TUBB
VINCRISTINEChEMBLPhase 4 (approved)TUBB
VINORELBINEChEMBLPhase 4 (approved)TUBB
PATUPILONEChEMBLPhase 3TUBB
ABT-751ChEMBLPhase 2TUBB
DOLASTATIN-10ChEMBLPhase 2TUBB
INDIBULINChEMBLPhase 2TUBB
MAYTANSINEChEMBLPhase 2TUBB
MOLIBRESIBChEMBLPhase 2TUBB
NOCODAZOLEChEMBLPhase 2TUBB
PARBENDAZOLEChEMBLPhase 2TUBB