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Cellular and Molecular Effects of Eribulin in Preclinical Models of Hematologic Neoplasms

Hugo Passos Vicari1, Keli Lima1,2, Leticia Veras Costa-Lotufo1

  • 1Department of Pharmacology, Institute of Biomedical Sciences, University of São Paulo, São Paulos 05508-000, Brazil.

Cancers
|December 23, 2022
PubMed

Insights

Eribulin effectively targets blood cancer cells, inducing cell death and DNA damage. Combining eribulin with elacridar may overcome drug resistance in hematologic neoplasms.

Area of Science:

  • Hematology
  • Oncology
  • Molecular Biology

Background:

  • Therapeutic options for relapsed/refractory hematologic neoplasms remain limited despite advances in cancer biology and drug approvals.
  • Eribulin, a microtubule inhibitor, is approved for metastatic breast cancer and soft tissue tumors, but its efficacy in blood cancers is less understood.

Purpose of the Study:

  • To investigate the cellular and molecular effects of eribulin in a diverse panel of hematologic neoplasms.
  • To identify potential biomarkers for eribulin responsiveness and explore combination therapies to overcome drug resistance.

Main Methods:

  • Eribulin's effects on cell viability, clonogenicity, apoptosis, and cell cycle arrest were assessed in hematologic neoplasm cell lines.
  • Molecular analyses included evaluating DNA damage, apoptosis markers, and the expression/activation of ABCB1, ABCC1, AKT, and NFκB.
  • Combination treatments with eribulin and elacridar (P-glycoprotein inhibitor) or PDTC (NFκB inhibitor) were tested in leukemia cells.

Main Results:

  • Eribulin demonstrated reduced cell viability and clonogenicity, induced apoptosis and cell cycle arrest in blood cancer cells, with minimal effects on normal leukocytes, suggesting selectivity.
  • Eribulin treatment led to DNA damage and apoptosis marker induction.
  • ABCB1, ABCC1, p-AKT, and p-NFκB levels correlated with eribulin response, leading to the construction of a resistance score. Combination with elacridar enhanced eribulin-induced apoptosis in leukemia cells.

Conclusions:

  • Eribulin induces mitotic catastrophe and cell death in hematologic neoplasms.
  • MDR1, PI3K/AKT, and NFκB pathway components may serve as predictive biomarkers for eribulin response.
  • Combination therapy with eribulin and elacridar shows potential for overcoming drug resistance in blood cancers.
Keywords:
acute leukemiasdrug resistanceeribulinmicrotubule dynamics

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