The non-peptide thrombopoietin receptor agonist eltrombopag stimulates megakaryopoiesis in bone marrow cells from patients with relapsed multiple myeloma

J Hematol Oncol. 2015 Apr 16:8:37. doi: 10.1186/s13045-015-0136-2.

Abstract

Background: Thrombocytopenia is a significant problem in patients with relapsed or refractory multiple myeloma, precipitating a need for supportive platelet transfusions and necessitating decreases in delivered doses of chemotherapy. Eltrombopag is a non-peptide, small molecule thrombopoietin (TPO) receptor agonist that promotes megakaryopoiesis similar to endogenous human TPO and may be an effective agent for thrombocytopenia in this patient population.

Methods: We examined the effects of eltrombopag on megakaryocyte colony-forming capacity in CD34+ cells in patients with multiple myeloma and investigated its impact on proliferation, viability, and apoptosis in primary CD138+ human myeloma cells and myeloma cell lines.

Results: Eltrombopag at doses of 0.1 to 100 μM did not enhance proliferation of primary human CD138+ multiple myeloma cells from patients with relapsed disease or myeloma cell lines when used alone or in combination with erythropoietin (EPO) and granulocyte colony-stimulating factor (G-CSF) and did not alter cell viability nor apoptosis of human myeloma cells exposed to bortezomib and lenalidomide. Eltrombopag stimulated megakaryopoiesis in human CD34+ cells from normal individuals and from patients with relapsed multiple myeloma via activation of Akt signaling pathways.

Conclusions: These results provide proof-of-principle supporting the design of future clinical studies examining eltrombopag for the treatment of thrombocytopenia in patients with advanced multiple myeloma.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzoates / pharmacology*
  • Cell Line, Tumor
  • Hematopoiesis / drug effects*
  • Humans
  • Hydrazines / pharmacology*
  • In Vitro Techniques
  • Megakaryocytes / drug effects*
  • Multiple Myeloma / complications*
  • Neoplasm Recurrence, Local / complications
  • Pyrazoles / pharmacology*
  • Receptors, Thrombopoietin / agonists
  • Thrombocytopenia / drug therapy*
  • Thrombocytopenia / etiology

Substances

  • Benzoates
  • Hydrazines
  • Pyrazoles
  • Receptors, Thrombopoietin
  • eltrombopag