Lenalidomide in combination with an activin A-neutralizing antibody: preclinical rationale for a novel anti-myeloma strategy

Leukemia. 2013 Aug;27(8):1715-21. doi: 10.1038/leu.2013.50. Epub 2013 Feb 18.

Abstract

Given the prevalence of osteolytic bone disease in multiple myeloma (MM), novel therapies targeting bone microenvironment are essential. Previous studies have identified activin A to be of critical importance in MM-induced osteolysis. Lenalidomide is a known and approved treatment strategy for relapsed MM. Our findings demonstrate that lenalidomide acts directly on bone marrow stromal cells via an Akt-mediated increase in Jun N-terminal kinase-dependent signaling resulting in activin A secretion, with consequent inhibition of osteoblastogenesis. Here, we attempted to augment the antitumor benefits of lenalidomide while overcoming its effects on osteoblastogenesis by combining it with a neutralizing antibody to activin A. Increased activin A secretion induced by lenalidomide was abrogated by the addition of activin A-neutralizing antibody, which effectively restored osteoblast function and inhibited MM-induced osteolysis without negating the cytotoxic effects of lenalidomide on malignant cells. This provides the rationale for an ongoing clinical trial (NCT01562405) combining lenalidomide with an anti-activin A strategy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Activins / antagonists & inhibitors*
  • Activins / metabolism
  • Angiogenesis Inhibitors / pharmacology*
  • Antibodies, Neutralizing / pharmacology*
  • Antineoplastic Agents / pharmacology*
  • Cell Differentiation / drug effects
  • Cell Line, Tumor
  • Humans
  • Lenalidomide
  • MAP Kinase Signaling System / drug effects
  • Multiple Myeloma / genetics
  • Multiple Myeloma / metabolism*
  • Osteoblasts / cytology
  • Osteoblasts / drug effects
  • Osteoblasts / metabolism
  • Stromal Cells / drug effects
  • Stromal Cells / metabolism
  • Thalidomide / analogs & derivatives*
  • Thalidomide / pharmacology

Substances

  • Angiogenesis Inhibitors
  • Antibodies, Neutralizing
  • Antineoplastic Agents
  • activin A
  • Activins
  • Thalidomide
  • Lenalidomide

Associated data

  • ClinicalTrials.gov/NCT01562405