Preclinical anti-myeloma activity of the novel HDAC-inhibitor JNJ-26481585

Br J Haematol. 2010 May;149(4):529-36. doi: 10.1111/j.1365-2141.2010.08126.x. Epub 2010 Mar 13.

Abstract

Pharmacological inhibitors of histone deacetylases (HDACs) are currently being developed and tested as anti-cancer agents and may be useful to enhance the therapeutic efficiency of established anti-myeloma treatments. This study preclinically evaluated the effects of the 'second generation' pan-HDAC inhibitor JNJ-26481585 on human multiple myeloma (MM) cells from established cell lines and primary MM samples (n=42). Molecular responses in both groups of MM cells included histone acetylation, a shift in Bcl2-family members towards proapoptotic bias, attenuation of growth and survival pathway activity and Hsp72 induction. Mcl-1 depletion and Hsp72 induction were the most reliable features observed in JNJ-26481585-treated primary MM samples. The drug alone effectively induced myeloma cell death at low nanomolar concentrations. In vitro combination of JNJ-26481585 with anti-myeloma therapeutic agents generally resulted In effects close to additivity. In view of the favourable activity of this novel HDAC-inhibitor towards primary myeloma cells further evaluation in a clinical setting is warranted.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylation / drug effects
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology
  • Apoptosis / drug effects
  • Dose-Response Relationship, Drug
  • Drug Evaluation, Preclinical / methods
  • Histone Deacetylase Inhibitors / pharmacology*
  • Histones / metabolism
  • Humans
  • Hydroxamic Acids / pharmacology*
  • Multiple Myeloma / metabolism
  • Multiple Myeloma / pathology*
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Histone Deacetylase Inhibitors
  • Histones
  • Hydroxamic Acids
  • quisinostat