The anti-histaminic cyproheptadine synergizes the antineoplastic activity of bortezomib in mantle cell lymphoma through its effects as a histone deacetylase inhibitor

Br J Haematol. 2009 Sep;146(6):656-9. doi: 10.1111/j.1365-2141.2009.07797.x. Epub 2009 Jul 8.

Abstract

Cyproheptadine, an inhibitor of the H1 histamine receptors, has recently shown activity in models of leukaemia and myeloma, presumably through inhibition of cyclin-D expression. Mantle cell lymphoma (MCL) is an aggressive subtype of non-Hodgkin lymphoma characterized by overexpression of cyclin-D1. We investigated the effect of cyproheptadine alone and in combination with the proteasome inhibitor bortezomib in models of MCL. The combination of these drugs was mathematically synergistic, producing significant reductions in the mitochondrial membrane potential leading to apoptosis. In a severe combined immunodeficient beige mouse model, cyproheptadine plus bortezomib demonstrated a statistically significant advantage compared to either agent alone.

MeSH terms

  • Actins / metabolism
  • Animals
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology*
  • Apoptosis / drug effects
  • Boronic Acids / administration & dosage
  • Bortezomib
  • Cyclin D1 / metabolism
  • Cyproheptadine / administration & dosage
  • Disease Models, Animal
  • Histamine H1 Antagonists / pharmacology*
  • Histone Deacetylase Inhibitors*
  • Lymphoma, Mantle-Cell / drug therapy*
  • Mice
  • Protease Inhibitors / pharmacology*
  • Pyrazines / administration & dosage

Substances

  • Actins
  • Boronic Acids
  • Histamine H1 Antagonists
  • Histone Deacetylase Inhibitors
  • Protease Inhibitors
  • Pyrazines
  • Cyclin D1
  • Cyproheptadine
  • Bortezomib