Synergistic Activity of Carfilzomib and Panobinostat in Multiple Myeloma Cells via Modulation of ROS Generation and ERK1/2

Biomed Res Int. 2015:2015:459052. doi: 10.1155/2015/459052. Epub 2015 Apr 27.

Abstract

Relapse of disease and subsequent resistance to established therapies remain as major challenges in the treatment of multiple myeloma (MM). New therapeutic options are needed for these extensively pretreated patients. To explore an optimized combinational therapy, interactions between the irreversible proteasome inhibitor carfilzomib exhibiting a well-tolerated side-effect profile and histone deacetylase inhibitor (HDACi) panobinostat (LBH589) were examined in MM cells. Coadministration of carfilzomib and LBH589 led to a synergistic inhibition of proliferation in MM cells. Further studies showed that the combined treatment synergistically increased mitochondrial injury, caspase activation, and apoptosis in MM cells. Lethality of the carfilzomib/LBH589 combination was associated with the reactive oxygen species (ROS) generation and ERK1/2 inactivation. In addition, the free radical scavenger N-acetylcysteine (NAC) could block carfilzomib and LBH589-induced oxidative stress and the subsequent apoptosis. Together, these findings argue that the strategy of combining carfilzomib and LBH589 warrants attention in MM.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis / drug effects
  • Caspases / metabolism
  • Cell Cycle / drug effects
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Drug Synergism
  • Enzyme Activation / drug effects
  • Humans
  • Hydroxamic Acids / pharmacology*
  • Indoles / pharmacology*
  • MAP Kinase Signaling System / drug effects
  • Mitochondria / drug effects
  • Mitochondria / metabolism
  • Mitogen-Activated Protein Kinase 1 / metabolism*
  • Mitogen-Activated Protein Kinase 3 / metabolism*
  • Multiple Myeloma / drug therapy*
  • Multiple Myeloma / enzymology
  • Multiple Myeloma / metabolism*
  • Multiple Myeloma / pathology
  • Oligopeptides / pharmacology*
  • Panobinostat
  • Reactive Oxygen Species / metabolism*

Substances

  • Hydroxamic Acids
  • Indoles
  • Oligopeptides
  • Reactive Oxygen Species
  • carfilzomib
  • Panobinostat
  • Mitogen-Activated Protein Kinase 1
  • Mitogen-Activated Protein Kinase 3
  • Caspases