Anti-invasive adjuvant therapy with imipramine blue enhances chemotherapeutic efficacy against glioma

Sci Transl Med. 2012 Mar 28;4(127):127ra36. doi: 10.1126/scitranslmed.3003016.

Abstract

The invasive nature of glioblastoma (GBM) represents a major clinical challenge contributing to poor outcomes. Invasion of GBM into healthy tissue restricts chemotherapeutic access and complicates surgical resection. Here, we test the hypothesis that an effective anti-invasive agent can "contain" GBM and increase the efficacy of chemotherapy. We report a new anti-invasive small molecule, Imipramine Blue (IB), which inhibits invasion of glioma in vitro when tested against several models. IB inhibits NADPH (reduced form of nicotinamide adenine dinucleotide phosphate) oxidase-mediated reactive oxygen species generation and alters expression of actin regulatory elements. In vivo, liposomal IB (nano-IB) halts invasion of glioma, leading to a more compact tumor in an aggressively invasive RT2 syngeneic astrocytoma rodent model. When nano-IB therapy was followed by liposomal doxorubicin (nano-DXR) chemotherapy, the combination therapy prolonged survival compared to nano-IB or nano-DXR alone. Our data demonstrate that nano-IB-mediated containment of diffuse glioma enhanced the efficacy of nano-DXR chemotherapy, demonstrating the promise of an anti-invasive compound as an adjuvant treatment for glioma.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Antineoplastic Combined Chemotherapy Protocols / pharmacokinetics
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Brain Neoplasms / drug therapy*
  • Brain Neoplasms / pathology*
  • Cell Line, Tumor
  • Cell Proliferation
  • Chemotherapy, Adjuvant
  • Doxorubicin / therapeutic use
  • Drug Carriers / chemistry
  • Drug Delivery Systems
  • Glioma / drug therapy*
  • Glioma / pathology*
  • Humans
  • Imipramine / chemical synthesis
  • Imipramine / chemistry
  • Imipramine / pharmacokinetics
  • Imipramine / therapeutic use*
  • Liposomes / chemistry
  • Nanoparticles / chemistry
  • Neoplasm Invasiveness
  • Rats
  • Treatment Outcome

Substances

  • Drug Carriers
  • Liposomes
  • Doxorubicin
  • Imipramine