Genotype-targeted local therapy of glioma

Proc Natl Acad Sci U S A. 2018 Sep 4;115(36):E8388-E8394. doi: 10.1073/pnas.1805751115. Epub 2018 Aug 6.

Abstract

Aggressive neurosurgical resection to achieve sustained local control is essential for prolonging survival in patients with lower-grade glioma. However, progression in many of these patients is characterized by local regrowth. Most lower-grade gliomas harbor isocitrate dehydrogenase 1 (IDH1) or IDH2 mutations, which sensitize to metabolism-altering agents. To improve local control of IDH mutant gliomas while avoiding systemic toxicity associated with metabolic therapies, we developed a precision intraoperative treatment that couples a rapid multiplexed genotyping tool with a sustained release microparticle (MP) drug delivery system containing an IDH-directed nicotinamide phosphoribosyltransferase (NAMPT) inhibitor (GMX-1778). We validated our genetic diagnostic tool on clinically annotated tumor specimens. GMX-1778 MPs showed mutant IDH genotype-specific toxicity in vitro and in vivo, inducing regression of orthotopic IDH mutant glioma murine models. Our strategy enables immediate intraoperative genotyping and local application of a genotype-specific treatment in surgical scenarios where local tumor control is paramount and systemic toxicity is therapeutically limiting.

Keywords: glioma; intraoperative diagnostics; local therapy; metabolic therapeutics.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Brain Neoplasms* / drug therapy
  • Brain Neoplasms* / enzymology
  • Brain Neoplasms* / genetics
  • Cyanides / pharmacology*
  • Drug Delivery Systems / methods
  • Female
  • Genotype*
  • Glioma* / drug therapy
  • Glioma* / enzymology
  • Glioma* / genetics
  • Guanidines / pharmacology*
  • Humans
  • Isocitrate Dehydrogenase / genetics*
  • Male
  • Mice
  • Mice, SCID
  • Molecular Targeted Therapy / methods*
  • Mutation*
  • Neoplasm Proteins / genetics*
  • Xenograft Model Antitumor Assays

Substances

  • Cyanides
  • Guanidines
  • N-(6-chlorophenoxyhexyl)-N''-cyano-N''-4-pyridylguanidine
  • Neoplasm Proteins
  • IDH2 protein, human
  • Isocitrate Dehydrogenase
  • IDH1 protein, human