CDKN2A/B Homozygous Deletion Sensitizes IDH-Mutant Glioma to CDK4/6 Inhibition

Clin Cancer Res. 2024 Jul 15;30(14):2996-3005. doi: 10.1158/1078-0432.CCR-24-0562.

Abstract

Purpose: Treatment paradigms for isocitrate dehydrogenase (IDH)-mutant gliomas are rapidly evolving. Although typically indolent and responsive to initial treatment, these tumors invariably recur at a higher grade and require salvage treatment. Homozygous deletion of the tumor suppressor gene CDKN2A/B frequently emerges at recurrence in these tumors, driving poor patient outcomes. We investigated the effect of CDK-Rb pathway blockade on IDH-mutant glioma growth in vitro and in vivo using CDK4/6 inhibitors (CDKi).

Experimental design: Cell viability, proliferation assays, and flow cytometry were used to examine the pharmacologic effect of two distinct CDKi, palbociclib and abemaciclib, in multiple patient-derived IDH-mutant glioma lines. Isogenic models were used to directly investigate the influence of CDKN2A/B status on CDKi sensitivity. Orthotopic xenograft tumor models were used to examine the efficacy and tolerability of CDKi in vivo.

Results: CDKi treatment leads to decreased cell viability and proliferative capacity in patient-derived IDH-mutant glioma lines, coupled with enrichment of cells in the G1 phase. CDKN2A inactivation sensitizes IDH-mutant glioma to CDKi in both endogenous and isogenic models with engineered CDKN2A deletion. CDK4/6 inhibitor administration improves survival in orthotopically implanted IDH-mutant glioma models.

Conclusions: IDH-mutant gliomas with deletion of CDKN2A/B are sensitized to CDK4/6 inhibitors. These results support the investigation of the use of these agents in a clinical setting.

MeSH terms

  • Aminopyridines* / pharmacology
  • Animals
  • Benzimidazoles* / pharmacology
  • Brain Neoplasms / drug therapy
  • Brain Neoplasms / genetics
  • Brain Neoplasms / pathology
  • Cell Line, Tumor
  • Cell Proliferation* / drug effects
  • Cyclin-Dependent Kinase 4* / antagonists & inhibitors
  • Cyclin-Dependent Kinase 4* / genetics
  • Cyclin-Dependent Kinase 6* / antagonists & inhibitors
  • Cyclin-Dependent Kinase 6* / genetics
  • Cyclin-Dependent Kinase Inhibitor p15* / genetics
  • Cyclin-Dependent Kinase Inhibitor p16* / genetics
  • Gene Deletion
  • Glioma* / drug therapy
  • Glioma* / genetics
  • Glioma* / pathology
  • Homozygote
  • Humans
  • Isocitrate Dehydrogenase* / antagonists & inhibitors
  • Isocitrate Dehydrogenase* / genetics
  • Mice
  • Mutation*
  • Piperazines* / pharmacology
  • Piperazines* / therapeutic use
  • Protein Kinase Inhibitors* / pharmacology
  • Protein Kinase Inhibitors* / therapeutic use
  • Pyridines* / pharmacology
  • Pyridines* / therapeutic use
  • Xenograft Model Antitumor Assays*

Substances

  • Cyclin-Dependent Kinase 4
  • Cyclin-Dependent Kinase 6
  • Cyclin-Dependent Kinase Inhibitor p16
  • Isocitrate Dehydrogenase
  • palbociclib
  • Benzimidazoles
  • Cyclin-Dependent Kinase Inhibitor p15
  • Aminopyridines
  • abemaciclib
  • CDK6 protein, human
  • Protein Kinase Inhibitors
  • Piperazines
  • Pyridines
  • CDK4 protein, human
  • CDKN2A protein, human
  • CDKN2B protein, human