Preclinical Efficacy of Brain Penetrant, Single Agent Avapritinib inPDGFRA EcDNA-amplified Glioblastoma

Document Type

Conference Proceeding

Publication Date

11-11-2025

Publication Title

Neuro Oncol

Keywords

Oncology, Neurosciences & Neurology

Abstract

The high prevalence of platelet derived growth factor receptor alpha (PDGFRA) alterations and its mitogenic function in oligodendrocyte precursor cells (OPC) make PDGFRA a promising therapeutic target in adult glioblastoma (GBM). Towards validating PDGFRA as an essential driver of GBM tumor maintenance, we have isolated subpopulations from a patient-derived model (HF3253), harboring two alterations in PDGFRA: internal deletion leading to constitutive activation and extrachromosomal (ecDNA) amplification driving high copy number and heterogeneity. HF3253 symptom-free survival correlated with the initial frequency of PDGFRA ecDNA(+) population implanted; prolonged symptom-free survival was due to selection for initially low-frequency PDGFRA ecDNA(+) clones. Employing bulk and single-cell RNA sequencing, PDGFRA modulated a biphasic injury response/developmental transcriptional signature corresponding to hijacked functions of OPCs and CNS fibroblasts. Exploiting intra-tumoral heterogeneity, we have isolated single cell clones from bulk cells that exhibit diploid PDGFRA copy number, very low levels of PDGFRA mRNA and undetectable PDGFRA protein. Symptom-free survival was substantially increased in 4 ecDNA(-) clones compared to parental ecDNA(+) (Log rank p< 0.0001; n ≥ 4/group). Rescue of wild-type PDGFRA by lentivirus in two ecDNA(-) populations decreased median survival by 50% in orthotopic xenograft relative to controls (log rank p = 0.3118, 0.0028; n=5/group). Avapritinib, a PDGFRA/KIT-selective kinase inhibitor, has shown promising efficacy in PDGFRA-mutated pediatric high-grade glioma. 5-week avapritinib (40 mg/kg) treatment abrogated HF3253 tumor growth by bioluminescent imaging. While treatment significantly improved survival compared to control in orthotopic male and female xenografts (log rank p=0.0047; n ≥ 9/group), independent of sex (pairwise log rank p=0.232), PDGFRA+ tumors rapidly developed within two weeks of drug removal. Similar to 5-week treatment, continuous avapritinib therapy improved xenograft survival (log rank p > 0.0001; n ≥ 8/group), increasing median survival by an additional 4 days in males. Our work validates PDGFRA ecDNA as a predictive biomarker for PDGFRA-targeted therapies and justifies the clinical implementation of avapritinib in the treatment of PDGFRA-altered brain tumors.

Volume

27

Issue

Supplement 5

First Page

v372

Last Page

v373

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