Thrilled to share our work with Mariella Filbin, Johannes Gojo and Carl Koschmann, now published in @cp-cancercell.bsky.social We present a translational approach identifying the PDGFRA inhibitor avapritinib as a novel targeted treatment for pHGG with PDGFRA alterations www.cell.com/cancer-cell/...
Effective targeting of PDGFRA-altered high-grade glioma with avapritinib
PDGFRA is commonly altered in pediatric HGG. Mayr et al. report that the PDGFRA/KIT
inhibitor avapritinib demonstrates on-target activity, brain penetrance, and survival
benefit in pre-clinical H3K27M...
www.cell.com
March 13, 2025 at 3:30 PM
Thrilled to share our work with Mariella Filbin, Johannes Gojo and Carl Koschmann, now published in @cp-cancercell.bsky.social We present a translational approach identifying the PDGFRA inhibitor avapritinib as a novel targeted treatment for pHGG with PDGFRA alterations www.cell.com/cancer-cell/...
Targeting PDGFRA in pediatric high-grade glioma 👏 www.cell.com/cancer-cell/...
Effective targeting of PDGFRA-altered high-grade glioma with avapritinib
PDGFRA is commonly altered in pediatric HGG. Mayr et al. report that the PDGFRA/KIT
inhibitor avapritinib demonstrates on-target activity, brain penetrance, and survival
benefit in pre-clinical H3K27M...
www.cell.com
April 14, 2025 at 11:44 PM
Targeting PDGFRA in pediatric high-grade glioma 👏 www.cell.com/cancer-cell/...
This week #JournalClub @labsoap.bsky.social #PDGFRA #HGG #BrainTumor @cp-cancercell.bsky.social @sinaneyazi.bsky.social
www.cell.com/cancer-cell/...
www.cell.com/cancer-cell/...
Effective targeting of PDGFRA-altered high-grade glioma with avapritinib
PDGFRA is commonly altered in pediatric HGG. Mayr et al. report that the PDGFRA/KIT
inhibitor avapritinib demonstrates on-target activity, brain penetrance, and survival
benefit in pre-clinical H3K27M...
www.cell.com
April 22, 2025 at 8:17 AM
Translational data indicate that the PDGFRA/KIT inhibitor avapritinib shows preclinical activity and effective blood-brain barrier penetration in PDGFRA-altered high-grade glioma (HGG). Early clinical observations in a small cohort (n=8) showed a radiographic response in 3/7 cases.
Effective targeting of PDGFRA-altered high-grade glioma with avapritinib
PDGFRA is commonly altered in pediatric HGG. Mayr et al. report that the PDGFRA/KIT
inhibitor avapritinib demonstrates on-target activity, brain penetrance, and survival
benefit in pre-clinical H3K27M...
www.cell.com
June 3, 2026 at 12:34 PM
Translational data indicate that the PDGFRA/KIT inhibitor avapritinib shows preclinical activity and effective blood-brain barrier penetration in PDGFRA-altered high-grade glioma (HGG). Early clinical observations in a small cohort (n=8) showed a radiographic response in 3/7 cases.
Hoffnung bei #Hirntumoren bei #Kindern: Forschungsteam der #MedUni #Wien entdeckt gezielte Therapie gegen aggressive #Gliome. Der #PDGFRA-Inhibitor #Avapritinib zeigt erste Erfolge – Tumore, die resistent gegen Bestrahlung waren, sprechen an. Vielversprechend! #Krebs
www.cell.com/cancer-cell/...
www.cell.com/cancer-cell/...
Effective targeting of PDGFRA-altered high-grade glioma with avapritinib
PDGFRA is commonly altered in pediatric HGG. Mayr et al. report that the PDGFRA/KIT
inhibitor avapritinib demonstrates on-target activity, brain penetrance, and survival
benefit in pre-clinical H3K27M...
www.cell.com
March 14, 2025 at 12:18 PM
Hoffnung bei #Hirntumoren bei #Kindern: Forschungsteam der #MedUni #Wien entdeckt gezielte Therapie gegen aggressive #Gliome. Der #PDGFRA-Inhibitor #Avapritinib zeigt erste Erfolge – Tumore, die resistent gegen Bestrahlung waren, sprechen an. Vielversprechend! #Krebs
www.cell.com/cancer-cell/...
www.cell.com/cancer-cell/...
Quite an interesting article on targeting PDGFRA altered High-Grade Glioma
#ISRVT25
Effective targeting of PDGFRA-altered high-grade glioma with avapritinib: Cancer Cell www.cell.com/cancer-cell/...
#ISRVT25
Effective targeting of PDGFRA-altered high-grade glioma with avapritinib: Cancer Cell www.cell.com/cancer-cell/...
Effective targeting of PDGFRA-altered high-grade glioma with avapritinib
PDGFRA is commonly altered in pediatric HGG. Mayr et al. report that the PDGFRA/KIT
inhibitor avapritinib demonstrates on-target activity, brain penetrance, and survival
benefit in pre-clinical H3K27M...
www.cell.com
March 17, 2025 at 2:38 PM
Quite an interesting article on targeting PDGFRA altered High-Grade Glioma
#ISRVT25
Effective targeting of PDGFRA-altered high-grade glioma with avapritinib: Cancer Cell www.cell.com/cancer-cell/...
#ISRVT25
Effective targeting of PDGFRA-altered high-grade glioma with avapritinib: Cancer Cell www.cell.com/cancer-cell/...
Effective targeting of PDGFRA-altered high-grade glioma with avapritinib
Effective targeting of PDGFRA-altered high-grade glioma with avapritinib
PDGFRA is commonly altered in pediatric HGG. Mayr et al. report that the PDGFRA/KIT inhibitor avapritinib demonstrates on-target activity, brain penetrance, and survival benefit in pre-clinical H3K27M DMG models. In pediatric HGG patients, avapritinib treatment is well tolerated and results in radiographic and clinical response in a subset of patients.
dlvr.it
April 15, 2025 at 6:51 PM
Effective targeting of PDGFRA-altered high-grade glioma with avapritinib
New hope for #BrainTumors in #Children: Research team from #MedUni #Vienna discovers targeted therapy for aggressive gliomas. The #PDGFRA inhibitor #Avapritinib shows initial success – tumors resistant to radiation are responding. Promising! #Cancer
www.cell.com/cancer-cell/...
www.cell.com/cancer-cell/...
Effective targeting of PDGFRA-altered high-grade glioma with avapritinib
PDGFRA is commonly altered in pediatric HGG. Mayr et al. report that the PDGFRA/KIT
inhibitor avapritinib demonstrates on-target activity, brain penetrance, and survival
benefit in pre-clinical H3K27M...
www.cell.com
March 14, 2025 at 12:19 PM
New hope for #BrainTumors in #Children: Research team from #MedUni #Vienna discovers targeted therapy for aggressive gliomas. The #PDGFRA inhibitor #Avapritinib shows initial success – tumors resistant to radiation are responding. Promising! #Cancer
www.cell.com/cancer-cell/...
www.cell.com/cancer-cell/...
Dr. Xueqing Dou discusses KIT/PDGFRA inhibitor avapritinib in 40 pts w/ core binding factor (CBF) AML w/ KIT mutations (possible higher risk of relapse) w/ R/R disease (n=12) or persistent MRD (n=28). 60% had ≥1-log MRD reduction as best response. Faster responses w/ t(8;21) (1/x) #ash24 #leusm
December 7, 2024 at 11:26 PM
Pediatric high-grade gliomas (pHGG), including H3K27M-DMGs, remain a major cause of cancer mortality in children. ~15% harbor PDGFRA alterations - making this receptor an attractive therapeutic target 🧵 1/n 👇👇
www.cell.com/cancer-cell/...
www.cell.com/cancer-cell/...
Effective targeting of PDGFRA-altered high-grade glioma with avapritinib
PDGFRA is commonly altered in pediatric HGG. Mayr et al. report that the PDGFRA/KIT
inhibitor avapritinib demonstrates on-target activity, brain penetrance, and survival
benefit in pre-clinical H3K27M...
www.cell.com
April 14, 2025 at 4:45 PM
Pediatric high-grade gliomas (pHGG), including H3K27M-DMGs, remain a major cause of cancer mortality in children. ~15% harbor PDGFRA alterations - making this receptor an attractive therapeutic target 🧵 1/n 👇👇
www.cell.com/cancer-cell/...
www.cell.com/cancer-cell/...
Development and characterization of KIT/PDGFRA inhibitors to define key molecular interactions underlying inhibitor selectivity and drug-resistance @DDHDortmund #MedicinalChemistry #GIST #DrugDiscovery #Kinase #StructuralBiology #ChemicalBiology
Structure-based scaffold hopping reveals strategies to overcome oncogenic KIT and PDGFRA mutation-driven drug-resistance in GIST - Nature Communications
In this work, the authors develop and characterize KIT/PDGFRA inhibitors to define key molecular interactions underlying inhibitor selectivity and drug-resistance, reporting structural insights for targeting solvent-front mutations across oncogenic kinases.
dlvr.it
August 7, 2026 at 12:30 PM
Development and characterization of KIT/PDGFRA inhibitors to define key molecular interactions underlying inhibitor selectivity and drug-resistance @DDHDortmund #MedicinalChemistry #GIST #DrugDiscovery #Kinase #StructuralBiology #ChemicalBiology
This study showed that avapritinib, a selective PDGFRA inhibitor, crosses the blood-brain barrier and potently suppresses PDGFRA-driven signaling in preclinical pHGG models with minimal toxicity. 2/n
April 14, 2025 at 4:45 PM
This study showed that avapritinib, a selective PDGFRA inhibitor, crosses the blood-brain barrier and potently suppresses PDGFRA-driven signaling in preclinical pHGG models with minimal toxicity. 2/n
Online Now: Effective targeting of PDGFRA-altered high-grade glioma with avapritinib
Effective targeting of PDGFRA-altered high-grade glioma with avapritinib
PDGFRA is commonly altered in pediatric HGG. Mayr et al. report that the PDGFRA/KIT inhibitor avapritinib demonstrates on-target activity, brain penetrance, and survival benefit in pre-clinical H3K27M DMG models. In pediatric HGG patients, avapritinib…
dlvr.it
March 19, 2025 at 6:51 PM
Online Now: Effective targeting of PDGFRA-altered high-grade glioma with avapritinib
💊 In #ACSMedChemLett, Mmonwa et al. report a human PDGFRA kinase inhibitor with potent antiplasmodium activity. Medicinal chemistry optimisation improved potency, selectivity and ADME, yielding compounds that inhibit haemozoin formation and kill late-stage parasites: pubs.acs.org/doi/10.1021/...
pubs.acs.org
January 9, 2026 at 9:06 AM
💊 In #ACSMedChemLett, Mmonwa et al. report a human PDGFRA kinase inhibitor with potent antiplasmodium activity. Medicinal chemistry optimisation improved potency, selectivity and ADME, yielding compounds that inhibit haemozoin formation and kill late-stage parasites: pubs.acs.org/doi/10.1021/...
5/ Among a panel of 2nd and 3rd generation TKIs, we identified the FDA-approved PDGFRA/KIT inhibitor avapritinib as selective against PDGFRA and highly effective against PDGFRA-altered patient-derived pHGG and DMG models in vitro.
March 13, 2025 at 3:30 PM
5/ Among a panel of 2nd and 3rd generation TKIs, we identified the FDA-approved PDGFRA/KIT inhibitor avapritinib as selective against PDGFRA and highly effective against PDGFRA-altered patient-derived pHGG and DMG models in vitro.