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Association details:
| Biomarker: | BRAF V600E |
|---|---|
| Cancer: | Glioma |
| Drug: | ulixertinib (BVD-523) (ERK2 inhibitor, ERK1 inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
The first-in-class ERK inhibitor ulixertinib shows promising activity in MAPK-driven pediatric low-grade glioma models
Published date:
07/27/2022
Excerpt:
Patient-derived pLGG models reflecting the two most common alterations in the disease, KIAA1549:BRAF-fusion and BRAF V600E mutation (DKFZ-BT66 and BT40, respectively) were used for in vitro and in vivo (zebrafish embryos and mice) efficacy testing….Ulixertinib inhibited MAPK pathway activity in both models, and reduced cell viability in BT40 with clinically achievable concentrations in the low nanomolar range. Combination treatment of ulixertinib with MEKi or BH3-mimetics showed strong evidence of anti-proliferative synergy in vitro....In a preclinical mouse trial, ulixertinib mono- and combined therapies slowed tumor growth and increased survival.
Secondary therapy:
MEK Inhibitor
DOI:
10.1093/neuonc/noac183
