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Association details:
| Biomarker: | EP300 mutation |
|---|---|
| Cancer: | Diffuse Large B Cell Lymphoma |
| Drug: | YF2 (Histone acetyltransferase activator) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
Development of First-in-Class Histone Acetyltransferase (HAT) Activators for Precision Targeting of Epigenetic Derangements in Lymphoma
Published date:
11/01/2018
Excerpt:
To assess the pharmacokinetics (PK) and preliminary in vivo efficacy of YF2, SUDHL-6 (EP300-mutated) xenograft bearing mice were treated once daily i.p. for 6 days with YF2 doses of 40mg/kg or 60mg/kg….It demonstrates selective cytotoxic effects in EP300-mutated DLBCL cell lines, and is both well tolerated and effective in xenograft mouse models of lymphoma suggesting potential clinical application and precision medicine opportunities for patients harboring this mutation.
DOI:
https://doi.org/10.1182/blood-2018-99-110447
