^
Association details:
Biomarker:EZH2 Y641F
Cancer:Melanoma
Drug:Tafinlar (dabrafenib) (BRAF inhibitor) +
JQEZ5 (EZH2 inhibitor)
Direction:Sensitive
Evidence:
Evidence Level:
Sensitive: D – Preclinical
New
Source:
Title:

An oncogenic Ezh2 mutation cooperates with particular genetic alterations to induce tumors in mice and redistributes H3K27 trimethylation throughout the genome

Excerpt:
Dabrafenib and JQEZ5 resulted in tumor growth inhibition in both Ezh2+/+ and Ezh2Y641F/+ tumors, with Dabrafenib being the more potent agent. Combinatorial treatment with Dabrafenib and JQEZ5 resulted in additive activity in Ezh2Y641F/+ but not Ezh2+/+ tumors...and is effective in combination with a B-RAF inhibitor in RAF-mutant melanoma.
DOI:
10.1038/nm.4092