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Association details:
Biomarker:KDM6A mutation
Cancer:Renal Cell Carcinoma
Drug:MRTX2219 (PRC2 inhibitor)
Direction:Sensitive
Evidence:
Evidence Level:
Sensitive: D – Preclinical
Title:

MRTX2219 is an imidazopyrimidine binder to EED that inhibits polycomb repressive complex 2 (PRC2) and demonstrates robust in vivo activity in EZH2 and SMARCB1-mutant, but not other SWI/SNF-mutant cancer models

Published date:
05/15/2020
Excerpt:
While a PRC2 inhibitor may be active in molecularly-defined subsets of SWI/SNF or KDM6A-mutant cancers, overall these data suggest this approach is unlikely to be broadly effective as a single agent in SWI/SNF or KDM6A-mutant cancers. In summary, MRTX2219 is a potent and orally bioactive EED inhibitor that represents a differentiated strategy to block PRC2 activity in selected cancers.