ARTICLE | Distillery Techniques


November 6, 2017 7:54 PM UTC

Tumor levels of SMARCA2 RNA could help predict responses to EZH2 inhibitors in cancers harboring mutations in the SWI/SNF complex. In 20 human ovarian, lung, gastrointestinal and other cancer cell lines with mutations in AT rich interactive domain 1A (ARID1A), SMARCB1 (SNF5; INI1), SMARCA4 (BRG1) or other components of the SWI/SNF complex, low SMARCA2 RNA levels correlated with sensitivity to the EZH2 inhibitor tazemetostat, as measured by cell proliferation. In a xenograft mouse model of ovarian cancer harboring a SMARCA4 mutation, low tumor levels of SMARCA2 RNA correlated with sensitivity to tazemetostat, as measured by tumor growth. Next steps by the Genentech Inc. unit of Roche include identification of additional biomarkers that predict sensitivity to epigenetic drugs.

Epizyme Inc. and Eisai Co. Ltd. have tazemetostat (E7438; EPZ-6438) in Phase II testing for B cell lymphoma, lymphoma, mesothelioma, sarcoma, solid tumors and non-Hodgkin's lymphoma (NHL)...