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Isosterix KAT6A-selective Inhibitor Summary

• Anti-tumor efficacy in ER+/HER2- Breast Cancer xenograft model as a single agent

• Strong anti-proliferative activity and inhibition of histone acetylation in ER+ breast cancer cell lines

• High oral bioavailability with excellent PK profile across preclinical species and prediction of human target dose

• Excellent in vitro safety profile

• High selectivity for KAT6A and over all HAT enzyme family members

• Demonstrated not genotoxic, in contrast to other epigenetic modifiers