8 minute read
Dec. 4, 2023

PF-9363: A First-in-Class KAT6A/B Epigenetic “Writer” Inhibitor for Breast Cancer


oral selective KAT6A/B inhibitor related PF-07248144 in Ph. I for ER+ HER2 breast cancer from HTS of 250k compound library Cell Chem. Biol., August 2023 Pfizer, CA/ Cancer Therapeutics, AU


PF-9363 (CTx-648) is a first-in-class, oral inhibitor of the KAT6A/B histone lysine acetyltransferases (HATs) for the treatment of ER+/luminal & KAT6A+ breast cancer discovered by Melbourne’s Cancer Therapeutics CRC (CTxT) and Pfizer, San Diego. This article discusses why the molecule is scientifically notable in drug discovery for epigenetic targets and transferable scientific insights from its decade-long KAT6 campaign including its target rationale, hit-finding and lead optimization, synthesis and relevant clinical data.



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