The discovery and development of new histone lysine acetyltransferase KAT6 inhibitors is a significant advancement in the management of breast cancer. Investigators from Olema Pharmaceuticals Inc. and Aurigene Oncology Ltd. recently presented data for their KAT6 inhibitor, OP-3136, as an approach for breast cancer.

KAT6 is a histone lysine acetyl transferase involved in the epigenetic regulation of oncogenes and it is often dysregulated in cancer, including breast cancer. Inhibiting KAT6 blocks the transcription of genes such as ESR1 and CCND1 and the use of KAT6 inhibitors together with endocrine therapy and CDK4/6 inhibitor therapy may enhance the effectiveness in cancer.

Olema Pharmaceuticals Inc. has advanced its program targeting KAT6, an epigenetic target dysregulated in breast and other cancers, with the selection of a development candidate, OP-3136. The orally bioavailable, potent KAT6A/B-selective inhibitor has been developed by Olema in collaboration with Aurigene Oncology Ltd.