MEN2312

MEN2312 is a potent and selective orally bioavailable small molecule inhibitor of lysine acetyltransferase 6A (KAT6A) and KAT6B, members of the MYST family of histone acetyltransferases. These enzymes acetylate histone H3K23 and non-histone proteins such as p53, playing an oncogenic role in several tumor types. In breast cancer, KAT6A is frequently amplified or overexpressed. By inhibiting KAT6A/B, MEN2312 blocks estrogen receptor (ER) activity at the transcriptional level, potentially overcoming resistance to endocrine therapies due to mutation or ligand-independent constitutive activation of ER. The drug is being developed for use as monotherapy and in combination with standard-of-care treatments for advanced/metastatic ER-positive/HER2-negative breast cancer[5][3][4]. It was also previously under development for acute myeloid leukemia[2].

Other names

KAT6A inhibitorKAT-6A inhibitorKAT 6A inhibitorInsilico Medicine KAT6A inhibitor