Novel therapies targeting the bromodomain acetyltransferases

While treatment options in blood cancers like acute myeloid leukaemia (AML) and multiple myeloma (MM) continue to develop, there remains an unmet need for better, less toxic therapies. EP300 and CREBBP are paralogous genes coding for multi-domain acetyltransferases targeting diverse cellular proteins.

CCS1477 (inobrodib), an EP300/CBP bromodomain inhibitor, induces cell-cycle arrest and differentiation in haematologic malignancy models through disrupting EP300/CBP recruitment to enhancer networks occupied by critical transcription factors. In patients with relapsed/refractory disease, CCS1477 monotherapy induces differentiation responses in AML and objective responses in myeloma.