Olema Pharmaceuticals, Inc., a clinical-stage biopharmaceutical company focused on the discovery, development, and commercialization of targeted therapies for women’s cancers, announced the selection of a development candidate for the Company’s program targeting KAT6, an epigenetic target that is dysregulated in breast cancer and other cancers. The compound, named OP-3136, is an orally bioavailable, potent KAT6A/B-selective inhibitor developed by Olema in collaboration with Aurigene Oncology.
Olema presented data regarding the discovery and pre-clinical development of its KAT6 program in a poster session at the 2023 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics (ANE 2023) in Boston, Massachusetts. OP-3136 is orally bioavailable in multiple non-clinical species with desirable pharmacokinetics and has demonstrated highly selective and potent activity against KAT6A and KAT6B versus other KAT family members. In KAT6-amplified and overexpressing estrogen receptor-positive (ER+) breast cancer cell lines, OP-3136 strongly inhibited cell proliferation whereas KAT6-low cell lines were insensitive to the compounds. In a non-clinical xenograft model, OP-3136 caused dose-dependent tumor growth inhibition and tumor regression comparable to or better than a positive-control patented KAT6 inhibitor and demonstrated synergy in combination with CDK4/6 inhibitors or palazestrant (OP-1250).
Olema is initiating non-clinical Investigational New Drug (IND) enabling studies in order to support a potential IND submission to the FDA for OP-3136 by the end of 2024.