Olema Oncology Nominates OP-3136, an Orally Bioavailable KAT6 Inhibitor, as a Development Candidate
10 Jan 2024
AACRExecutive Change
OP-3136 demonstrated potent anti-tumor activity alone and in combination with both palazestrant and CDK4/6 inhibitors in preclinical ER+ breast cancer models
Initiating IND-enabling studies with goal to advance into clinical development by end of 2024
Jan. 08, 2024 -- Olema Pharmaceuticals, Inc. (“Olema”, “Olema Oncology”, Nasdaq: OLMA), a clinical-stage biopharmaceutical company focused on the discovery, development, and commercialization of targeted therapies for women’s cancers, today 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.
“We are excited to advance our KAT6 program with the nomination of OP-3136 as a development candidate. OP-3136 has the potential to become a new targeted therapy for breast cancer and other cancers,” said Dr. David C. Myles, Ph.D., Chief Discovery and Non-Clinical Development Officer of Olema Oncology. “Our KAT6 program supports our commitment to discovering and developing new treatment options for women living with cancer and is a natural complement to Olema’s ongoing development of palazestrant in ER+/HER2- breast cancer. We look forward to providing future updates on our progress with OP-3136 development.”
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 U.S. Food and Drug Administration (FDA) for OP-3136 by the end of 2024.
About Olema Oncology
Olema Oncology is a biopharmaceutical company committed to transforming the standard of care and improving outcomes for women living with cancer. Olema is advancing a pipeline of novel therapies by leveraging our deep understanding of endocrine-driven cancers, nuclear receptors, and mechanisms of acquired resistance. In addition to our lead product candidate, palazestrant (OP-1250), a proprietary, orally-available complete estrogen receptor (ER) antagonist (CERAN) and a selective ER degrader (SERD), Olema is developing a potent KAT6 inhibitor. Olema is headquartered in San Francisco and has operations in Cambridge, Massachusetts. For more information, please visit us at www.olema.com.
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