- Activity in preclinical models of ovarian, prostate, and non-small cell lung cancer supports potential utility of OP-3136, a KAT6 inhibitor, in indications beyond breast cancer
- Patient recruitment ongoing in Phase 1 trial of OP-3136 as a monotherapy and in combination regimens in multiple solid tumor types
- Data to be presented at 2025 AACR Annual Meeting
SAN FRANCISCO, April 25, 2025 (GLOBE NEWSWIRE) -- Olema Pharmaceuticals, Inc. (“Olema” or “Olema Oncology”, Nasdaq: OLMA), a clinical-stage biopharmaceutical company focused on the discovery, development, and commercialization of targeted therapies for breast cancer and beyond, today announced preclinical data demonstrating the anti-tumor activity of OP-3136, a novel small molecule that potently and selectively inhibits lysine acetyltransferase 6 (KAT6), in prostate, ovarian, and non-small cell lung cancer (NSCLC) models. These findings are being presented in a late-breaking poster session at the American Association for Cancer Research (AACR) Annual Meeting taking place April 25-30 in Chicago, Illinois.
“These data showcase the potential of OP-3136 for the treatment of challenging cancers beyond breast cancer,” said David C. Myles, Ph.D., Chief Discovery and Non-Clinical Development Officer of Olema Oncology. “OP-3136 has shown inhibition across all models explored, and we were excited to observe potent tumor growth inhibition and sustained tumor regression with OP-3136 as a monotherapy in ovarian cancer models. We are actively recruiting the Phase 1 trial of OP-3136 in multiple solid tumor types and will continue to explore its potential in other indications of high unmet need.”
Poster Presentation Details Title: OP-3136, a selective KAT6 inhibitor, demonstrates anti-tumor activity in prostate, ovarian, and non-small cell lung cancer preclinical models Poster/Abstract: LB166Session: Late-Breaking Research: Tumor Biology 2Date/Time: April 28, 2025, from 9:00am-12:00pm CT / 10:00am-1:00pm ETPresenter: Dr. Gopinath S. Palanisamy, DVM, Ph.D.
Key findings include:
- OP-3136 showed potent anti-proliferative activity in multiple ovarian, NSCLC, and prostate cell lines in vitro.
- OP-3136 showed activity that was independent of KAT6 amplification or over expression.
- OP-3136 monotherapy demonstrated anti-tumor activity in in vivo xenograft models of ovarian (OVCAR3), NSCLC (LCLC-97TM1), and prostate (22Rv1) cancers.
- In the OVCAR3 model, OP-3136 monotherapy demonstrated sustained tumor regression across the 28-day study period and robust tumor growth inhibition.
- In the LCLC-97TM1 model, OP-3136 monotherapy demonstrated tumor growth inhibition comparable to ribociclib and, when combined with ribociclib, demonstrated synergy and enhanced anti-tumor activity.
- In the 22Rv1 model, OP-3136 inhibited tumor growth in a dose-dependent manner and, when combined with docetaxel, resulted in enhanced anti-tumor activity.
- These data indicate OP-3136 may be effective in treating ovarian, lung, and prostate cancer indications in addition to breast cancer.
A copy of this poster is available on the Publications page of Olema’s website. Additional information can be found on the AACR Annual Meeting website, including abstracts.
About OP-3136OP-3136 is a novel, orally available small molecule that potently and selectively inhibits lysine acetyltransferase 6 (KAT6), an epigenetic target that is dysregulated in breast and other cancers. In preclinical studies, OP-3136 has demonstrated significant anti-proliferative activity in ER+ breast cancer models and is combinable and synergistic with endocrine therapies, including palazestrant and cyclin-dependent kinase 4/6 (CDK4/6) inhibitors. The Investigational New Drug (IND) application for OP-3136 was cleared by the U.S. Food and Drug Administration (FDA) in December 2024 and patients are currently enrolling in the Phase 1 clinical trial.
About Olema OncologyOlema Oncology is a clinical-stage biopharmaceutical company committed to transforming the standard of care and improving outcomes for patients living with breast cancer and beyond. Olema is advancing a pipeline of novel therapies by leveraging our deep understanding of endocrine-driven cancers, nuclear receptors, and mechanisms of acquired resistance. Our lead product candidate, palazestrant (OP-1250), is a proprietary, orally available complete estrogen receptor (ER) antagonist (CERAN) and a selective ER degrader (SERD), currently in a Phase 3 clinical trial called OPERA-01. In addition, Olema is developing OP-3136, a potent lysine acetyltransferase 6 (KAT6) inhibitor, now in a Phase 1 clinical trial. Olema is headquartered in San Francisco and has operations in Cambridge, Massachusetts. For more information, please visit www.olema.com.
Media and Investor Relations ContactCourtney O’KonekVice President, Corporate CommunicationsOlema Oncologymedia@olema.com
