Olema Oncology Announces New Preclinical Data for OP-3136 Demonstrating Anti-Tumor Activity in Multiple Solid Tumor Models at AACR 2025
Olema Oncology (OLMA) has revealed promising preclinical data for OP-3136, their novel KAT6 inhibitor, demonstrating significant anti-tumor activity across multiple solid tumor types. The data, presented at AACR 2025, showed effectiveness in ovarian, prostate, and non-small cell lung cancer (NSCLC) models.
Key findings include potent anti-proliferative activity in various cell lines and notable results in xenograft models:
- OVCAR3 (ovarian) model showed sustained tumor regression over 28 days
- LCLC-97TM1 (NSCLC) model demonstrated tumor inhibition comparable to ribociclib
- 22Rv1 (prostate) model exhibited dose-dependent tumor growth inhibition
The company is currently recruiting patients for a Phase 1 trial of OP-3136 as both monotherapy and in combination regimens for multiple solid tumor types.
Olema Oncology (OLMA) ha presentato dati preclinici promettenti per OP-3136, il loro nuovo inibitore di KAT6, dimostrando un'attività antitumorale significativa in diversi tipi di tumori solidi. I dati, presentati all'AACR 2025, hanno evidenziato efficacia nei modelli di tumore ovarico, prostata e carcinoma polmonare non a piccole cellule (NSCLC).
I risultati principali includono una potente attività antiproliferativa in varie linee cellulari e risultati rilevanti nei modelli xenotrapiantati:
- Il modello OVCAR3 (ovaio) ha mostrato una regressione tumorale sostenuta per 28 giorni
- Il modello LCLC-97TM1 (NSCLC) ha evidenziato un’inibizione tumorale paragonabile a ribociclib
- Il modello 22Rv1 (prostata) ha mostrato un’inibizione della crescita tumorale dipendente dalla dose
L'azienda sta attualmente reclutando pazienti per uno studio di Fase 1 su OP-3136, sia come monoterapia sia in combinazione, per diversi tipi di tumori solidi.
Olema Oncology (OLMA) ha revelado datos preclínicos prometedores para OP-3136, su novedoso inhibidor de KAT6, demostrando una actividad antitumoral significativa en varios tipos de tumores sólidos. Los datos, presentados en AACR 2025, mostraron eficacia en modelos de cáncer de ovario, próstata y cáncer de pulmón no microcítico (NSCLC).
Los hallazgos clave incluyen una potente actividad antiproliferativa en diversas líneas celulares y resultados destacados en modelos xenoinjertados:
- El modelo OVCAR3 (ovario) mostró una regresión tumoral sostenida durante 28 días
- El modelo LCLC-97TM1 (NSCLC) demostró una inhibición tumoral comparable a ribociclib
- El modelo 22Rv1 (próstata) exhibió una inhibición del crecimiento tumoral dependiente de la dosis
La compañía está reclutando pacientes para un ensayo de Fase 1 de OP-3136, tanto en monoterapia como en regímenes combinados para varios tipos de tumores sólidos.
Olema Oncology (OLMA)는 새로운 KAT6 억제제인 OP-3136에 대한 유망한 전임상 데이터를 공개했으며, 여러 고형암 유형에서 뛰어난 항종양 활성을 보였습니다. 이 데이터는 AACR 2025에서 발표되었으며, 난소암, 전립선암, 비소세포폐암(NSCLC) 모델에서 효과가 확인되었습니다.
주요 결과는 다양한 세포주에서 강력한 항증식 활성과 이식편 모델에서의 주목할 만한 결과를 포함합니다:
- OVCAR3 (난소) 모델에서 28일간 지속적인 종양 퇴축 관찰
- LCLC-97TM1 (NSCLC) 모델에서 리보시클립과 유사한 종양 억제 효과 확인
- 22Rv1 (전립선) 모델에서 용량 의존적 종양 성장 억제 확인
회사는 현재 OP-3136의 단독 요법 및 병용 요법으로 여러 고형암 유형을 대상으로 하는 1상 임상시험에 환자를 모집 중입니다.
Olema Oncology (OLMA) a dévoilé des données précliniques prometteuses pour OP-3136, leur nouvel inhibiteur de KAT6, démontrant une activité antitumorale significative sur plusieurs types de tumeurs solides. Les données, présentées lors de l’AACR 2025, ont montré une efficacité dans des modèles de cancer de l’ovaire, de la prostate et du poumon non à petites cellules (NSCLC).
Les résultats clés incluent une puissante activité antiproliférative sur différentes lignées cellulaires et des résultats notables dans des modèles xénogreffes :
- Le modèle OVCAR3 (ovaire) a montré une régression tumorale soutenue pendant 28 jours
- Le modèle LCLC-97TM1 (NSCLC) a démontré une inhibition tumorale comparable à celle du ribociclib
- Le modèle 22Rv1 (prostate) a présenté une inhibition de la croissance tumorale dépendante de la dose
L’entreprise recrute actuellement des patients pour un essai de phase 1 d’OP-3136, en monothérapie ainsi qu’en association, pour plusieurs types de tumeurs solides.
Olema Oncology (OLMA) hat vielversprechende präklinische Daten zu OP-3136, ihrem neuartigen KAT6-Inhibitor, vorgestellt, die eine signifikante antitumorale Aktivität bei verschiedenen soliden Tumorarten zeigen. Die Daten, präsentiert auf der AACR 2025, zeigten Wirksamkeit in Modellen von Eierstock-, Prostata- und nicht-kleinzelligem Lungenkrebs (NSCLC).
Wesentliche Ergebnisse umfassen eine starke antiproliferative Wirkung in verschiedenen Zelllinien und bemerkenswerte Resultate in Xenotransplantatmodellen:
- Das OVCAR3 (Eierstock)-Modell zeigte eine anhaltende Tumorrückbildung über 28 Tage
- Das LCLC-97TM1 (NSCLC)-Modell zeigte eine Tumorhemmung vergleichbar mit Ribociclib
- Das 22Rv1 (Prostata)-Modell zeigte eine dosisabhängige Hemmung des Tumorwachstums
Das Unternehmen rekrutiert derzeit Patienten für eine Phase-1-Studie mit OP-3136 als Monotherapie sowie in Kombinationsregimen für verschiedene solide Tumorarten.
- Demonstrated sustained tumor regression in ovarian cancer models over 28 days
- Showed comparable efficacy to established drug ribociclib in NSCLC models
- Exhibited synergistic effects when combined with existing treatments
- Demonstrated activity independent of KAT6 amplification or overexpression
- Successfully expanded potential therapeutic applications beyond breast cancer
- Still in early Phase 1 trials with no human efficacy data available
- Results to preclinical models only
Insights
OP-3136 shows promising preclinical anti-tumor activity in multiple cancer types beyond breast cancer, expanding its potential therapeutic applications.
The preclinical data for Olema's OP-3136 represents a significant development in targeted oncology therapies. As a selective KAT6 inhibitor, this compound targets a specific epigenetic mechanism involved in cancer cell proliferation, with data showing efficacy across multiple challenging cancer types.
Particularly notable is the sustained tumor regression observed in ovarian cancer models throughout the 28-day study period. In oncology drug development, achieving regression (actual tumor shrinkage) rather than merely slowing growth is a higher bar that suggests potentially robust efficacy.
The compound demonstrates two clinically valuable characteristics: activity independent of KAT6 amplification/overexpression (suggesting broader patient applicability without requiring biomarker selection), and effectiveness in both monotherapy and combination settings. The synergistic effects when combined with ribociclib in NSCLC and docetaxel in prostate cancer models suggest rational combination strategies that could enhance therapeutic outcomes.
In the NSCLC model, OP-3136 showed tumor inhibition comparable to ribociclib (an established CDK4/6 inhibitor), providing a benchmark for its potential clinical relevance. The dose-dependent response observed in prostate cancer models further validates the compound's mechanism of action.
The ongoing Phase 1 trial across multiple solid tumor types represents the critical next step in determining whether these promising preclinical signals translate to human patients. This expansion beyond breast cancer into additional high-need indications significantly broadens the potential therapeutic applications of this compound.
Olema's expansion of OP-3136 into multiple cancer indications strategically broadens its market potential while still in early clinical development.
This preclinical data package substantially expands the potential value proposition for OP-3136 within Olema's pipeline. By demonstrating anti-tumor activity across ovarian, prostate, and lung cancer models, the company establishes scientific rationale for a multi-indication development strategy beyond its initial breast cancer focus.
The data reveals two particularly valuable development paths: as monotherapy in settings where OP-3136 showed robust single-agent activity (particularly in ovarian cancer with sustained regression), and in combination regimens where enhanced effects were observed (with ribociclib in NSCLC and docetaxel in prostate cancer).
KAT6 inhibition represents a differentiated mechanism of action in the oncology landscape. The demonstrated activity independent of target overexpression potentially eliminates the need for companion diagnostic development, which would streamline the regulatory pathway and broaden the eligible patient population.
From a strategic perspective, the parallel exploration of multiple solid tumor indications in early clinical development follows an efficient, data-driven approach that can accelerate identification of the most promising applications. This diversification across multiple cancer types effectively distributes clinical development risk rather than concentrating on a single indication.
While these results support the ongoing Phase 1 program, it's important to recognize that significant clinical development milestones remain ahead before potential commercialization. Nevertheless, this expansion beyond the company's initial breast cancer focus enhances the long-term commercial potential of OP-3136 by addressing multiple areas of high unmet need.
- 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: LB166
Session: Late-Breaking Research: Tumor Biology 2
Date/Time: April 28, 2025, from 9:00am-12:00pm CT / 10:00am-1:00pm ET
Presenter: 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-3136
OP-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 Oncology
Olema 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 Contact
Courtney O’Konek
Vice President, Corporate Communications
Olema Oncology
media@olema.com
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