OP-3136 / Olema Pharma, Dr. Reddy’s - LARVOL DELTA

Phase 1 Study of OP-3136 in Advanced or Metastatic Solid Tumors (clinicaltrials.gov) - P1 | N=160 | Recruiting | Sponsor: Olema Pharmaceuticals, Inc. | N=90 ➔ 160

Enrollment change • First-in-human • Breast Cancer • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Prostate Cancer • Solid Tumor

Olema Oncology Reports Second Quarter 2025 Financial and Operating Results (GlobeNewswire) - "Anticipated Upcoming Events:...Report initial clinical results for OP-3136 in 2026."

P1 data • Solid Tumor

OP-3136, a selective KAT6 inhibitor, demonstrates anti-tumor activity in prostate, ovarian, and non-small cell lung cancer preclinical models (AACR 2025) - "In the LCLC-97TM1 NSCLC xenograft model, monotherapy with OP-3136 at 1 mg/kg achieved a TGI of 62%. These findings highlight the potential of OP-3136 monotherapy to treat prostate, ovarian, and NSCLC tumors and strongly support expanding the clinical investigation of KAT6 inhibitors beyond ER+/HER2- breast cancer."

Late-breaking abstract • Preclinical • Breast Cancer • Estrogen Receptor Positive Breast Cancer • Genito-urinary Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Oral Cancer • Ovarian Cancer • Prostate Cancer • Solid Tumor • ER • HER-2 • KAT6A • KAT6B

Olema Oncology Announces New Preclinical Data for OP-3136 Demonstrating Anti-Tumor Activity in Multiple Solid Tumor Models at AACR 2025 (GlobeNewswire) - "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."

Preclinical • Breast Cancer • Non Small Cell Lung Cancer • Ovarian Cancer • Prostate Cancer

Olema Oncology Reports Fourth Quarter and Full Year 2024 Financial and Operating Results (GlobeNewswire) - "OP-3136 Phase 1 trial initiated before the end of 2024; patients now enrolling....Anticipated Upcoming Events:...Present new preclinical data for OP-3136."

Preclinical • Trial status • Solid Tumor

Olema Oncology to Present Preclinical Data for OP-3136, a Potent KAT6 Inhibitor, Demonstrating Anti-Tumor Activity in Multiple Solid Tumor Models at the 2025 AACR Annual Meeting (GlobeNewswire) - "Olema Pharmaceuticals...announced it will present a poster highlighting preclinical 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 models in a late-breaking session at the American Association for Cancer Research (AACR) Annual Meeting..."

Late-breaking abstract • Preclinical • Non Small Cell Lung Cancer • Ovarian Cancer • Prostate Cancer

Study of OP-3136 in Advanced or Metastatic Solid Tumors (clinicaltrials.gov) - P1 | N=90 | Recruiting | Sponsor: Olema Pharmaceuticals, Inc.

New P1 trial • Breast Cancer • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Prostate Cancer • Solid Tumor

Olema Oncology Announces FDA Clearance of Investigational New Drug Application for OP-3136, a Potent KAT6 Inhibitor (GlobeNewswire) - "Olema Pharmaceuticals, Inc...announced that the U.S. Food and Drug Administration (FDA) has cleared its Investigational New Drug (IND) application for OP-3136, a novel small molecule that potently and selectively inhibits KAT6, a validated epigenetic target that is dysregulated in breast and other cancers....Phase 1 clinical trial for OP-3136 to initiate in early 2025."

IND • New P1 trial • Breast Cancer

Olema Oncology Reports Third Quarter 2024 Financial Results and Provides Corporate Update (GlobeNewswire) - "Anticipated Upcoming Milestones :(i) Present updated Phase 2 data showing palazestrant in combination with ribociclib at the San Antonio Breast Cancer Symposium (SABCS) in December 2024; (ii) Submit the IND application for OP-3136 to the U.S. Food and Drug Administration (FDA) before year-end; initiate the Phase 1 clinical study for OP-3136 in early 2025."

IND • New P1 trial • P2 data • Estrogen Receptor Positive Breast Cancer • HER2 Negative Breast Cancer

Olema Oncology Presents Compelling New Preclinical Data Demonstrating Anti-Tumor Activity for OP-3136 with Enhanced Activity of Palazestrant Combinations at ENA 2024 (GlobeNewswire) - "Olema Pharmaceuticals...announced results...presented during poster sessions at the 36th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics (ENA 2024)....'We look forward to submitting our Investigational New Drug (IND) application for OP-3136 to the US Food and Drug Administration before the end of this year'; Abstract: 230:...Key findings include:...OP-3136 led to either tumor growth inhibition or tumor regression in vivo in xenograft models across all treatment groups. In combination with OP-3136, palazestrant was consistently superior to fulvestrant and led to improved anti-tumor activity and tumor regression. OP-3136 showed robust synergistic anti‑tumor activity when combined with fulvestrant or palazestrant as doublet therapy in breast cancer models."

IND • Preclinical • Estrogen Receptor Positive Breast Cancer • HER2 Negative Breast Cancer

Combining OP-3136, a KAT6 inhibitor, with endocrine therapy and CDK4/6 inhibitor enhances anti-tumor activity in ER+/HER2- breast cancer models (EORTC-NCI-AACR 2024) - "In mouse xenograft studies, OP-3136 showed enhanced, statistically significant tumor growth inhibition with both double and triple combinations involving palazestrant and ribociclib. Notably, the efficacy observed for OP-3136 in combination with palazestrant was statistically superior to that observed for OP-3136 in combination with fulvestrant.OP-3136 displayed favorable combinability with palazestrant and ribociclib across multiple preclinical models, indicating the promise of this drug regimen for the treatment of ER+/HER2- breast cancer patients."

Preclinical • Breast Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • ER • HER-2 • KAT6A • KAT6B

Olema Oncology Announces New Preclinical Combination Data to be Presented at the 2024 EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics (GlobeNewswire) - "Olema Pharmaceuticals...announced that it will be presenting multiple posters during the 36th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics (ENA 2024)....Poster presentations include new preclinical data demonstrating activity for palazestrant in combination with capivasertib and everolimus, and OP-3136, Olema’s KAT6 inhibitor, in combination with palazestrant and other targeted agents."

Preclinical • Estrogen Receptor Positive Breast Cancer • HER2 Negative Breast Cancer

Olema Oncology Reports Fourth Quarter and Full-Year 2023 Financial Results and Provides Corporate Update (GlobeNewswire) - "Upcoming Milestones: Initiated OPERA-01 pivotal Phase 3 monotherapy trial in Q4 2023; top-line results expected in 2026; File an Investigational New Drug, or IND, application with the FDA for OP-3136, a KAT6 inhibitor, in late 2024, and advance clinical development; Prepare for pivotal Phase 3 first-line trial in combination with CDK4/6 inhibitor, ribociclib."

IND • New P3 trial • P3 data • Breast Cancer • Estrogen Receptor Positive Breast Cancer • Oncology • Solid Tumor

Olema Oncology Nominates OP-3136, an Orally Bioavailable KAT6 Inhibitor, as a Development Candidate (GlobeNewswire) - "Olema Pharmaceuticals...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 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."

IND • Pipeline update • Breast Cancer

Olema Oncology KAT6 Inhibitor Compounds Demonstrate Potent Anti-Tumor Activity (GlobeNewswire) - "Olema Pharmaceuticals, Inc...today announced new preclinical data regarding the discovery of novel compounds targeting KAT6....These data will be presented today at a poster session at the 2023 AACR-NCI-EORTC....Olema KAT6 compounds were selective and potent against KAT6A and KAT6B (250-fold selectivity over other KAT family members, including the essential genes KAT5 and KAT8. In KAT6-amplified and overexpressing breast cancer cell lines, Olema KAT6 compounds strongly inhibited cell proliferation whereas KAT6-low cell lines were insensitive to the compounds. Olema KAT6 inhibitor compounds caused dose-dependent tumor growth inhibition and tumor regression comparable to or better than a positive-control patented KAT6 inhibitor....Olema KAT6 inhibitor compounds demonstrate histone target engagement and efficacy, as well as synergism with palbociclib or palazestrant (OP-1250)."

Preclinical • Breast Cancer • Oncology • Solid Tumor

Olema Oncology Announces New Preclinical KAT6 Inhibitor Data to be Presented at the 2023 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics (GlobeNewswire) - "Olema Pharmaceuticals, Inc...announced a poster presentation on new discovery compounds targeting KAT6, an epigenetic target that is dysregulated in breast and other cancers. The poster, demonstrating the activity of Olema’s KAT6 inhibitors, will be presented at the 2023 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics (ANE 2023) taking place October 11-15, 2023, in Boston, Massachusetts."

Preclinical • Breast Cancer • Estrogen Receptor Positive Breast Cancer • Oncology • Solid Tumor