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

Anticipated Upcoming Events (GlobeNewswire) - "(i) Initiate enrollment in the Phase 1b/2 study evaluating OP-3136 in combination with darolutamide in mCRPC in collaboration with Bayer in the fourth quarter of 2026; (ii) Report top-line data from the pivotal Phase 3 OPERA-01 trial in the first quarter of 2027."

New P1/2 trial • P3 data: top line • Castration-Resistant Prostate Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Negative Breast Cancer

A phase 1, first-in-human study of OP-3136, a novel oral selective KAT6A/B inhibitor, as monotherapy in advanced solid tumors and in combination with endocrine therapy in ER+, HER2− advanced breast cancer (ABC): Preliminary results. (ASCO 2026) - P1 | "OP-3136 demonstrated a manageable safety profile and favorable PK, both as monotherapy and in combination with fulvestrant. Preliminary evidence of antitumor activity in ER+ HER2- ABC and mCRPC was observed in these heavily pretreated pts. Dose escalation and enrollment in combination with fulvestrant or palazestrant are ongoing and updated data will be presented."

Combination therapy • First-in-human • Metastases • Monotherapy • P1 data • Breast Cancer • Castration-Resistant Prostate Cancer • Estrogen Receptor Positive Breast Cancer • Genito-urinary Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Leukopenia • Lung Cancer • Neutropenia • Non Small Cell Lung Cancer • Oncology • Prostate Cancer • Solid Tumor • ER • HER-2 • KAT6A

OP-3136: “Preliminary safety from Part 1A of the Phase 1 study of OP-3136 in multiple solid tumor types”; Breast cancer (Olema Oncology) - Corporate Presentation: “OP-3136 monotherapy demonstrated tumor shrinkage in over 2/3 of patients across dose levels in various advanced solid tumor types”

P1 data • Breast Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Negative Breast Cancer • Oncology

Olema Oncology Announces Clinical Trial Collaboration and Supply Agreement with Bayer to Evaluate OP-3136 in Combination with NUBEQA (darolutamide) in Metastatic Castration-Resistant Prostate Cancer (The Manila Times) - "The Phase 1b/2 study is designed to assess the safety, tolerability, and preliminary anti-tumor activity of OP-3136 in combination with darolutamide in approximately 36 patients...expected to initiate in H2 2026."

Licensing / partnership • New P1/2 trial • Castration-Resistant Prostate Cancer

Olema Oncology Announces Encouraging Initial Clinical Data from the Phase 1 Study of OP-3136, a KAT6 Inhibitor, at 2026 ASCO Annual Meeting (GlobeNewswire) - "Among 19 response-evaluable patients across dose levels and tumor types, tumor shrinkage was observed in 13 patients; partial responses (PR) were observed in 3 patients with measurable disease, with 2 confirmed PRs and 1 unconfirmed PR. The longest duration of treatment is 62 weeks. 11 patients remain on treatment, including 9 with ABC and 2 with mCRPC....Pharmacokinetics: OP-3136 exhibited predictable, dose-proportional plasma exposure across all doses tested. At doses of 6 mg and above, steady-state concentrations exceeded efficacy targets based on preclinical models."

P1 data • PK/PD data • Castration-Resistant Prostate Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Negative Breast Cancer

Anticipated Upcoming Events: (Olema Oncology Press Release) - "Present initial clinical data from the Phase 1 study evaluating the safety, tolerability, pharmacokinetics, pharmacodynamics, and preliminary efficacy of OP-3136 in a poster presentation at the 2026 American Society of Clinical Oncology (ASCO) Annual Meeting...Present trial-in-progress poster for the ongoing pivotal Phase 3 OPERA-02 trial evaluating palazestrant in combination with ribociclib in frontline ER+/HER2- metastatic breast cancer at ASCO...Report top-line data from the pivotal Phase 3 OPERA-01 trial of palazestrant as a monotherapy in second- and third-line ER+/HER2- metastatic breast cancer in the fall of 2026."

P1 data • P3 data: top line • Trial status • Estrogen Receptor Positive Breast Cancer • HER2 Negative Breast Cancer

Phase 1 Study of OP-3136 in Advanced or Metastatic Solid Tumors (clinicaltrials.gov) - P1 | N=180 | Recruiting | Sponsor: Olema Pharmaceuticals, Inc. | N=48 ➔ 180

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 • ER • HER-2

Palazestrant, a CERAN, in combination with OP-3136, a KAT6 inhibitor, synergistically downregulates cell proliferation and metastasis related gene signatures (AACR 2026) - "The transcriptional changes align with enhanced anti-tumor efficacy and establish a mechanistic rationale for this combination over fulvestrant in ER+ breast cancer. The palazestrant–OP-3136 combination is currently being evaluated in a phase I clinical trial in ER+/HER2– metastatic breast cancer patients."

Combination therapy • Gene Signature • Breast Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • E2F1 • FOXA1 • GATA3 • HER-2 • KAT6A • KAT6B • TNFA

Olema Oncology to Present Initial Clinical Data for OP-3136 at the 2026 ASCO Annual Meeting (GlobeNewswire) - "Olema Oncology...will present initial clinical data from the Phase 1 study of OP-3136 in a poster presentation....The Company will also present a trial-in-progress poster for the Phase 3 OPERA-02 trial."

P1 data • Trial status • Estrogen Receptor Positive Breast Cancer • HER2 Negative Breast Cancer

Phase 1 Study of OP-3136 in Advanced or Metastatic Solid Tumors (clinicaltrials.gov) - P1 | N=48 | Recruiting | Sponsor: Olema Pharmaceuticals, Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • First-in-human • Breast Cancer • HER2 Breast Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Prostate Cancer • Solid Tumor • ER • HER-2

Title: Palazestrant, a CERAN, in combination with OP-3136, a KAT6 inhibitor, synergistically downregulates cell proliferation and metastasis related gene signatures (GlobeNewswire) - "Olema Oncology Announces Preclinical Data...at the 2026 AACR Annual Meeting....Combining OP-3136 with palazestrant drives synergistic anti-tumor activity in in vivo ER+/HER2- breast cancer models, which is mediated by suppression of cell-cycle and estrogen receptor-driven oncogenic signaling processes....Combining OP-3136 with palazestrant or fulvestrant suppresses expression of genes associated with MTORC1 signaling, indicating that targeting KAT6 and ER-alpha can suppress mechanisms of acquired resistance."

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

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 to Present Preclinical Data for Palazestrant and OP-3136 at the 2026 AACR Annual Meeting (GlobeNewswire)

Preclinical • Oncology

Anticipated Upcoming Events (GlobeNewswire) - "Report initial clinical results for OP-3136 in Q2 2026 at a major medical conference. Report top-line data from the pivotal Phase 3 OPERA-01 trial of palazestrant as a monotherapy in second- and third-line (2/3L) ER+/HER2- metastatic breast cancer in the fall of 2026."

First-in-human • P1 data • P3 data: top line • Castration-Resistant Prostate Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Negative Breast Cancer • Non Small Cell Lung Cancer

OP-3136-101: Phase 1 Study of OP-3136 in Advanced or Metastatic Solid Tumors (clinicaltrialsregister.eu) - P1 | N=42 | Not yet recruiting | Sponsor: Olema Pharmaceuticals Inc.

New P1 trial • Oncology • Solid Tumor

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

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