A Phase 3 Randomized, Double-Blind, Active-Controlled Study of Palazestrant With Ribociclib Versus Letrozole With Ribociclib for the First-Line Treatment of ER+, HER2- Advanced Breast Cancer (OPERA-02)

This phase 3 clinical trial compares the efficacy and safety of palazestrant with ribociclib to letrozole and ribociclib in women and men who have not received prior systemic anti-cancer treatment for advanced breast cancer.

开始日期2025-11-03

申办/合作机构

Olema Pharmaceuticals, Inc.

[+1]

NCT06784193

/ Recruiting临床1期

A Phase 1 First-in-Human, Open-Label, Multicenter Study of OP-3136 in Adult Participants With Advanced or Metastatic Solid Tumors

This is a first-in-human, open-label, multicenter phase 1 study to evaluate safety, tolerability, pharmacokinetics (PK), pharmacodynamics (PD), and preliminary efficacy of OP-3136, a lysine acetyltransferases 6A and 6B (KAT6A/B) inhibitor, as monotherapy and in combination with other anticancer agents in participants with advanced solid tumors.
This study consists of 2 parts: a dose escalation part (Part 1) and dose expansion part (Part 2).

开始日期2024-12-16

申办/合作机构

Olema Pharmaceuticals, Inc.

NCT06016738

/ Recruiting临床3期

A Phase 3 Randomized, Open-Label Study of OP-1250 Monotherapy vs Standard of Care for the Treatment of ER+, HER2- Advanced or Metastatic Breast Cancer Following Endocrine and CDK 4/6 Inhibitor Therapy (OPERA-01)

This phase 3 clinical trial compares the safety and efficacy of palazestrant (OP-1250) to the standard-of-care options of fulvestrant or an aromatase inhibitor in women and men with breast cancer whose disease has advanced on one endocrine therapy in combination with a CDK4/6 inhibitor.

开始日期2023-11-16

申办/合作机构

Olema Pharmaceuticals, Inc.

100 项与 Palazestrant 相关的临床结果

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100 项与 Palazestrant 相关的转化医学

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100 项与 Palazestrant 相关的专利（医药）

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项与 Palazestrant 相关的文献（医药）

2025-06-10·ACS Omega

Discovery of Palazestrant (OP-1250), a Potent and Orally Bioavailable Complete Estrogen Receptor Antagonist (CERAN) and Selective Estrogen Receptor Degrader (SERD)

Article

作者: Rich, Brian ; Yu, Guijun ; Kushner, Peter J. ; Peña, Guadalupe ; Phukan, Samiron ; Hodges-Gallagher, Leslie ; Sapugay, Judevin ; Chawla, Reena ; Andersen, Samuel E. ; Millikin, Robert ; Sun, Richard ; Parisian, Alison ; Zhou, Fei ; Duncan, Alexis ; Wang, Chenbo ; Zak, David R. ; Hearn, Brian R. ; Barratt, Susanna ; Ng, Raymond A. ; Satish Kher, Samir ; Fanning, Sean W. ; Watanabe, Teruki ; Myles, David C. ; Palanisamy, Gopinath S. ; Yeghikyan, David ; Thangathirupathy, Srinivasan ; Robello, Brandon ; Greene, Geoffrey ; Harmon, Cyrus L. ; Heerding, Dirk A.

Metastatic breast cancer (mBC) is a leading cause of cancer death in women. Most breast cancer patients are administered estrogen-receptor-targeted endocrine therapies to treat or prevent progressive metastatic disease. Development of endocrine resistance through acquisition of mutations in the estrogen receptor gene, ESR1, that constitutively activate the estrogen receptor leads to relapse. Complete antagonism of both WT and mutant ESR1 (mutESR1) with an oral therapeutic that persistently antagonizes ER-driven oncogenic transcriptional activities is a requirement for efficacy. Here, we describe our discovery of the investigational drug OP-1250 (palazestrant). OP-1250 is a potent complete estrogen receptor antagonist (CERAN) and selective estrogen receptor degrader (SERD) that is active in both WT and mutESR1 breast cancer tumors. OP-1250's effective induction of tumor regression either as a single agent or in combination with a CDK4/6 inhibitor has led to the rapid advancement of this compound into a Phase 3 clinical trial (OPERA-01).

2024-03-04·Molecular cancer therapeutics

Palazestrant (OP-1250), A Complete Estrogen Receptor Antagonist, Inhibits Wild-type and Mutant ER-positive Breast Cancer Models as Monotherapy and in Combination

Article

作者: Barratt, Susanna A ; Sun, Richard ; Peña, Guadalupe ; Hodges-Gallagher, Leslie ; Myles, David C ; Ortega, Fabian E ; Parisian, Alison D ; Palanisamy, Gopinath S ; Kulp, David ; Robello, Brandon ; Kushner, Peter J ; Harmon, Cyrus L ; Sapugay, Judevin

Abstract:

The estrogen receptor (ER) is a well-established target for the treatment of breast cancer, with the majority of patients presenting as ER-positive (ER+). Endocrine therapy is a mainstay of breast cancer treatment but the development of resistance mutations in response to aromatase inhibitors, poor pharmacokinetic properties of fulvestrant, agonist activity of tamoxifen, and limited benefit for elacestrant leave unmet needs for patients with or without resistance mutations in ESR1, the gene that encodes the ER protein. Here we describe palazestrant (OP-1250), a novel, orally bioavailable complete ER antagonist and selective ER degrader. OP-1250, like fulvestrant, has no agonist activity on the ER and completely blocks estrogen-induced transcriptional activity. In addition, OP-1250 demonstrates favorable biochemical binding affinity, ER degradation, and antiproliferative activity in ER+ breast cancer models that is comparable or superior to other agents of interest. OP-1250 has superior pharmacokinetic properties relative to fulvestrant, including oral bioavailability and brain penetrance, as well as superior performance in wild-type and ESR1-mutant breast cancer xenograft studies. OP-1250 combines well with cyclin-dependent kinase 4 and 6 inhibitors in xenograft studies of ER+ breast cancer models and effectively shrinks intracranially implanted tumors, resulting in prolonged animal survival. With demonstrated preclinical efficacy exceeding fulvestrant in wild-type models, elacestrant in ESR1-mutant models, and tamoxifen in intracranial xenografts, OP-1250 has the potential to benefit patients with ER+ breast cancer.

BREAST CANCER RESEARCH

Palazestrant, a novel oral Complete Estrogen Receptor Antagonist (CERAN) and Selective Estrogen Receptor Degrader (SERD), in patients with ER+/HER2− advanced or metastatic breast cancer: phase 1/2 study results

Article

作者: Patel, Manish R ; Shilkrut, Mark ; Shaw, Morena ; McCarthy, Nicole ; Hamilton, Erika P ; Tonda, Margaret ; Meisel, Jane L ; Borges, Virginia F ; Conlin, Alison K ; Okera, Meena ; Wesolowski, Robert ; Miller, Kathy D ; Pluard, Timothy J ; Lin, Nancy U ; Sabanathan, Dhanusha ; Alemany, Carlos A

Abstract:

Background:

Endocrine resistance is a major challenge in treating patients with ER+ /HER2− metastatic breast cancer (MBC) necessitating a switch from endocrine therapy to more toxic therapies. Mutations in ESR1 constitute a key mechanism of resistance to endocrine therapy in ER+ /HER2− BC. Therapies that overcome endocrine resistance are needed. Palazestrant is a novel oral complete estrogen receptor (ER) antagonist (CERAN) and selective ER degrader (SERD) belonging to a new class of ER-targeting agents that completely blocks estrogen-induced transcriptional activity, regardless of ESR1 mutation status. This first-in-human, open-label, multicenter, phase 1/2 dose-escalation/expansion study was designed to determine the recommended phase 2 dose (RP2D) and to evaluate safety, pharmacokinetics, and antitumor activity of palazestrant in patients with ER+ /HER2− MBC with disease progression on prior treatment.

Methods:

Adults with ER+ /HER2‒ MBC who received ≥ 1 prior line of endocrine therapy for advanced disease and ≤ 2 prior chemotherapy regimens for metastatic disease were eligible. Patients received once-daily oral palazestrant (30–300 mg) in 28-day cycles until progression or intolerable toxicity.

Results:

This study enrolled 146 patients. No dose-limiting toxicities were observed at doses up to 300 mg/day palazestrant. Confirmed partial responses were observed with 60 and 120 mg/day palazestrant. Both doses showed similar and tolerable safety profiles, favorable pharmacokinetics, and steady-state plasma concentrations above the predicted threshold for complete ER inhibition. Greater clinical benefit at palazestrant 120 mg/day (46%) versus 60 mg/day (19%) led to selection of 120 mg/day as RP2D and study expansion dose. At 120 mg/day, the median progression-free survival was 4.8 months (95% CI, 3.5–7.1) overall and 5.6 months (95% CI, 4.8–NE) among patients with cancers with ESR1 mutations. Most treatment-emergent adverse events (TEAEs) were grade 1–2. The most common TEAEs were nausea (62.8%), vomiting (29.1%), and fatigue (25.6%). The most common grade ≥ 3 TEAE was transient neutropenia (10.5%) managed by dose interruption and reduction.

Conclusions:

Palazestrant demonstrated a manageable safety profile, with antitumor activity observed in patients with heavily pretreated cancers with wild-type and ESR1-mutated BC. These data support the ongoing phase 3 study evaluating palazestrant in patients with ER+ /HER2 − MBC.

Trial registration:

ClinicalTrials.gov, NCT04505826. Registered August 6, 2020.

109

项与 Palazestrant 相关的新闻（医药）

2025-11-19

·GlobeNewswire-Health Care

Olema Oncology Announces Pricing of $190.0 Million Public Offering of Common Stock

SAN FRANCISCO, Nov. 19, 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 the pricing of an underwritten public offering of 10,000,000 shares of its common stock at a price to the public of $19.00 per share. All of the shares in the offering are to be sold by Olema. The gross proceeds to Olema from the offering, before deducting underwriting discounts and commissions and estimated offering expenses, are expected to be approximately $190.0 million. In addition, Olema has granted the underwriters a 30-day option to purchase up to an additional 1,500,000 shares of common stock at the public offering price, less underwriting discounts and commissions. The offering is expected to close on November 20, 2025, subject to the satisfaction of customary closing conditions. TD Cowen, Evercore ISI, Guggenheim Securities, LifeSci Capital, Oppenheimer & Co. and H.C. Wainwright & Co. are acting as book-running managers for the offering. The offering is being made pursuant to a shelf registration statement on Form S-3, including a base prospectus, that was filed with the Securities and Exchange Commission (the “SEC”) on January 6, 2025 and declared effective on January 15, 2025. A preliminary prospectus supplement and accompanying prospectus relating to the proposed offering was filed with the SEC and is available for free on the SEC’s website located at http://www.sec.gov. A final prospectus supplement and accompanying prospectus relating to the proposed offering will be filed with the SEC and will be available for free on the SEC’s website located at http://www.sec.gov. Copies of the final prospectus supplement and the accompanying prospectus relating to the offering may be obtained, when available from: TD Securities (USA) LLC, c/o Broadridge Financial Solutions, 1155 Long Island Avenue, Edgewood, NY 11717 or by email at TDManualrequest@broadridge.com. This press release shall not constitute an offer to sell or a solicitation of an offer to buy, nor shall there be any sale of these securities in any state or jurisdiction in which such offer, solicitation or sale would be unlawful prior to registration or qualification under the securities laws of any such state or jurisdiction. 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 its deep understanding of endocrine-driven cancers, nuclear receptors, and mechanisms of acquired resistance. Olema’s lead product candidate, palazestrant (OP-1250), is a proprietary, orally available complete estrogen receptor antagonist (CERAN) and a selective ER degrader (SERD), currently in two Phase 3 clinical trials. In addition, Olema is developing OP-3136, a potent lysine acetyltransferase 6 (KAT6) inhibitor, now in a Phase 1 clinical study. Olema is headquartered in San Francisco and has operations in Cambridge, Massachusetts. Forward-Looking StatementsStatements contained in this press release regarding matters that are not historical facts are “forward-looking statements” within the meaning of Section 27A of the Securities Act of 1933 and Section 21E of the Securities Exchange Act of 1934. Words such as “anticipate,” “expect,” “may,” “plan,” “will,” and similar expressions (as well as other words or expressions referencing future events, conditions or circumstances) are intended to identify forward-looking statements. These statements include, among others, statements regarding the expected timing and completion of the offering and gross proceeds expected to be received from the offering. Because such statements deal with future events and are based on Olema’s current expectations, they are subject to various risks and uncertainties, and actual results, performance or achievements of Olema could differ materially from those described in or implied by the statements in this press release. These forward-looking statements are subject to risks and uncertainties, including, without limitation, those discussed in the section titled “Risk Factors” in Olema’s Quarterly Report on Form 10-Q for the quarter ended September 30, 2025, the prospectus supplement related to the offering and other filings and reports that Olema makes from time to time with the SEC. Except as required by law, Olema assumes no obligation to update these forward-looking statements, including in the event that actual results differ materially from those anticipated in the forward-looking statements. Media and Investor Relations ContactCourtney O’KonekVice President, Corporate CommunicationsOlema Oncologymedia@olema.com

临床1期临床3期

2025-11-19

·雪球

Olema oncology:专注于乳腺癌疗法的biotech

$Olema(OLMA)$01公司简介OlemaPharmaceuticals是一家专注于开发女性癌症（特别是乳腺癌）靶向疗法的临床阶段生物制药公司。2006年8月公司在美国特拉华州以"CombiThera"之名成立。2009年3月25日更名为OlemaPharmaceuticals。2020年11月19日首次公开募股（IPO），发行价19美元，募资约2.09亿美元。02研发管线Olema公司的战略核心是围绕两大候选药物，致力于解决女性癌症治疗中的未满足需求：1.主打候选药物：Palazestrant(OP-1250)这是一种新型的、口服的小分子药物，具有完全雌激素受体拮抗剂（CERAN）和选择性雌激素受体降解剂（SERD）的双重活性。它旨在用于治疗雌激素受体阳性（ER+）、人表皮生长因子受体2阴性（HER2-）的乳腺癌。目前，该药物正在进行针对转移性乳腺癌的III期临床试验。2.其他研发管线：OP-3136这是一款有效的KAT6抑制剂，目前处于I期临床试验阶段，主要用于治疗ER+/HER2-转移性乳腺癌及其他癌症。关于乳腺癌全球ER+/HER2-转移性乳腺癌市场蕴含着200亿美元以上的机会。70%的乳腺癌患者是雌激素受体阳性/HER2阴性。针对一线ER+/HER2-的临床试验为OPERA-02，针对二线ER+/HER2-的临床试验为OPERA-01。Palazestrant（OP-1250）有可能成为转移性乳腺癌一线内分泌治疗的best-in-class药物。Palazestrant是ER受体的完全拮抗剂，对ESR1正常型和野生型肿瘤都有活性。并且具有良好的耐受性和口服给药的最优药代动力学特性。当前一线治疗为芳香化酶抑制剂（AI）+CDK4/6抑制剂，2/3线治疗为内分泌治疗(ET)+CDK4/6i,ET+mTORi,orAKTiorPI3Ki，3线后为化疗或ADC。Palazestrant联合ribociclib有可能成为1LER+/HER2-MBC的新标准治疗方案。Palazestrant单药治疗2/3线ER+/HER2-乳腺癌，预计于2027年NDA。OP-3136有可能创造更多价值，并对转移性乳腺癌的治疗格局产生重大影响。Palazestrant作用机制：拮抗剂+降解剂致癌因子EGFR，mTOR等与激活因子1（AF1）结合，雌二醇可以和激活因子2（AF2）结合来激活雌激素受体，从而启动增值基因的转录。选择性雌激素受体调节剂/降解剂（SERM/SERDs）一般作用于AF2，并使AF2失活。但是AF1的激活仍旧会导致增值基因的转录。Palazestrant不仅是完全的雌激素受体拮抗剂（CERAN），它也可以通过招募核受体辅阻遏物（N-CoR）来作为选择性雌激素受体降解剂。从而完全抑制雌激素受体的活性。Palazestrant能完全抑制雌激素受体，并提供更优的治疗药物浓度。临床试验Palazestrant联合ribociclib在1LER+/HER2-MBC中的临床设计安全性良好，无剂量限制毒性。120mg剂量患者总体mPFS为15.5个月，CDK4/6i+ET经治患者的mPFS为12.2个月。显著优于现有标准治疗（5个月）。在ESR1突变型和野生型2L+患者中均显示出活性Palazestrant联合ribociclib在既往接受过CDK4/6抑制剂治疗的2L+患者中显示出良好的活性。3期临床设计Palazestrant单药在2/3LER+/HER2-MBC中的临床设计安全性：Palazestrant耐受性良好，大多数治疗相关不良事件为1/2级有效性：在符合EMERALD研究条件的2/3线化疗后患者中，ESR1突变型患者的中位无进展生存期为7.3个月；野生型患者为5.5个月Palazestrant是唯一一种在ESR1突变型和野生型中均有获批潜力的CERAN/SERD类药物。OPERA-013期临床设计OP-3136:KAT6inhibitor作用机制：KAT6是一个经过临床验证的靶点，其过度表达与雌激素受体阳性（ER+）乳腺癌的不良临床结局相关。KAT6抑制可下调参与雌激素受体信号传导及其他信号通路的基因。这种抑制通过阻断组蛋白的乙酰化来调节基因表达。OP-3136对其他必需的KAT家族成员（KAT5和KAT8）显示出超过500倍的选择性。OP-3136对KAT5和KAT8的选择性更高，可能带来安全性优势。PF-81445每日一次给药达到稳态时的暴露量约为3000-4000纳摩尔，高于KAT5和KAT8的IC50值。OP-3136一期临床设计04里程碑Palazestrant：OPERA-01三期试验有望在2026年下半年获得顶线数据。OPERA-02三期试验与ribociclib联合用药，现已开始招募患者。预计2027年获得美国批准并上市，2029年扩大适应症。OP-3136：1期研究现已招募患者预计2026年获得初步数据

临床2期ASH会议临床3期siRNA

2025-11-10

·GlobeNewswire-Health Care

Olema Oncology Reports Third Quarter 2025 Financial and Operating Results

Announced new clinical trial agreement with Pfizer to evaluate palazestrant in combination with atirmociclib in ER+/HER2- metastatic breast cancerInitiated OPERA-02 Phase 3 trial of palazestrant in combination with ribociclib in frontline ER+/HER2- metastatic breast cancerPresented compelling new data from Phase 1b/2 study of palazestrant plus ribociclib at ESMO 2025Ended the quarter with $329.0 million in cash, cash equivalents, and marketable securities SAN FRANCISCO, Nov. 10, 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 reported financial and operating results for the third quarter ended September 30, 2025. "We have made significant progress advancing our programs this quarter, highlighted by the initiation of the Phase 3 OPERA-02 trial evaluating palazestrant in combination with ribociclib in the frontline setting and the presentation of compelling data at ESMO that further positions palazestrant to become a potential best-in-class backbone endocrine therapy for ER+/HER2- metastatic breast cancer,” said Sean P. Bohen, M.D., Ph.D., President and Chief Executive Officer of Olema Oncology. “Our clinical trial agreement with Pfizer to combine palazestrant with atirmociclib further underscores our confidence in palazestrant’s activity in combination with other agents in the metastatic setting.” Bohen continued, “Enrollment in the OPERA-01 trial evaluating palazestrant as a monotherapy in second- and third-line ER+/HER2- metastatic breast cancer continues to progress well and we remain on track for top-line data in the second half of next year. The Phase 1/2 study of our KAT6 inhibitor, OP-3136, recently expanded into combinations with fulvestrant and palazestrant and continues to benefit from strong investigator interest. As we look ahead to 2026, we remain focused on sustaining positive momentum across the business, transforming the breast cancer treatment paradigm, and bringing palazestrant to market.” Recent Progress Announced a clinical trial collaboration and supply agreement with Pfizer to evaluate the safety and combinability of palazestrant plus atirmociclib, Pfizer’s investigational, highly selective-CDK4 inhibitor, in a Phase 1b/2 study in patients with estrogen receptor-positive, human epidermal growth factor receptor 2-negative (ER+/HER2-) metastatic breast cancer.Initiated the OPERA-02 Phase 3 trial of palazestrant in combination with ribociclib in frontline ER+/HER2- metastatic breast cancer.Presented updated data from the Phase 1b/2 study of palazestrant plus ribociclib at the European Society for Medical Oncology (ESMO) Congress 2025, demonstrating encouraging activity in both ESR1 mutant and wild-type patients.Continued enrollment in the OPERA-01 Phase 3 trial of palazestrant as a monotherapy in second- and third-line ER+/HER2- metastatic breast cancer.Advanced the Phase 1 study evaluating the safety, tolerability, pharmacokinetics, pharmacodynamics, and preliminary efficacy of OP-3136, as a monotherapy and in combination with fulvestrant and palazestrant, in participants with advanced solid tumors. Anticipated Upcoming Events Initiate the Phase 1b/2 study evaluating palazestrant with atirmociclib in ER+/HER2- metastatic breast cancer in Q4 2025.Present trial-in-progress poster entitled “OPERA-02: a phase 3 randomized, double-blind, active-controlled study of palazestrant with ribociclib versus letrozole with ribociclib for the first-line treatment of ER+, HER2- advanced breast cancer” at the San Antonio Breast Cancer Symposium (SABCS) in December 2025.Report initial clinical results for OP-3136 in mid-2026.Report top-line data from OPERA-01 in the second half of 2026. Third Quarter 2025 Financial ResultsCash, cash equivalents, and marketable securities of $329.0 million as of September 30, 2025. Net loss for the quarter ended September 30, 2025 was $42.2 million, as compared to $34.6 million for the quarter ended September 30, 2024. The increase in net loss for the third quarter was primarily related to increased spending on research and development activities as a result of the ongoing late-stage clinical trials for palazestrant and the advancement of OP-3136, partially offset by higher interest income earned from marketable securities. GAAP research and development (R&D) expenses were $40.0 million for the quarter ended September 30, 2025, as compared to $33.2 million for the quarter ended September 30, 2024. The increase in R&D expenses was primarily related to increased spending on clinical development-related activities as Olema continues to advance palazestrant through late-stage clinical trials, and the advancement of OP-3136, partially offset by decreases in stock-based compensation expense of $1.7 million. Non-GAAP R&D expenses were $37.4 million for the quarter ended September 30, 2025, excluding $2.6 million non-cash stock-based compensation expense. Non-GAAP R&D expenses were $28.9 million for the quarter ended September 30, 2024, which excluded $4.3 million non-cash stock-based compensation expense. A reconciliation of GAAP to non-GAAP financial measures used in this press release can be found at the end of this press release. GAAP general and administrative (G&A) expenses were $5.9 million for the quarter ended September 30, 2025, as compared to $4.4 million for the quarter ended September 30, 2024. The increase in G&A expenses was primarily due to corporate-related costs, including increases in stock-based compensation expense of $0.3 million. Non-GAAP G&A expenses were $4.3 million for the quarter ended September 30, 2025, excluding $1.7 million non-cash stock-based compensation expense. Non-GAAP G&A expenses were $3.0 million for the quarter ended September 30, 2024, excluding $1.3 million non-cash stock-based compensation expense. A reconciliation of GAAP to non-GAAP financial measures used in this press release can be found at the end of this press release. 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 antagonist (CERAN) and a selective estrogen receptor degrader (SERD), currently in two Phase 3 clinical trials. In addition, Olema is developing OP-3136, a potent lysine acetyltransferase 6 (KAT6) inhibitor, now in a Phase 1 clinical study. Olema is headquartered in San Francisco and has operations in Cambridge, Massachusetts. For more information, please visit www.olema.com. About Palazestrant (OP-1250)Palazestrant (OP-1250) is a novel, orally available small molecule with dual activity as both a complete estrogen receptor antagonist (CERAN) and selective estrogen receptor degrader (SERD). It is currently being investigated in patients with recurrent, locally advanced or metastatic ER-positive (ER+), human epidermal growth factor receptor 2-negative (HER2-) breast cancer. In clinical studies, palazestrant completely blocks ER-driven transcriptional activity in both wild-type and mutant forms of metastatic ER+ breast cancer and has demonstrated anti-tumor efficacy along with attractive pharmacokinetics and exposure, favorable tolerability, central nervous system penetration, and combinability with cyclin-dependent kinase 4/6 (CDK4/6) inhibitors. Palazestrant has been granted U.S. Food and Drug Administration (FDA) Fast Track designation for the treatment of ER+/HER2- metastatic breast cancer that has progressed following one or more lines of endocrine therapy with at least one line given in combination with a CDK4/6 inhibitor. It is being evaluated as a single agent in the ongoing pivotal Phase 3 clinical trial, OPERA-01, and in combination with ribociclib in the ongoing pivotal Phase 3 clinical trial, OPERA-02. Palazestrant is also being evaluated in multiple Phase 1/2 studies in combination with ribociclib, palbociclib, alpelisib, everolimus, and atirmociclib. 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 study. Non-GAAP Financial InformationThe results presented in this press release include both GAAP information and non-GAAP information. As used in this release, non-GAAP R&D expense is defined by Olema as GAAP R&D expense excluding stock-based compensation expense, and non-GAAP G&A expense is defined by Olema as GAAP G&A expense excluding stock-based compensation expense. We use these non-GAAP financial measures to evaluate our ongoing operations and for internal planning and forecasting purposes. We believe that non-GAAP financial information, when taken collectively, may be helpful to investors because it provides consistency and comparability with past financial performance. However, non-GAAP financial information is presented for supplemental informational purposes only, has limitations as an analytical tool, and should not be considered in isolation or as a substitute for financial information presented in accordance with GAAP. Other companies, including companies in our industry, may calculate similarly titled non-GAAP measures differently or may use other measures to evaluate their performance, all of which could reduce the usefulness of our non-GAAP financial measures as tools for comparison. Investors are encouraged to review the related GAAP financial measures and the reconciliation of these non-GAAP financial measures to their most directly comparable GAAP financial measures and not rely on any single financial measure to evaluate our business. Forward-Looking StatementsStatements contained in this press release regarding matters that are not historical facts are “forward-looking statements” within the meaning of Section 27A of the Securities Act of 1933 and Section 21E of the Securities Exchange Act of 1934. Words such as “anticipate,” “believe,” “could,” “expect,” “goal,” “intend,” “may,” “on track,” “potential,” “upcoming,” “will” and similar expressions (as well as other words or expressions referencing future events, conditions or circumstances) are intended to identify forward-looking statements. These statements include those related to the potential for palazestrant to become a best-in-class, backbone endocrine therapy for metastatic breast cancer, potential beneficial characteristics including but not limited to safety, tolerability, activity, efficacy and therapeutic effects of palazestrant or OP-3136, the combinability of palazestrant or OP-3136 with other drugs, including in the metastatic setting, timelines for initiation and enrollment for potential and current clinical studies and for the receipt and presentation of results of clinical trials of palazestrant and OP-3136 each as a monotherapy and in combination trials, Olema’s ability to transform the breast cancer paradigm, Olema’s potential commercial capabilities, Olema’s leadership and ability to develop novel therapies for breast cancer and beyond, and Olema’s financial condition and resources, results of operations, cash position and balance sheet strength. Because such statements deal with future events and are based on Olema’s current expectations, they are subject to various risks and uncertainties, and actual results, performance, or achievements of Olema could differ materially from those described in or implied by the statements in this press release. These forward-looking statements are subject to risks and uncertainties, including, without limitation, those discussed in the section titled “Risk Factors” in Olema’s Quarterly Report on Form 10-Q for the quarter ended September 30, 2025, and future filings and reports that Olema makes from time to time with the U.S. Securities and Exchange Commission. Except as required by law, Olema assumes no obligation to update these forward-looking statements, including in the event that actual results differ materially from those anticipated in the forward-looking statements. Media and Investor Relations ContactCourtney O’KonekVice President, Corporate CommunicationsOlema Oncologymedia@olema.com Olema Pharmaceuticals, Inc.Condensed Consolidated Balance Sheets Data(Unaudited)(In thousands) September 30, December 31, 2025 2024 Cash, cash equivalents and marketable securities $ 328,960 $ 434,086Total assets 352,453 450,979 Total current liabilities 41,655 41,758Total liabilities 44,965 42,015Total stockholders’ equity 307,488 408,964Total liabilities and stockholders’ equity $ 352,453 $ 450,979 Olema Pharmaceuticals, Inc.Condensed Consolidated Statements of Operations (Unaudited)(In thousands, except for share and per share data) Three Months Ended September 30, Nine Months Ended September 30, 2025 2024 2025 2024 Operating expenses: Research and development (1)$39,951 $33,226 $114,477 $92,218General and administrative (2)5,926 4,395 14,137 13,272Total operating expenses45,877 37,621 128,614 105,490Loss from operations(45,877) (37,621) (128,614) (105,490)Other income: Interest income3,648 2,928 12,214 9,388Other income12 138 10 195Total other income3,660 3,066 12,224 9,583Net loss$(42,217) $(34,555) $(116,390) $(95,907)Net loss per share, basic and diluted$(0.49) $(0.60) $(1.36) $(1.80)Weighted average shares used to compute net loss per share, basic and diluted (3)85,732,221 57,262,803 85,553,078 53,194,081 (1) Research and development expenses for the nine-months ended September 30, 2025 include a $10.0 million milestone payment in connection with the Aurigene Agreement.Research and development expenses for the nine-months ended September 30, 2024 include a $5.0 million milestone payment in connection with the Aurigene Agreement.(1) and (2) Used to reference to the table below.(3) The weighted average shares used to compute net loss per share, basic and diluted include the effect from the pre-funded warrants. Reconciliation of GAAP to Non-GAAP Information(In thousands) Three Months Ended September 30, Nine Months Ended September 30, 2025 2024 2025 2024 (1) Research and development reconciliation GAAP research and development$39,951 $33,226 $114,477 $92,218Less: stock-based compensation expense2,582 4,280 9,592 11,925Non-GAAP research and development$37,369 $28,946 $104,885 $80,293 (2) General and administrative reconciliation GAAP general and administrative$5,926 $4,395 $14,137 $13,272Less: stock-based compensation expense1,668 1,346 3,728 4,334Non-GAAP general and administrative$4,258 $3,049 $10,409 $8,938

临床1期临床3期财报快速通道临床结果

100 项与 Palazestrant 相关的药物交易

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研发状态

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适应症	最高研发状态	国家/地区	公司	日期
ER阳性乳腺癌	临床3期	美国	Olema Pharmaceuticals, Inc.	2025-11-03
ER阳性乳腺癌	临床3期	澳大利亚	Olema Pharmaceuticals, Inc.	2025-11-03
HER2 阴性乳腺癌	临床3期	美国	Olema Pharmaceuticals, Inc.	2025-11-03
HER2 阴性乳腺癌	临床3期	澳大利亚	Olema Pharmaceuticals, Inc.	2025-11-03
局部晚期乳腺癌	临床3期	美国	Olema Pharmaceuticals, Inc.	2025-11-03
局部晚期乳腺癌	临床3期	澳大利亚	Olema Pharmaceuticals, Inc.	2025-11-03
转移性乳腺癌	临床3期	美国	Olema Pharmaceuticals, Inc.	2025-11-03
转移性乳腺癌	临床3期	澳大利亚	Olema Pharmaceuticals, Inc.	2025-11-03
ER阳性/HER2阴性乳腺癌	临床3期	美国	Olema Pharmaceuticals, Inc.	2023-11-16
ER阳性/HER2阴性乳腺癌	临床3期	阿根廷	Olema Pharmaceuticals, Inc.	2023-11-16

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临床结果

适应症

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT05508906 (ESMO2025)	临床1/2期	ER阳性/HER2阴性乳腺癌 ER+ \| HER2-	72	Palazestrant 120 mg plus ribociclib	齋製糧遞築觸製築齋願(簾製積鏇網餘廠夢鹽糧) = 35% 製繭醖壓衊選觸鏇憲鏇 (衊蓋構製壓築鑰憲鑰鹹 ) 更多	积极	2025-10-17
				Palazestrant 120 mg plus ribociclib (prior CDK4/6i)
NCT04505826 (phase 1/2 study, Pubmed \| Breast Cancer Res)	临床1/2期	HR阳性乳腺腺癌 \| HER2 阴性乳腺癌 \| HR阳性/HER2阴性乳腺癌 ESR1 mutations	146	Palazestrant 60 mg/day	鹹壓遞蓋醖選鹹製鑰遞(夢衊願觸製鹽選遞夢壓) = 25.6% 獵製鹽憲憲膚觸襯獵簾 (繭醖艱膚鬱糧選膚糧鑰 ) 更多	积极	2025-07-01
				Palazestrant 120 mg/day
NCT05508906 (Company_Website) 人工标引	临床1/2期	ER阳性/HER2阴性乳腺癌一线	63	Palazestrant + Ribociclib	艱窪醖鏇壓繭構憲糧齋(衊蓋選鏇積衊醖窪衊糧) = 淵襯顧簾壓夢鹽衊鹽艱獵顧簾醖鹽鹽鏇構鹹醖 (築衊壓襯構鑰鹹餘積構 ) 更多	积极	2024-12-10
				Palazestrant + Ribociclib (prior treatment with a CDK4/6i plus an endocrine therapy)	艱窪醖鏇壓繭構憲糧齋(衊蓋選鏇積衊醖窪衊糧) = 憲積艱簾鹹醖淵蓋鏇膚獵顧簾醖鹽鹽鏇構鹹醖 (築衊壓襯構鑰鹹餘積構 ) 更多
NCT05508906 (ESMO_BC2024) 人工标引	临床1/2期	ER阳性/HER2阴性乳腺癌一线 HER2 Negative \| ER Positive	33	palazestrant+ribociclib	顧淵鹹蓋鏇夢選製醖壓(齋願網衊醖衊鹹壓壓齋) = The most common (≥25%) were nausea, neutropenia (G4: 2 pts; 6%), WBC count decreased, fatigue, anemia, and diarrhea. Most TEAEs were grade 1-2 and consistent with the known safety profiles of each drug. 鏇鹹淵襯餘顧鏇觸糧窪 (鹽憲遞遞鏇鏇繭鏇選鹹 )	积极	2024-05-16
GlobeNewswire 人工标引	临床1/2期	ER阳性/HER2阴性乳腺癌 ESR1 Mutation \| ER Positive \| HER2 Negative	46	palbociclib 125 mg+palazestrant 120 mg	淵範積顧選夢簾願壓餘(鏇夢窪鹽顧觸膚網壓鬱) = There was no observed drug-drug interaction between palazestrant and palbociclib, and there was no induced metabolism or increase in exposure of either palbociclib or palazestrant when administered in combination. 鏇鬱繭積夢淵鹹壓衊蓋 (鏇齋願襯憲範壓艱齋範 ) 更多	积极	2023-12-05
				palbociclib 125 mg+palazestrant 120 mg (ESR1 mutation)
GlobeNewswire 人工标引	临床1/2期	ER阳性/HER2阴性乳腺癌 HER2 Negative \| ER Positive	19	Ribociclib 600 mg+Palazestrant 120 mg	顧蓋襯艱顧顧選獵膚窪(淵鏇繭鹹窪襯膚糧廠鑰) = well tolerated, with no safety signals or enhancement of toxicity and an overall safety profile remains consistent with the expected safety profile of ribociclib plus an endocrine therapy. 襯夢蓋築網選願廠顧鬱 (壓艱糧糧獵構鏇淵遞鹹 ) 更多	积极	2023-12-05
NCT04505826 (ESMO 12023 \| ESMO 22023) 人工标引	临床1/2期	ER阳性/HER2阴性乳腺癌 ER Positive \| HER2 Negative	86	OP-1250 120 mg	糧簾衊蓋獵膚繭簾艱艱(艱鬱醖膚蓋衊繭餘鬱鬱) = nausea, vomiting, neutropenia, fatigue, headache, constipation, and diarrhea 夢齋鏇夢衊壓鹽衊艱顧 (鬱選選簾餘鬱壓餘壓繭 ) 更多	积极	2023-10-22
				OP-1250 120 mg (ESR1 mutation)
NCT04505826 (ENA2022) 人工标引	临床1期	ER阳性/HER2阴性乳腺癌 ER positive \| HER2 negative	37	OP-1250 (60mg)	製鏇繭鏇網顧製構觸範(網淵繭製夢製繭製積鬱) = The most common treatment emergent adverse events reported (≥10%) in Phase 1b in the 60 mg/120 mg cohorts were nausea (28%/21%), vomiting (17%/16%), fatigue (17%/5%) and headache (11%/ 11%). 窪衊襯獵獵艱鬱夢淵蓋 (顧糧蓋糧製鹹齋構鹽憲 ) 更多	积极	2022-10-28
				OP-1250 (120mg)
NCT04505826 (Biospace) 人工标引	临床1/2期	ER阳性/HER2阴性乳腺癌 ER positive \| HER2 negative	-	OP-1250	鬱蓋選鏇觸簾壓壓餘廠(獵艱憲觸製願鹹廠憲繭) = 齋遞繭選築鹽憲廠膚壓膚願糧鏇鑰選淵鏇遞糧 (鬱範艱膚觸餘製獵夢網 ) 更多	积极	2021-11-30