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2025-10-31

申办/合作机构

Olema Pharmaceuticals, Inc.

[+1]

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.

NCT05508906

/ Active, not recruiting临床1期

A Phase 1b Open-Label Multicenter Study of OP-1250 (Palazestrant) in Combination With the CDK4/6 Inhibitor Ribociclib, With the PI3K Inhibitor Alpelisib, or With the mTOR Inhibitor Everolimus in Adult Subjects With Advanced and/or Metastatic ER Positive, HER2 Negative Breast Cancer

This is a Phase 1b open-label, 2-part study in 3 treatment groups. The 3 treatment groups are as follows:
Treatment Group 1: Palazestrant (OP-1250) in combination with ribociclib (KISQALI®, Novartis Pharmaceuticals Corporation).
Treatment Group 2: Palazestrant (OP-1250) in combination with alpelisib (PIQRAY®, Novartis Pharmaceuticals Corporation).
Treatment Group 3: Palazestrant (OP-1250) in combination with everolimus.

开始日期2022-08-31

申办/合作机构

Olema Pharmaceuticals, Inc.

[+1]

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 ; Tonda, Margaret ; Hamilton, Erika P ; 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.

101

项与 Palazestrant 相关的新闻（医药）

2025-09-03

·GlobeNewswire-Health Care

Olema Oncology Announces New Clinical Trial Agreement with Pfizer to Combine Palazestrant with Atirmociclib in ER+/HER2- Metastatic Breast Cancer

Study to explore the palazestrant-atirmociclib combination in approximately 35 patients with initiation anticipated in H2 2025 Results to inform potential pivotal Phase 3 trial of novel combination in frontline metastatic breast cancer setting Sept. 02, 2025 -- 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 a new clinical trial collaboration and supply agreement with Pfizer Inc. (NYSE: PFE) in metastatic breast cancer. The companies will evaluate in a Phase 1b/2 study the safety and combinability of palazestrant plus atirmociclib, Pfizer’s investigational, highly selective-CDK4 inhibitor, in patients with estrogen receptor-positive, human epidermal growth factor receptor 2-negative (ER+/HER2-) metastatic breast cancer. "We are excited to assess this combination in the clinic as we seek to establish palazestrant as a potential backbone endocrine therapy for metastatic breast cancer,” said Sean P. Bohen, M.D., Ph.D., President and Chief Executive Officer of Olema Oncology. “Based on the promising profiles of palazestrant and atirmociclib to date, we look forward to evaluating the potential of this novel combination and, if successful, advancing to a pivotal trial in the frontline setting. With OPERA-01, our first pivotal study of palazestrant, underway and our OPERA-02 ribociclib combination trial in frontline metastatic breast cancer anticipated to initiate this quarter, we remain focused on achieving our goal of transforming the metastatic breast cancer treatment paradigm.” Under the terms of the agreement, Pfizer will supply atirmociclib for use in the Phase 1b/2 study and Olema will lead the conduct of the study. All clinical data and inventions relating to the combined use of atirmociclib and palazestrant resulting from the study will be jointly owned, with Olema maintaining full global commercial and marketing rights to palazestrant. This announcement represents Olema’s second clinical trial agreement with Pfizer. The companies’ previous agreement was established in November 2020 to evaluate palazestrant in combination with palbociclib (IBRANCE®) in patients with recurrent, locally advanced or metastatic ER+/HER2- breast cancer. 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 study. Olema is headquartered in San Francisco and has operations in Cambridge, Massachusetts. Palazestrant (OP-1250) is a novel, orally available small molecule with dual activity as both a complete estrogen receptor (ER) antagonist (CERAN) and selective ER 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 is anticipated to be evaluated in combination with ribociclib in the planned pivotal Phase 3 clinical trial, OPERA-02. The content above comes from the network. if any infringement, please contact us to modify.

快速通道引进/卖出

2025-08-14

·PRNewswire

Biotech Stocks Rally as Oncology Market Targets $866B by 2034

Equity Insider News Commentary Issued on behalf of Oncolytics Biotech Inc. VANCOUVER, BC, Aug. 14, 2025 /PRNewswire/ -- Equity Insider News Commentary – Despite alarming federal budget cuts that stand to potentially harm the national battle against cancer, it appears that the private sector continues to step up, with hundreds of millions of VC dollars pouring into oncology ventures so far in 2025. While there has been a recent victory in the Senate to restore $15 million for the Pancreatic Cancer Research Program (PCARP), the prior elimination of the only federal program dedicated solely to researching pancreatic cancer served as a stark reminder of these ongoing funding challenges. This dynamic is setting the stage for a "flight to quality" among investors, who are now more than ever looking for innovative leaders with strong pipelines and clear paths to regulatory execution, a key milestone that can separate a promising biotech from a potential breakthrough like Oncolytics Biotech Inc. (NASDAQ: ONCY) (TSX: ONC), ProPhase Labs, Inc. (NASDAQ: PRPH), IO Biotech, Inc. (NASDAQ: IOBT), Olema Pharmaceuticals, Inc. (NASDAQ: OLMA), and PDS Biotechnology Corporation (NASDAQ: PDSB). According to a report from Global Market Insights, the global oncology market was estimated at US$345.1 billion in 2025, and while growing at an impressive 10.8% CAGR, is projected to reach US$866.1 billion by 2034 — with $377.1 billion of that coming from the USA alone. Even more optimistic is a report from Vision Research Reports, which sees the global cancer drug sector surpassing US$900 billion in sales by 2034. Oncolytics Biotech Inc. (NASDAQ: ONCY) (TSX: ONC) has officially entered the most critical phase of its development journey—pursuing a potential registration-enabling trial in first-line metastatic pancreatic ductal adenocarcinoma (mPDAC) for its flagship asset, pelareorep. In its latest Q2 2025 report, the company confirmed it has begun formal discussions with the U.S. Food and Drug Administration (FDA) aimed at finalizing a pivotal study design, with trial start-up activities expected to begin as early as Q4 2025. For investors and potential partners, this represents a clear transition from promising clinical data to potential regulatory approval in one of medicine's most challenging cancer types. "We have turned the corner from proof-of-concept studies and will be sprinting toward regulatory clarity for the remainder of the year," said Jared Kelly, CEO of Oncolytics. "As we shore up our intellectual property, get a clear registration path for pelareorep, and allow our GOBLET data to mature, we will establish our position as the only platform immunotherapy in gastrointestinal tumors." The strategic focus on mPDAC reflects both compelling clinical results and a significant market opportunity. Pelareorep is a systemically delivered oncolytic virus designed to convert immunologically "cold" tumors—those typically invisible to the immune system—into "hot" tumors that can respond to immunotherapy. In first-line pancreatic cancer studies, pelareorep-based regimens have demonstrated a notable 21.9% two-year overall survival rate, compared to a 9.2% historical benchmark for standard chemotherapy alone. Even more compelling, when pelareorep was combined with chemotherapy and a checkpoint inhibitor, researchers recorded a 62% objective response rate—particularly significant given that checkpoint inhibitors are not currently approved for use in this indication. These results stem from pelareorep's dual mechanism: it both replicates within cancer cells and activates the body's immune response against tumors. "This robust data set, amassed from several studies in cancers that have historically resisted immunotherapeutic approaches, provides definitive validation of pelareorep's immune-mediated mechanism of action," said Dr. Thomas Heineman, Chief Medical Officer of Oncolytics. "We observed tumor biopsy-confirmed virus replication, immune cell activation, and the recruitment of cytotoxic T cells into the TME—all consistent with the durable responses observed in patients with metastatic PDAC and HR+/HER2- breast cancer who were treated with pelareorep." Translational data from the GOBLET and AWARE-1 studies demonstrate how pelareorep transforms the tumor microenvironment, increasing PD-L1 expression, heightening interferon signaling, and mobilizing tumor-infiltrating lymphocytes in the blood—changes that correlate with tumor size reduction. This mechanistic validation, combined with survival data from over 1,100 patients across multiple studies, has solidified the company's decision to prioritize this indication. Oncolytics' execution-focused strategy is being led by Jared Kelly and Andrew Aromando, who both played key roles in Ambrx Biopharma's US$2 billion acquisition by Johnson & Johnson. Kelly was appointed CEO earlier this year, while Aromando recently joined as Chief Business Officer. In line with their focus on capital efficiency, the company has terminated its At-the-Market and Equity Line of Credit facilities, citing sufficient resources to advance key milestones without near-term shareholder dilution. Regulatory advantages are already in place to accelerate development. Pelareorep holds Fast Track and Orphan Drug designations for pancreatic cancer from the FDA, meaning the agency has already recognized both the drug's potential and the serious unmet need in this patient population. These statuses streamline review processes and enhance the program's attractiveness to potential pharmaceutical partners. The context underscores the opportunity: pancreatic cancer remains one of the deadliest common cancers, with a five-year survival rate of less than 14%. Unlike other cancers where immunotherapies have transformed treatment, mPDAC has largely resisted immunotherapeutic approaches—making pelareorep's immune-activating mechanism particularly promising for this underserved patient population. Back in July, Oncolytics hosted a key opinion leader event featuring gastrointestinal cancer experts who reviewed survival outcomes for patients and biomarker validation. The expert panel reinforced the view that pelareorep's mechanism of activating innate and adaptive immune responses is both biologically sound and commercially relevant for first-line mPDAC treatment. With this latest milestone, Oncolytics is entering a phase where FDA feedback will shape both clinical plans and potential commercial partnerships. If the agency accepts the company's proposed trial framework centered on an overall survival endpoint, the resulting study could provide definitive proof of pelareorep's market potential in mPDAC. The company expects to provide an updated clinical timeline in Q3 2025, with trial start-up activities potentially beginning as early as Q4 2025. With compelling survival data, regulatory designations in place, and an experienced leadership team driving execution, Oncolytics is positioning pelareorep for a pivotal test in one of oncology's most challenging and underserved markets. CONTINUED… Read this and more news for Oncolytics Biotech at: In other recent industry developments and happenings in the market include: ProPhase Labs, Inc. (NASDAQ: PRPH) announced it received a U.S. patent for its BE-Smart test that can detect early signs of Barrett's esophageal cancer, a deadly disease that kills most patients because it's usually caught too late. The test works with simple brush and forceps biopsies and achieved over 95% accuracy in clinical testing, potentially allowing doctors to catch this cancer when it's still treatable. "This achievement, coming on the heels of our BE-Smart™ validation demonstrating greater than a 95% technical success rate and dual compatibility with both brush and forceps biopsies, solidifies our leadership in medical innovation and brings us one step closer to transforming early detection and treatment strategies for this serious condition," said Ted Karkus, CEP of ProPhase. "With this newly issued patent, we believe we are well positioned to accelerate commercialization and broaden clinical access to BE-Smart." ProPhase's breakthrough could save thousands of lives by identifying patients at high risk for esophageal cancer before the disease becomes incurable, representing a major advancement in early cancer detection. IO Biotech, Inc. (NASDAQ: IOBT) recently announced that its experimental cancer vaccine (Cylembio) meaningfully extended the time before advanced melanoma patients got worse, with patients living 19.4 months without disease progression compared to 11 months for those on standard treatment alone. The vaccine works by training the immune system to attack both cancer cells and the cells that help tumors hide from treatment, and it showed particularly strong results in patients whose tumors were PD-L1 negative and unlikely to respond to current immunotherapies. "In this study, we observed a highly encouraging improvement in progression free survival and consistent trend in overall survival in patients treated with Cylembio," said Mai-Britt Zocca, PhD, President and CEO of IO Biotech. "The magnitude and durability of clinical effect observed consistently across subgroups supports our confidence in Cylembio and its potential as a treatment for advanced melanoma patients. We look forward to engaging with the FDA to determine a potential path to approval based on these data." IO Biotech plans to meet with the FDA this fall to discuss approval for this treatment that could become a new standard of care for the deadliest form of skin cancer. Olema Pharmaceuticals, Inc. (NASDAQ: OLMA) reported progress on its experimental breast cancer pill called palazestrant, which is designed to completely block estrogen signals that fuel most breast cancers and is currently being tested in two large Phase 3 trials expected to finish in 2026. "Having achieved regulatory alignment on the selected dose for our pivotal palazestrant program during the second quarter, we are focused on accelerating enrollment in OPERA-01, which is on track for top-line data in the second half of 2026," said Sean P. Bohen, M.D., Ph.D., President and CEO of Olema. "Palazestrant's demonstrated activity and combinability with multiple compounds offers the potential for it to become a best-in-class, backbone endocrine therapy for metastatic breast cancer." The company is also developing OP-3136, a pill that targets a different pathway cancer cells use to grow and spread, with early results expected in 2026. Olema's drugs are designed to work where current treatments fail, potentially offering hope to the thousands of breast cancer patients whose tumors eventually become resistant to existing therapies. PDS Biotechnology Corporation (NASDAQ: PDSB) reported promising results from a colorectal cancer study where its experimental treatment achieved impressive response rates, leading to expansion of the trial to treat more patients with this hard-to-treat cancer. "Our second quarter of 2025 and recent weeks have been a productive period for PDS Biotech, highlighted by the continued progress in our VERSATILE-003 Phase 3 clinical trial," said Frank Bedu-Addo, Ph.D., President and CEO of PDS Biotech. "We look forward to publishing the full data set for this trial later this year, as we continue to progress our VERSATILE-003 trial, the only registrational stage trial specifically targeting HPV16-positive HNSCC patients." The company's lead program targets head and neck cancers caused by HPV, the same virus that is a major cause of cervical cancer, and is currently being tested in the only late-stage trial specifically designed for these patients. PDS Biotech's approach uses its immune-boosting technology to help the body's natural defenses better recognize and destroy cancer cells, potentially offering new hope for patients with limited treatment options. Source: CONTACT: Equity Insider [email protected] (604) 265-2873 DISCLAIMER: Nothing in this publication should be considered as personalized financial advice. We are not licensed under securities laws to address your particular financial situation. No communication by our employees to you should be deemed as personalized financial advice. Please consult a licensed financial advisor before making any investment decision. This is a paid advertisement and is neither an offer nor recommendation to buy or sell any security. We hold no investment licenses and are thus neither licensed nor qualified to provide investment advice. The content in this report or email is not provided to any individual with a view toward their individual circumstances. Equity Insider is a wholly-owned subsidiary of Market IQ Media Group, Inc. ("MIQ"). MIQ has been paid a fee for Oncolytics Biotech Inc. advertising and digital media from the company directly. There may be 3rd parties who may have shares of Oncolytics Biotech Inc., and may liquidate their shares which could have a negative effect on the price of the stock. This compensation constitutes a conflict of interest as to our ability to remain objective in our communication regarding the profiled company. Because of this conflict, individuals are strongly encouraged to not use this publication as the basis for any investment decision. The owner/operator of MIQ own shares of Oncolytics Biotech Inc. which were purchased in the open market, and reserve the right to buy and sell, and will buy and sell shares of Oncolytics Biotech Inc. at any time without any further notice commencing immediately and ongoing. We also expect further compensation as an ongoing digital media effort to increase visibility for the company, no further notice will be given, but let this disclaimer serve as notice that all material, including this article, which is disseminated by MIQ has been approved by Oncolytics Biotech Inc.; this is a paid advertisement, we currently own shares of Oncolytics Biotech Inc. and will buy and sell shares of the company in the open market, or through private placements, and/or other investment vehicles. While all information is believed to be reliable, it is not guaranteed by us to be accurate. Individuals should assume that all information contained in our newsletter is not trustworthy unless verified by their own independent research. Also, because events and circumstances frequently do not occur as expected, there will likely be differences between the any predictions and actual results. Always consult a licensed investment professional before making any investment decision. Be extremely careful, investing in securities carries a high degree of risk; you may likely lose some or all of the investment. Logo - SOURCE Equity Insider WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

临床3期免疫疗法高管变更

2025-07-01

·CPHI制药在线

从康辰药业KC1086看KAT6靶向药潜力：辉瑞、恒瑞等药企抢滩，或攻克CDK4/6耐药

关注并星标CPHI制药在线日前，北京康辰药业股份有限公司（简称：康辰药业）1类新药KC1086片在国内获得临床试验默示许可，拟用于晚期复发或转移性实体瘤。KC1086是康辰药业完全自主研发的一款具有全新结构的强效、高选择性赖氨酸乙酰转移酶6（KAT6）的小分子抑制剂。临床前研究显示：在ER+/HER2-的乳腺癌药效模型中，同等剂量水平下KC1086对肿瘤生长具有更强的抑制作用，且在其他实体瘤药效模型中显示出类似的效果。此外，KC1086的ADME特性和安全性评价结果显示可有效解决此类化合物的蓄积问题，无明显的种属差异。康辰药业是集研产销于一体的创新药企业，除了KC1086，公司还有多款在研项目，其中ZY5301（“金草片”）是NMPA批准的针对“盆腔炎性疾病后遗症慢性盆腔痛”的唯一中药，其3期临床试验已达到主要研究终点，完成递交Pre-NDA并已获得受理。ZY5301属于我国在研中药1.2类新药，其主要成分是总环烯醚萜苷，由筋骨草全草提取获得。2024年3月，公司宣布该药在女性盆腔炎性疾病后遗症慢性盆腔痛患者中开展的3期临床试验（CTR20222693）已达到主要研究终点。统计分析结果显示：ZY5301在为期12周治疗期内VAS评分的疼痛消失率达到主要研究终点，其安全性及耐受性表现良好，且不良事件发生率低。KC1036进展也较快，是其公司自主研发且具有完全自主知识产权的II型非竞争性AXL、VEGFR多靶点受体酪氨酸激酶抑制剂，通过抑制AXL、VEGFR2等靶点实现抗肿瘤活性，被开发针对消化系统肿瘤、胸腺肿瘤等多个适应症。已公布的临床试验结果显示：截至2023年7月31日，KC1036单药治疗晚期食管鳞癌（ESCC）的ORR为26.1%，疾病控制率DCR为69.6%，中位OS为7.1月，明显优于现有临床结果。关于KAT6及其靶向药进展KAT6属于MYST家族组蛋白乙酰化酶，在调节转录、发育、造血细胞分化、细胞周期进程和有丝分裂方面发挥关键作用。KAT6 包括 KAT6A、KAT6B两种亚型其中KAT6A于1996年在急性髓系白血病（AML）的染色体异位中首次被发现。KAT6B于1999年被鉴定为KAT6A的旁系同源物。研究发现，KAT6通过对组蛋白H3和非组蛋白进行乙酰化修饰，在细胞周期调控、干细胞自我更新等方面发挥着重要作用，其异常表达（包括突变、基因组扩增、缺失或融合）往往会导致乳腺癌、卵巢癌、宫颈癌、胶质母细胞瘤、白血病等多种疾病的发生。因此，KAT6被认为是肿瘤药研发的潜力靶点。据不完全统计，全球还有多款在研KAT6靶向药，详见下表。在研KAT6靶向药大多处于早期临床，恒瑞医药的HRS-2189进展较快，其前列腺癌适应症已进入2期阶段。辉瑞的PF-07248144是全球最先开展临床研究的KAT6抑制剂，通过与KAT6A/B选择性结合，抑制组蛋白H3第23位赖氨酸乙酰化修饰（H3K23Ac），从而影响基因转录发挥治疗作用。2025 ASCO大会上公布的PF-07248144作为单药疗法，以及与氟维司群治疗曾接受过大量治疗的ER+/HER2-转移性乳腺癌的首次人体 1期剂量递增/扩展研究结果显示：1mg、5mgPF-07248144+氟维司群治疗组的ORR分别为24.1%、37.2%，CBR分别为37.9%、55.8%，mDOR分别为4.6个月、15.8个月，mPFS分别为3.6个月、10.7个月。安全性方面，最常见的3级及以上副作用为中性粒细胞贫血，该副作用可以逆转且可以通过剂量调整来控制，未发生肺炎副作用。辉瑞计划今年开展该药的关键3期临床，进一步巩固公司在乳腺癌领域的优势。Olema Oncology的OP-3136在临床前研究中显示出显著的抗肿瘤活性，无论单药使用还是与palazestrant（一款雌激素受体完全拮抗剂）联合。齐鲁制药的QLS1304在ER+/HER2-乳腺癌体内模型中无论单药还是与SoC联用均展示出了强劲的抗肿瘤疗效，今年5月被FDA授予快速通道资格认定。复宏汉霖的HLX97-053在对CDK4/6抑制剂耐药患者来源的异种移植瘤模型中表现出与氟维司群和哌柏西利明显更强的协同作用，且其血液学毒性也显著降低，具有同类最佳的潜力。此外，KAT6靶向药领域已有BD交易达成。2024年1月，英矽智能将ISM5043的全球独家开发和商业化权益授予给美纳里尼，总金额高达5亿美元。总结整体来看，KAT6靶向药大多处于早期阶段，辉瑞的PF-07248144预计有望最先进入3期临床。适应症上看，当前KAT6靶向药主要集中在乳腺癌，有望攻克CDK4/6抑制剂耐药问题。期待KAT6靶向药早日迎来重大突破，造福广大肿瘤患者。END智药研习社近期直播预告来源：CPHI制药在线声明：本文仅代表作者观点，并不代表制药在线立场。本网站内容仅出于传递更多信息之目的。如需转载，请务必注明文章来源和作者。投稿邮箱：Kelly.Xiao@imsinoexpo.com▼更多制药资讯，请关注CPHI制药在线▼点击阅读原文，进入智药研习社~

临床结果申请上市

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.	2025-10-31
ER阳性乳腺癌	临床3期	澳大利亚	Olema Pharmaceuticals, Inc.	2025-10-31
HER2 阴性乳腺癌	临床3期	美国	Olema Pharmaceuticals, Inc.	2025-10-31
HER2 阴性乳腺癌	临床3期	澳大利亚	Olema Pharmaceuticals, Inc.	2025-10-31
局部晚期乳腺癌	临床3期	美国	Olema Pharmaceuticals, Inc.	2025-10-31
局部晚期乳腺癌	临床3期	澳大利亚	Olema Pharmaceuticals, Inc.	2025-10-31
转移性乳腺癌	临床3期	美国	Olema Pharmaceuticals, Inc.	2025-10-31
转移性乳腺癌	临床3期	澳大利亚	Olema Pharmaceuticals, Inc.	2025-10-31
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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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


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	鏇窪鏇願襯醖蓋齋願網(積壓齋製糧顧齋糧淵醖) = 25.6% 獵鹹餘窪築觸鬱鑰構遞 (網衊餘選餘鹹艱選鏇衊 ) 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	窪壓築觸構鏇獵積鏇糧(憲繭壓淵襯糧襯願夢範) = 衊繭繭齋鹽繭繭糧築製鑰範夢網鬱糧窪壓積選 (蓋築鏇蓋糧醖鹹積壓糧 ) 更多	积极	2024-12-10
				Palazestrant + Ribociclib (prior treatment with a CDK4/6i plus an endocrine therapy)	窪壓築觸構鏇獵積鏇糧(憲繭壓淵襯糧襯願夢範) = 蓋膚遞艱艱齋夢廠積鹹鑰範夢網鬱糧窪壓積選 (蓋築鏇蓋糧醖鹹積壓糧 ) 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	網鬱餘簾網鬱鹹壓蓋繭(願鏇製壓醖網簾築淵顧) = 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. 鏇鏇膚膚顧鹹醖顧艱獵 (繭齋齋廠製獵齋艱鏇簾 )	积极	2024-05-16
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	積餘遞膚餘餘糧簾觸鹽(顧憲餘膚繭鑰醖膚構遞) = 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. 觸構築淵衊艱鹽鏇顧鑰 (夢簾積獵膚鬱襯顧醖夢 ) 更多	积极	2023-12-05
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	廠壓鏇夢遞壓獵積糧積(夢遞鹽範蓋選觸廠網鏇) = 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. 簾顧膚糧構鏇願鹹壓窪 (窪構齋鑰構鏇繭糧壓鹹 ) 更多	积极	2023-12-05
				palbociclib 125 mg+palazestrant 120 mg (ESR1 mutation)
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	選蓋獵築鹹鏇範糧範願(鑰憲製蓋壓獵蓋壓鑰淵) = nausea, vomiting, neutropenia, fatigue, headache, constipation, and diarrhea 製鏇願艱範鹽獵觸鬱醖 (遞獵鏇構衊願積繭願糧 ) 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)	築壓積繭壓醖願願遞衊(鹹積獵獵鬱築蓋願遞構) = 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%). 鬱糧窪憲夢觸製觸鑰鏇 (構蓋憲積餘顧艱餘壓鹽 ) 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	窪齋築鹽衊簾網積鹹壓(艱糧淵積淵繭淵蓋膚製) = 鑰鏇膚繭糧選願壓繭遞選鏇選網糧醖窪鑰餘顧 (築鬱膚齋齋簾鹹網艱夢 ) 更多	积极	2021-11-30