Palazestrant(Palazestrant) - 药物靶点：ER_在研适应症：ER阳性乳腺癌，HER2 阴性乳腺癌，局部晚期乳腺癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

OP-1250

靶点

ER

作用方式

降解剂

作用机制

ERs降解剂(雌激素受体家族降解剂)

治疗领域

肿瘤皮肤和肌肉骨骼疾病泌尿生殖系统疾病

在研适应症

ER阳性乳腺癌HER2 阴性乳腺癌局部晚期乳腺癌+ [4]

非在研适应症

HR阳性乳腺腺癌HR阳性/HER2阴性乳腺癌

原研机构

Olema Pharmaceuticals, Inc.

在研机构

Olema Pharmaceuticals, Inc.

非在研机构-

权益机构

Olema Pharmaceuticals, Inc.

Pfizer Inc.

Novartis AG

最高研发阶段临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评快速通道 (美国)

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结构/序列

分子式C28H36FN3O

InChIKeyLBSFUBLFDCAEKV-XHCCPWGMSA-N

CAS号2092925-89-6

关联

6

项与 Palazestrant 相关的临床试验

NCT07085767

/ Recruiting临床3期

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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5

项与 Palazestrant 相关的文献（医药）

2026-01-14·Future Oncology

OPERA-01: a phase III study of palazestrant for ER+, HER2– advanced breast cancer after CDK4/6 inhibitor therapy

Article

作者: Chan, Arlene ; Schmid, Peter ; Sohn, Joohyuk ; McArthur, Heather ; Bellet Ezquerra, Meritxell ; Pistilli, Barbara ; de Kermadec, Elisabeth ; Del Mastro, Lucia ; Meisel, Jane ; Zheng, Lianqing

Endocrine therapy (ET) resistance is a major concern when treating estrogen receptor-positive (ER+) human epidermal growth factor receptor 2-negative (HER2-) breast cancer. A combination of cyclin-dependent kinase 4/6 inhibitors (CDK4/6i) and ET is the current first-line standard of care (SOC) for patients with ER+, HER2- advanced breast cancer. Despite the benefits of ET plus a CDK4/6i, disease progression due to endocrine resistance remains a significant challenge. More effective ETs that can overcome resistance are needed to improve clinical outcomes and maintain quality of life by delaying chemotherapy. Palazestrant is a novel oral, complete estrogen receptor antagonist (CERAN) and selective estrogen receptor degrader (SERD) that blocks both transcriptional activation function domains, AF1 and AF2, resulting in complete inhibition of ER-driven transcription, regardless of estrogen receptor 1 (ESR1) mutation status. As monotherapy, palazestrant showed tolerable safety, favorable pharmacokinetics, and antitumor efficacy in heavily pretreated patients during phase I/II studies. OPERA-01 (NCT06016738) is a phase III study designed to evaluate the safety and efficacy of palazestrant monotherapy compared to SOC ET in patients with ER+, HER2- locally advanced or metastatic breast cancer, regardless of ESR1 mutation status, whose disease advanced following treatment with at least one ET in combination with a CDK4/6i.Clinical Trial Registration: Clinicaltrials.gov NCT06016738. Registered 17 August 2023.

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 ; Zak, David R. ; Wang, Chenbo ; 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).

2024-11-01·LANCET ONCOLOGY

The state of the science of oral selective oestrogen receptor degraders

Article

作者: Mayer, Erica L ; Fanucci, Kristina

144

项与 Palazestrant 相关的新闻（医药）

2026-07-02

·BioSpace

Olema Oncology Reports Inducement Grants Under Nasdaq Listing Rule 5635(c)(4) - July 2, 2026

SAN FRANCISCO, July 02, 2026 (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 that the Company granted stock options to eight new employees to purchase an aggregate of 215,800 shares of the Company's common stock, effective as of July 1, 2026. These awards were approved by the Compensation Committee of Olema’s Board of Directors and granted under the Company's 2022 Inducement Plan as an inducement material to the new employees entering into employment with Olema, in accordance with Nasdaq Listing Rule 5635(c)(4). The stock options vest over four years, with 25 percent vesting on the first anniversary of the vesting commencement date for such employee and the remainder vesting in 36 equal monthly installments over the following three years, subject to the employee being continuously employed by Olema as of such vesting dates. The stock options have a 10-year term and an exercise price of $12.08 per share, equal to the last reported sale price of the Company's common stock as reported by Nasdaq on July 1, 2026. The stock options are subject to the terms of the Olema Pharmaceuticals, Inc., 2022 Inducement Plan. Olema is providing this information in accordance with Nasdaq Listing Rule 5635(c)(4). About Olema Oncology Olema Oncology is a clinical-stage biopharmaceutical company committed to transforming the standard of care and improving outcomes for patients living with breast cancer and beyond. Olema is advancing a pipeline of novel therapies by leveraging our deep understanding of endocrine-driven cancers, nuclear receptors, and mechanisms of acquired resistance. Our lead product candidate, palazestrant (OP-1250), is a proprietary, orally available complete estrogen receptor 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 . Media and Investor Relations Contact Courtney O’Konek Vice President, Corporate Communications Olema Oncology media@olema.com

临床3期临床1期

2026-06-10

·医脉通

HR+转移性乳腺癌CDK4/6i治疗进展后的精准诊疗前沿

CDK4/6抑制剂（CDK4/6i）联合内分泌治疗已成为HR阳性（HR+）/HER2阴性（HER2-）晚期乳腺癌的一线标准方案，显著改善了患者的无进展生存期（PFS）和总生存期（OS）。然而，耐药几乎不可避免，后续治疗选择成为临床难题。近期，一篇发表于American Society of Clinical Oncology Educational Book的综述系统梳理了CDK4/6i进展后的治疗格局，涵盖靶向ESR1突变、PI3K/AKT通路、新型内分泌药物、抗体药物偶联物（ADC）以及下一代CDKi等前沿进展。本文将核心内容梳理如下，以飨读者。一、CDK4/6i耐药机制 CDK4/6i联合内分泌治疗的耐药机制呈现高度异质性，主要集中于细胞周期调控异常与癌基因信号通路过度激活两大维度。细胞周期相关异常是耐药的核心驱动因素之一，包括RB1基因缺失、AURKA激活突变、FAT1基因缺失（间接上调CDK6表达）及CCNE1/CCNE2基因扩增（异常激活CDK2活性），上述改变会破坏CDK4/6i对细胞周期的阻滞作用，促使肿瘤细胞持续增殖。癌基因信号通路异常也同样会导致肿瘤耐药，其中包括PI3K/AKT通路异常激活（PIK3CA/AKT1/PTEN基因改变），RAS/MAPK通路的KRAS突变、NF1缺失，ERBB2、FGFR1/2等受体酪氨酸激酶异常扩增。临床实践中，分子检测时机与方法的选择对耐药机制解析至关重要，优先推荐在CDK4/6i治疗前后或疾病进展即刻开展循环肿瘤细胞DNA（ctDNA）检测，避免多线治疗后基因组变异干扰检测结果；二代测序（NGS）是临床决策的重要工具，而全外显子测序、RNA转录组及甲基化测序可进一步揭示罕见耐药机制，为精准治疗提供更全面依据。二、基于生物标志物改变的精准治疗策略基于分子标志物的精准分层治疗，已成为CDK4/6i耐药后HR+/HER2-转移性乳腺癌的核心治疗策略。临床需根据不同的耐药突变给予精准治疗策略。 1. ESR1突变 ESR1突变会导致ER不依赖雌激素持续激活，是HR+/HER2-乳腺癌患者在内分泌治疗后最常见的获得性耐药机制之一。口服SERD是当前临床实践中ESR1突变患者的首选药物。III期EMERALD试验显示，对于ESR1突变人群，口服SERD艾拉司群对比标准内分泌治疗，中位PFS显著延长（3.8个月 vs 1.9个月，HR=0.55）。值得注意的是，既往CDK4/6i治疗超过12个月的患者获益更明显（中位PFS：8.6个月 vs 1.9个月，HR=0.41）。基于此，Elacestrant已获美国食品药品监督管理局（FDA）批准用于ESR1突变晚期乳腺癌的后线治疗。此外，更多口服SERD类药物正在探索中。 2. PI3K/AKT通路改变 PI3K/AKT通路异常激活与乳腺癌内分泌治疗耐药、预后不良相关。约50%的HR+转移性乳腺癌存在PI3K/AKT通路异常激活。INAVO120试验提示，与哌柏西利联合内分泌治疗相比，PI3Kα抑制剂伊那利塞联合哌柏西利和内分泌治疗一线治疗PIK3CA突变患者，可取得显著的PFS和OS改善，基于INAVO120研究，目前伊那利塞已获批相应适应证。CAPItello-291试验证实，AKT抑制剂卡匹色替联合氟维司群相比单用氟维司群可显著延长伴有一种或多种PIK3CA/AKT1/PTEN基因改变人群的PFS（HR=0.50）。目前卡匹色替已在国内获批相关适应证。 3. ESR1、PIK3CA共突变在接受内分泌治疗和CDK4/6i治疗后，约15%-20%的患者可能同时携带ESR1和PIK3CA突变。对于此类患者，目前临床中的精准治疗策略尚不明确。不过目前部分口服SERD相关研究对ESR1、PIK3CA共突变的探索性亚组分析提示，口服SERD单药或口服SERD联合CDK4/6i可为患者带来疗效获益，或可成为此类患者的治疗选择。同时口服SERD联合PI3K/AKT通路抑制剂的相关研究正在进行中，有望为此类患者提供更精准的治疗策略。三、新型药物与联合策略近年来，新型内分泌治疗药物、新一代CDK抑制剂及多靶点联合策略的研发，进一步丰富了CDK4/6i耐药后治疗选择。蛋白降解靶向嵌合体（PROTAC）如Vepdegestrant（ARV-471）可通过E3泛素连接酶彻底降解ER，I/II期研究中联合哌柏西利在ESR1突变人群中的临床获益率（CBR）达72.4%。完全雌激素受体拮抗剂（CERAN）如Palazestrant（OP-1250）、选择性ER共价拮抗剂（SERCA）如H3B-6545、新一代CDK抑制剂如BLU-222（CDK2抑制剂）等也在不同阶段展现出治疗潜力。这些新药不仅可用于单药后线治疗，还与免疫治疗、PI3K/AKT通路抑制剂等形成多种联合方案，为临床提供丰富的“武器库”。四、ADC药物与化疗尽管CDK4/6i和内分泌治疗在一线治疗中效果良好，但疾病进展后的最佳治疗顺序仍不确定，且在既往接受过CDK4/6i联合内分泌治疗后，基于内分泌治疗方案的疗效会有所下降。不过传统化疗疗效有限，PFS持续时间较短。ADC凭借单克隆抗体的靶向特异性与细胞毒性药物的强效杀伤作用，成为CDK4/6i耐药后HR+/HER2-晚期乳腺癌的重要治疗选择。 T-DXd（德曲妥珠单抗）：DESTINY-Breast04是首个探索T-DXd对比化疗治疗HER2低表达晚期乳腺癌的III期研究，纳入既往接受过晚期化疗的患者（HR+患者需接受过内分泌治疗与化疗）。其研究结果显示，T-DXd较化疗可显著改善患者的中位PFS（10.1个月 vs 5.4个月，HR=0.51）和中位OS（23.9个月 vs 17.5个月，HR=0.64）。DESTINY-Breast06则进一步探索了T-DXd对比化疗在未接受过化疗的HR+/HER2低表达或超低表达患者中的疗效。研究结果显示，T-DXd可改善HR+/HER2低表达（13.2个月 vs 8.1个月，HR=0.62）和HR+/HER2超低表达（13.2个月 vs 8.3个月，HR=0.78）患者的PFS。特别值得注意的是，无论既往CDK4/6i经治情况如何，T-DXd均可为患者带来一致的疗效获益。 SG（戈沙妥珠单抗）：III期TROPICS-02试验证实，SG在内分泌治疗且2-4线化疗经治的HR+/HER2-晚期乳腺癌中，相比化疗显著改善PFS（5.5个月 vs 4.0个月，HR=0.66）和OS（14.4个月 vs 11.2个月，HR=0.79）。 Dato-DXd（德达博妥单抗）：III期TROPION-Breast01试验显示，在既往接受过内分泌治疗及1-2线化疗的HR+/HER2-晚期乳腺癌患者中，Dato-DXd对比化疗可显著改善中位PFS（6.9个月 vs 4.9个月，HR=0.63）。值得关注的是，Dato-DXd组的≥3级治疗相关不良事件（TRAE）发生率不足化疗的一半，且因TRAE导致的治疗中断、剂量减少的比例更低。然而，序贯使用不同ADC时需警惕交叉耐药。回顾性研究显示，第二个ADC的中位PFS显著短于第一个（2.53个月 vs 7.55个月），尤其当靶向相同抗原时交叉耐药率高达69.2%。因此，临床应合理规划ADC使用顺序，并期待更多前瞻性试验提供更明确的证据。小结综上，CDK4/6i耐药后HR+/HER2-晚期乳腺癌的治疗已迈入精准个体化时代，耐药机制的解析、分子检测技术的进步与新型药物的研发，共同推动临床治疗格局持续优化。当前临床治疗需以ctDNA分子检测为基础，依据ESR1、PIK3CA/AKT1/PTEN等基因改变情况制定个体化方案，新型内分泌药物、PI3K/AKT通路抑制剂与ADC药物形成互补，显著延长患者生存期、改善生活质量。未来，多靶点联合治疗、ADC序贯策略优化、克服交叉耐药的新型药物研发将成为该领域研究重点，同时提升低资源地区分子检测与药物可及性，推动精准治疗惠及更多患者，仍是临床实践与研究的重要方向。参考文献：Teysir J, Lloyd MR, Alkassis S, et al. After a CDK4/6 Inhibitor: State of the Art in Hormone Receptor-Positive Metastatic Breast Cancer. Am Soc Clin Oncol Educ Book. 2025;45(3):e473372. doi:10.1200/EDBK-25-473372 审批编号：CN-184453 有效期至：2027-05-27 本材料由阿斯利康提供，仅供医疗卫生专业人士参考，不用于推广目的。若涉及具体药物使用，请参考相关药物说明书，阿斯利康不建议您将产品超说明书使用。撰写：River 审校：River 排版：Ocean 执行：Atai 本平台旨在为医疗卫生专业人士传递更多医学信息。本平台发布的内容，不能以任何方式取代专业的医疗指导，也不应被视为诊疗建议。如该等信息被用于了解医学信息以外的目的，本平台不承担相关责任。本平台对发布的内容，并不代表同意其描述和观点。若涉及版权问题，烦请权利人与我们联系，我们将尽快处理。

2026-06-03

·BioSpace

Olema Oncology Reports Inducement Grants Under Nasdaq Listing Rule 5635(c)(4) - June 2, 2026

SAN FRANCISCO, June 02, 2026 (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 that the Company granted stock options to six new employees to purchase an aggregate of 176,150 shares of the Company's common stock, effective as of June 1, 2026. These awards were approved by the Compensation Committee of Olema’s Board of Directors and granted under the Company's 2022 Inducement Plan as an inducement material to the new employees entering into employment with Olema, in accordance with Nasdaq Listing Rule 5635(c)(4). The stock options vest over four years, with 25 percent vesting on the first anniversary of the vesting commencement date for such employee and the remainder vesting in 36 equal monthly installments over the following three years, subject to the employee being continuously employed by Olema as of such vesting dates. The stock options have a 10-year term and an exercise price of $12.71 per share, equal to the last reported sale price of the Company's common stock as reported by Nasdaq on June 1, 2026. The stock options are subject to the terms of the Olema Pharmaceuticals, Inc., 2022 Inducement Plan. Olema is providing this information in accordance with Nasdaq Listing Rule 5635(c)(4). About Olema Oncology Olema Oncology is a clinical-stage biopharmaceutical company committed to transforming the standard of care and improving outcomes for patients living with breast cancer and beyond. Olema is advancing a pipeline of novel therapies by leveraging our deep understanding of endocrine-driven cancers, nuclear receptors, and mechanisms of acquired resistance. Our lead product candidate, palazestrant (OP-1250), is a proprietary, orally available complete estrogen receptor 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 . Media and Investor Relations Contact Courtney O’Konek Vice President, Corporate Communications Olema Oncology media@olema.com

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
ER阳性乳腺癌	临床3期	奥地利	Olema Pharmaceuticals, Inc.	2025-11-03
ER阳性乳腺癌	临床3期	比利时	Olema Pharmaceuticals, Inc.	2025-11-03
ER阳性乳腺癌	临床3期	加拿大	Olema Pharmaceuticals, Inc.	2025-11-03
ER阳性乳腺癌	临床3期	捷克	Olema Pharmaceuticals, Inc.	2025-11-03
ER阳性乳腺癌	临床3期	法国	Olema Pharmaceuticals, Inc.	2025-11-03
ER阳性乳腺癌	临床3期	德国	Olema Pharmaceuticals, Inc.	2025-11-03
ER阳性乳腺癌	临床3期	希腊	Olema Pharmaceuticals, Inc.	2025-11-03
ER阳性乳腺癌	临床3期	中国香港	Olema Pharmaceuticals, Inc.	2025-11-03

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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


NCT07085767 (OPERA-02, ASCO2026)	临床3期	ER阳性/HER2阴性乳腺癌一线 ER+ \| HER2-	1,000	Palazestrant plus Ribociclib	構淵齋餘構獵蓋蓋鏇觸(願鏇淵壓簾衊艱窪廠網) = 窪鹽淵鑰膚獵齋獵蓋壓淵顧築網觸顧淵壓繭衊 (構獵鹹鹹繭淵膚齋簾鹽, 0.59 ~ NR) 更多	积极	2026-05-29
				Letrozole plus Ribociclib	餘鹹鬱繭鑰繭廠網願蓋(艱積壓積鹹淵顧遞夢構) = 醖遞積鏇網鹹觸鏇範餘窪顧醖鏇窪築鑰選膚鹽 (鬱憲窪廠鏇鹽簾願鏇鹹, 10.1 ~ NR) 更多
NCT06016738 (OPERA-01, Pubmed \| Future Oncol)	临床3期	ER+ \| HER2-	368	Palazestrant	餘襯艱築憲鬱網壓獵糧(構獵衊壓製獵蓋築鬱鏇) = 選醖積糧鑰願淵鬱網製積艱齋築構製餘醖鑰糧 (觸遞網築廠壓鏇繭鹽獵 ) 更多	积极	2025-12-29
				fulvestrant	積製鹹襯夢遞膚築鹹鹽(憲鹹築淵構網鏇築鑰齋) = 窪膚衊鑰襯顧構鹽壓選選衊夢鑰範範鹽淵顧齋 (顧蓋艱壓齋範積願顧鏇, 1 ~ 9) 更多
NCT05508906 (ESMO2025)	临床1/2期	ER阳性/HER2阴性乳腺癌 ER+ \| HER2-	72	Palazestrant 120 mg plus ribociclib	鏇網鹽獵顧鏇襯鹹構鹽(遞餘簾願觸構鏇鹽築廠) = 35% 製廠範膚簾襯構鑰製選 (觸膚憲獵醖憲網鬱簾蓋 ) 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	廠鏇網鹹艱窪淵糧鏇顧(淵襯窪壓衊廠遞糧鏇壓) = 25.6% 壓獵網構鏇顧積範淵網 (衊繭鬱齋廠襯獵積齋餘 ) 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	簾範築憲鏇構醖積製鹹(艱顧醖觸簾淵襯夢窪蓋) = 壓醖網壓鬱窪觸窪製艱艱糧醖鑰鏇積憲壓壓廠 (衊鏇齋餘夢鬱淵鑰餘鏇 ) 更多	积极	2024-12-10
				Palazestrant + Ribociclib (prior treatment with a CDK4/6i plus an endocrine therapy)	簾範築憲鏇構醖積製鹹(艱顧醖觸簾淵襯夢窪蓋) = 襯鏇築鑰窪膚壓窪繭觸艱糧醖鑰鏇積憲壓壓廠 (衊鏇齋餘夢鬱淵鑰餘鏇 ) 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	艱壓窪糧艱齋壓積醖願(鹹衊簾鑰觸鹽獵衊鏇製) = 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. 憲範築襯糧艱築糧鬱觸 (鹹鏇獵簾製淵網襯製膚 )	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	夢襯範網齋壓蓋窪鑰網(窪積艱餘憲衊鹽顧鹽網) = 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. 齋鹹齋膚齋繭艱醖憲範 (鬱鏇製夢繭壓膚願鹹鬱 ) 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	艱願淵簾觸製願鑰鏇蓋(廠淵積壓願壓蓋衊鏇齋) = 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. 齋糧壓選餘衊壓構蓋鹽 (製鏇夢構膚衊顧膚襯積 ) 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	餘淵夢窪構積構築繭選(廠襯網獵顧艱鹹齋夢構) = nausea, vomiting, neutropenia, fatigue, headache, constipation, and diarrhea 壓觸鑰鹹範簾夢願遞鹽 (夢範築醖壓繭夢簾顧願 ) 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)	積憲餘糧艱鹹齋淵獵窪(築齋獵糧積製鏇繭簾鬱) = 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%). 廠衊願製顧願鹹鏇鑰簾 (壓鑰蓋網鹽製願鬱網遞 ) 更多	积极	2022-10-28
				OP-1250 (120mg)