SHANGHAI, Oct. 23, 2023 /PRNewswire/ -- From October 20 to 24, the 2023 ESMO Congress was held in Madrid, Spain. LX-039, an innovative anti-tumor drug developed by Luoxin Pharmaceuticals Group Stock Co., Ltd. (Luoxin Pharmaceutical), was selected for poster presentation at the 2023 ESMO Annual Congress..

上海，2023年10月23日/PRNewswire/-10月20日至24日，2023年ESMO大会在西班牙马德里举行。Luoxin Pharmaceuticals Group Stock Co.，Ltd。（Luoxin Pharmaceutical）开发的创新抗肿瘤药物LX-039被选中，于2023年ESMO年会上发表海报。。

ESMO is one of the most influential oncology conferences globally, attracting over 30,000 professionals every year from more than 150 countries and regions. The Congress covers basic research, translational research, and the latest advancements in clinical studies, providing an exchange platform in clinical diagnosis, treatment, and academic discussions..

ESMO是全球最具影响力的肿瘤学会议之一，每年吸引来自150多个国家和地区的30000多名专业人员。大会涵盖基础研究，转化研究和临床研究的最新进展，为临床诊断，治疗和学术讨论提供交流平台。。

LX-039 is an innovative selective estrogen receptor degrader (SERD) for oral administration. The aims of the dose escalation and expansion phase I study was to explore the safety, tolerability, efficacy, pharmacokinetics (PK) and pharmacodynamics (PD) profiles of LX-039 in postmenopausal patients with ER+ and HER2- advanced breast cancer who have failed endocrine therapy.

LX-039是一种用于口服的创新型选择性雌激素受体降解剂（SERD）。剂量递增和扩展I期研究的目的是探讨LX-039在ER+和HER2-晚期乳腺癌失败的绝经后患者中的安全性，耐受性，有效性，药代动力学（PK）和药效学（PD）谱内分泌治疗。

The study was led by Professor Hu Xichun from Fudan University Shanghai Cancer Center..

该研究由复旦大学上海肿瘤中心胡锡春教授领导。。

In a 3+3 design, the trial evaluated the safety and tolerability from a daily dose of 50 mg to 1200 mg, with two dosage groups selected for expansion. [18F] Fluoroestradiol PET/CT imaging was used for PD study. All 44 enrolled subjects had previously undergone multiple lines of endocrine therapy. Specifically, 72.7% had received second-line therapy or higher.

在3+3设计中，试验评估了50 mg至1200 mg日剂量的安全性和耐受性，并选择了两个剂量组进行扩增。[18F]氟雌二醇PET/CT成像用于PD研究。所有44名入选受试者以前都接受过多线内分泌治疗。具体而言，72.7%接受过二线或更高的治疗。

More than half had been treated with fulvestrant, a medication commonly used for hormone receptor-positive breast cancer. Also, over 50% had received advanced chemotherapy, and 40.9% had been treated with CDK4/6 inhibitors..

超过一半的人接受了氟维司群治疗，氟维司群是一种常用于激素受体阳性乳腺癌的药物。此外，超过50%接受过晚期化疗，40.9%接受过CDK4/6抑制剂治疗。。

Maximum tolerated dose (MTD) was not reached in this study. Most adverse events are graded as mild to moderate (grade 1-2). The exposure of LX-039 increased along with the dose escalation, and no obvious accumulation after multiple doses. Inhibition of the ER pathway is observed in all subjects participating in the PD exploration.

本研究未达到最大耐受剂量（MTD）。大多数不良事件分级为轻度至中度（1-2级）。LX-039的暴露随着剂量递增而增加，并且在多次剂量后没有明显的积累。在参与PD探索的所有受试者中观察到ER途径的抑制。

Four subjects achieved partial response, with an objective response rate of 10.8% and a clinical benefit rate at 24 weeks of 40%. LX-039 demonstrates good tolerability and PK/PD properties in ER+ and HER2- advanced breast cancer and shows preliminary anti-tumor activity. These encouraging results suggest that LX-039 holds great potential for further development.

4名受试者获得部分缓解，客观缓解率为10.8%，24周时临床获益率为40%。LX-039在ER+和HER2-晚期乳腺癌中表现出良好的耐受性和PK/PD特性，并显示出初步的抗肿瘤活性。这些令人鼓舞的结果表明LX-039具有进一步发展的巨大潜力。

Consequently, a phase II study is under planning..

因此，正在计划进行II期研究。。

About 75% of breast cancer cases are classified as ER+. This subtype of breast cancer relies on the estrogen signaling pathway for its growth and progression. The primary therapeutic approach for ER+ breast cancer involves inhibiting the estrogen signaling pathway through various methods. Notably, drugs like tamoxifen and fulvestrant have been utilized in clinical settings to target the ER pathway.

大约75%的乳腺癌病例被归类为ER+。这种乳腺癌亚型的生长和发展依赖于雌激素信号通路。ER+乳腺癌的主要治疗方法涉及通过各种方法抑制雌激素信号传导途径。值得注意的是，他莫昔芬和氟维司群等药物已在临床环境中用于靶向ER途径。

However, tamoxifen resistance and treatment non-compliance with fulvestrant have led to unmet clinical needs..

然而，他莫昔芬耐药和治疗不依从氟维司群导致临床需求未得到满足。。

LX-039, an orally administered selective ER degrader (SERD) developed by Louxin Pharmaceutical, specifically focuses on modulating the estrogen signaling pathway. It antagonizes ER actions and promotes its ubiquitination and degradation within breast cancer cells, downregulating ER expression. LX-039 offers unique therapeutic benefits compared to selective ER modulators and aromatase inhibitors.

由Louxin Pharmaceutical开发的口服选择性ER降解剂（SERD）LX-039特别关注调节雌激素信号传导途径。它拮抗ER作用并促进其在乳腺癌细胞内的泛素化和降解，下调ER表达。与选择性ER调节剂和芳香化酶抑制剂相比，LX-039提供独特的治疗益处。

Additionally, its oral formulation enhances patient convenience and compliance, as it eliminates the need for injections. There are currently no domestically available oral drugs with a similar mechanism of action to LX-039 in the market..

此外，其口服制剂增强了患者的便利性和依从性，因为它消除了注射的需要。目前市场上没有国内可用的口服药物具有与LX-039类似的作用机制。。

References:

参考文献：

Wang Y, Ayres K L, Goldman D A, et al. 18F-fluoroestradiol PET/CT measurement of estrogen receptor suppression during a phase I trial of the novel estrogen receptor-targeted therapeutic GDC-0810: using an imaging biomarker to guide drug dosage in subsequent trials[J]. Clinical Cancer Research, 2017, 23(12): 3053-3060..

Wang Y，Ayres K L，Goldman D A等人18F-氟雌二醇PET/CT测量新型雌激素受体靶向治疗性GDC-0810的I期试验期间的雌激素受体抑制：使用成像生物标志物指导药物剂量在随后的试验中[J]。临床癌症研究，2017,23（12）：3053-3060。。

Patel H K, Bihani T. Selective estrogen receptor modulators (SERMs) and selective estrogen receptor degraders (SERDs) in cancer treatment[J]. Pharmacology & therapeutics, 2018, 186: 1-24.

Patel H K，Bihani T.癌症治疗中的选择性雌激素受体调节剂（SERMs）和选择性雌激素受体降解剂（SERDs）[J]。药理学与治疗学，2018186:1-24。

About Luoxin Pharma

关于罗新制药

Luoxin Pharmaceutical Group Stock Co., Ltd. ('Luoxin Pharma', stock code: 002793.SZ ) was founded in 1988. With the mission of 'Source of health', Luoxin Pharma insists upon innovation of science and technology, focuses on the unmet medical needs in GI, respiratory and oncology, etc., and dedicates bringing more innovative medicine to patients around the world..

罗新制药集团股票有限公司（“罗新制药”，股票代码：002793.SZ）成立于1988年。凭借“健康来源”的使命，罗新制药坚持科技创新，注重胃肠道，呼吸系统和肿瘤学等未满足的医疗需求，致力于为世界各地的患者带来更多创新药物。。

Luoxin Pharma has a rich and competitive portfolio of products and the star products take the lead in GI and respiratory. Many products were listed in major science and technology projects, such as National Major New Product Plan, National Torch Plan as well as Major New Drug R&D. In addition, having been ranking among Top 100 Chinese Pharmaceutical Enterprises since 2006, and among Best Enterprises in Chinese Pharmaceutical R&D Pipelines since 2011, Luoxin Pharma was recognized as State Key High-tech Enterprise, State Technology Innovation Model Enterprise, National Industrial Quality Model Enterprise, and multiple scientific research achievements were awarded the 2nd prize for the State Sci.

罗新制药拥有丰富而有竞争力的产品组合，星级产品在GI和呼吸领域占据领先地位。许多产品被列入国家重大新产品计划，国家火炬计划和重大新药研发等重大科技项目。此外，自2006年以来一直位居中国制药企业前100名，自2011年以来一直位居中国制药研发管道最佳企业之列，罗新制药被认定为国家重点高科技企业，国家技术创新示范企业，国家工业质量模型企业，多项科研成果获国家科学院二级奖。

& Tech Progress..

&技术进步。。

For more information, please visit www.luoxin.cn.

欲了解更多信息，请访问www.luoxin.cn。

SOURCE Luoxin Pharmaceutical Group Stock Co., Ltd.

来源罗新制药集团股份有限公司。