– Bayer announced today initiation of a Phase I clinical trial with

– 拜耳今天宣布启动了一项 I 期临床试验

225 Ac-GPC3 (BAY 3547926), an investigational targeted alpha radiopharmaceutical being developed to treat tumors expressing Glypican-3 (GPC3) in patients with advanced hepatocellular carcinoma (HCC). Oncofetal protein GPC3 is a membrane-associated proteoglycan which is overexpressed in 70-75% of HCC lesions making it an attractive target for targeted radionuclide therapy.[1].

225 Ac-GPC3（BAY 3547926）是一种正在开发的靶向α放射性药物，用于治疗表达磷脂酰肌醇蛋白聚糖-3（GPC3）的肿瘤，针对晚期肝细胞癌（HCC）患者。胎瘤蛋白GPC3是一种膜相关蛋白聚糖，在70-75%的HCC病灶中过度表达，因此成为靶向放射性核素治疗的一个有吸引力的目标。[1]

[2] The first-in-human, dose escalation study (

[2] 首次人体试验，剂量递增研究 (

NCT06764316

NCT06764316

) will evaluate the safety, tolerability and preliminary efficacy of BAY 3547926 alone, and as a combination therapy in patients with advanced HCC.

）将评估 BAY 3547926 单独使用及作为联合疗法在晚期肝细胞癌患者中的安全性、耐受性和初步疗效。

“Hepatocellular carcinoma continues to be a devastating disease for millions of patients and a pressing unmet need in cancer care. The launch of the Phase I trial using the

“肝细胞癌对于数百万患者来说仍然是一种毁灭性的疾病，也是癌症治疗中一个迫切且未满足的需求。使用

Ac-GPC3 radionuclide therapy marks an important milestone in our commitment to develop new medicines targeting cancer cells with high effect size and precision to improve the lives of people living with cancer,” said Dominik Ruettinger, M.D., Ph.D., Global Head of Research and Early Development for Oncology at Bayer’s Pharmaceuticals Division.

“Ac-GPC3放射性核素疗法标志着我们在致力于开发针对癌细胞的高效、高精准度新药物方面迈出了重要一步，这将改善癌症患者的生活，”拜耳制药部门肿瘤学全球研发和早期开发主管Dominik Ruettinger博士表示。

“Through continued research innovation we can unlock the full potential of targeted alpha therapies which is an emerging class of targeted radionuclide therapy and a strategic focus area for Bayer’s precision oncology development portfolio.”.

“通过持续的研究创新，我们可以充分释放靶向α疗法的潜力，这是新兴的靶向放射性核素疗法类别，也是拜耳精准肿瘤学开发组合的战略重点。”

Liver cancer, including hepatocellular carcinoma, is the third leading cause of cancer-related deaths in the world with almost 900,000 new cases annually.[3] It is the most rapidly growing cause of cancer deaths in the US accounting for approximately 2% of new cases and 5% of cancer deaths.[4] Despite recent scientific advancements, most patients do not experience durable therapeutic benefits from the currently available treatments..

肝癌，包括肝细胞癌，是全球癌症相关死亡的第三大原因，每年新增近90万例。[3] 它是美国癌症死亡增长最快的原因，约占新发病例的2%和癌症死亡的5%。[4] 尽管近年来科学取得了进展，但大多数患者仍未从现有治疗中获得持久的疗效。

Targeted alpha therapy (TAT) has the potential to address high unmet medical need across various cancer types. Bayer’s growing TAT portfolio combines alpha particle-emitting radionuclides with different targeting moieties.

靶向α疗法（TAT）有潜力满足多种癌症类型中未被满足的高医疗需求。拜耳不断增长的TAT产品组合将发射α粒子的放射性同位素与不同的靶向部分结合在一起。

Ac-GPC3 is the third TAT program in clinical development and the first investigational targeted radiopharmaceutical for Bayer in HCC. The newly disclosed targeted alpha conjugate joins

Ac-GPC3是第三个处于临床开发阶段的TAT项目，也是拜耳在肝细胞癌（HCC）领域的首个研究性靶向放射性药物。此次新披露的靶向α结合物加入到了...

Ac-PSMA-Trillium, which are currently in Phase I clinical trials in patients with advanced metastatic castration resistant prostate cancer.

目前正处于晚期转移性去势抵抗性前列腺癌患者的I期临床试验中。

On April 28, 2025 Bayer introduced

2025年4月28日，拜耳公司推出

Ac-GPC3 in an oral presentation during the “New Drugs on the Horizon” session at the AACR (American Association of Cancer Research) Annual Meeting, showcasing preclinical characterization of the asset including the low uptake and fast clearance from normal organs as well as induction of tumor regression in .

在AACR（美国癌症研究协会）年会的“新药前沿”环节中，Ac-GPC3在口头报告中展示了该药物的临床前特性，包括在正常器官中的低摄取和快速清除，以及在肿瘤消退方面的诱导作用。

models. Recognition in this special symposium highlights the company’s commitment for precision oncology development portfolio.

模型。此次特别研讨会的认可突显了该公司对精准肿瘤学发展组合的承诺。

About BAY 3547926

关于BAY 3547926

BAY 3547926 is an investigational targeted alpha radiopharmaceutical being developed to treat tumors expressing Glypican-3 (GPC3) in patients with advanced hepatocellular carcinoma (HCC). It is composed of a GPC3 targeting high affinity antibody radiolabeled with actinium-225 (

BAY 3547926 是一种正在开发的靶向α放射性药物，用于治疗表达磷脂酰肌醇蛋白聚糖-3（GPC3）的晚期肝细胞癌（HCC）患者。它由一个高亲和力的GPC3靶向抗体与锕-225（actinium-225）放射性标记组成。

Ac-GPC3 delivers highly potent alpha-particles to the GPC3-expressing cancer cells, with the potential to inducing DNA double-strand breaks, reducing cancer cell viability which may potentially cause anti-tumor activity.

Ac-GPC3 将高活性的 α 粒子递送到表达 GPC3 的癌细胞，可能诱导 DNA 双链断裂，降低癌细胞存活率，从而可能引发抗肿瘤活性。

About Targeted Alpha Therapy

关于靶向α疗法

Targeted alpha therapy (TAT) is an emerging class of radionuclide therapy that can be used against a variety of tumors. It delivers alpha particle radiation directly to the tumor inside the body, either via its bone-seeking property (radium-223) or by combining alpha radionuclides, such as actinium-225, with specific targeting moieties..

靶向α治疗（TAT）是一类新兴的放射性核素治疗，可用于对抗多种肿瘤。它通过骨骼靶向特性（镭-223）或结合特定靶向部分的α放射性核素（如锕-225），将α粒子辐射直接递送至体内的肿瘤部位。

Actinium-225 is an alpha particle–emitting radionuclide with a 9.9-day half-life. Alpha particles deposit highly ionizing radiation over a short range. This localized delivery of the radioactive payload induces irreparable DNA double-strand breaks, often resulting in cell death. At the same time, because the energy travels a short range, damage to nearby normal tissues is much reduced.[5],[6],[7] .

锕-225是一种发射α粒子的放射性核素，其半衰期为9.9天。α粒子在短距离内释放高电离辐射。这种局部递送放射性有效载荷会诱导不可修复的DNA双链断裂，通常导致细胞死亡。同时，由于能量传播范围较短，对附近正常组织的损伤大大减少。[5],[6],[7]

About Oncology at Bayer

关于拜耳的肿瘤学

Bayer is committed to delivering science for a better life by advancing a portfolio of innovative treatments. The company has the passion and determination to develop new medicines that help improve and extend the lives of people living with cancer. The oncology franchise at Bayer includes several marketed products across diverse indications and multiple compounds in different stages of clinical development.

拜耳致力于通过推进一系列创新治疗方案来为更美好的生活提供科学支持。该公司有热情和决心开发新药物，帮助改善和延长癌症患者的生命。拜耳的肿瘤学产品组合包括多种已上市的产品，涵盖不同的适应症，同时还有多个化合物处于临床开发的不同阶段。

We have a wealth of expertise in areas including Tumor Cell Intrinsic Pathways, Targeted Radionuclide Therapies, and selective Next-Generation Immuno-Oncology. With our portfolio we are advancing cancer treatments from early to metastatic stage, with the goal of extending survival while limiting side effects for the cancer patients we serve..

我们在肿瘤细胞内在通路、靶向放射性核素治疗和选择性下一代免疫肿瘤学等领域拥有丰富的专业知识。通过我们的产品组合，我们正在推动癌症治疗从早期到转移阶段的发展，目标是延长患者的生存期，同时减少我们所服务的癌症患者的副作用。

About Bayer

关于拜耳

Bayer is a global enterprise with core competencies in the life science fields of health care and nutrition. In line with its mission, “Health for all, Hunger for none,” the company’s products and services are designed to help people and the planet thrive by supporting efforts to master the major challenges presented by a growing and aging global population.

拜耳是一家在医疗保健和营养等生命科学领域具有核心竞争力的全球性企业。秉承“人人健康，无饥饿”的使命，公司通过支持应对不断增长和老龄化的全球人口所带来的重大挑战，设计其产品和服务以帮助人类和地球繁荣发展。

Bayer is committed to driving sustainable development and generating a positive impact with its businesses. At the same time, the Group aims to increase its earning power and create value through innovation and growth. The Bayer brand stands for trust, reliability and quality throughout the world. In fiscal 2024, the Group employed around 93,000 people and had sales of 46.6 billion euros.

拜耳致力于通过其业务推动可持续发展并产生积极影响。同时，集团旨在通过创新和增长提高盈利能力并创造价值。拜耳品牌在全球范围内代表信任、可靠性和质量。2024财年，该集团拥有约93,000名员工，销售额达466亿欧元。