The investigators will study SPECT imaging of radiopharmaceutical therapies given as standard of care or as part of other compatible research protocols. The goal is to validate the quantitative SPECT image reconstruction methods developed in this proposal, and to investigate the relation between dosimetry calculated from SPECT images and the outcomes. Patients will be recruited for SPECT/CT imaging during treatment. This is an observational study no additional new drugs or activities will be administrated. The investigators will perform SPECT imaging on a total of 80 patients (
20 each from year 2 to year 5). Each participant will be imaged 3 times after the first and last cycles of planned radiopharmaceutical therapy.

开始日期2025-02-03

申办/合作机构

The Sidney Kimmel Comprehensive Cancer Center

[+1]

NCT05924672

/ Recruiting临床2期IIT

Efficacy of Ra-223 in PSMA PET Optimally Selected Patients

This phase II trial studies how well prostate-specific membrane antigen (PSMA) positron emission tomography (PET) scans (in combination with bone scans) work in selecting patients for Ra-223 radiation therapy that have castration-resistant prostate cancer that has spread from where it first started (primary site) to the bones (bone metastasis). Ra-223 is a type of therapy that emits radiation. Radiation gives off energy which can kill tumor cells and other cells that may support the tumor cells. Ra-223 is given by infusion into the veins, where it is absorbed by the bones. PSMA PET is a type of scan used to detect prostate cancer tumors. PSMA is a radioactive tracer that binds to a specific protein that is found on prostate tumor cells. The PSMA tracer shows the areas on the PET scan where tumor cells are active. A PET scan uses a special camera to detect the energy given off from radioactive tracers (such as PSMA) to make detailed pictures of areas where the tracer accumulates in the body. The PET scan is often combined with a magnetic resonance imaging (MRI) or computed tomography (CT) scan, which helps to map the locations where PSMA has accumulated. PSMA PET scans may be able to select patients that will benefit the most from Ra-223 treatment.

开始日期2024-08-30

申办/合作机构

The University of California, San Francisco

[+1]

NL-OMON56209

/ SuspendedN/A

A FEASIBILITY STUDY OF 177LU-PSMA RADIOLIGAND THERAPY ALTERNATED WITH RADIUM-223 IN PATIENTS WITH BONE-METASTATIC, OLIGO-METASTATIC HORMONE-SENSITIVE PROSTATE CANCER AFTER CURATIVE THERAPY. THE DUET STUDY - DUET trial

开始日期2023-12-01

申办/合作机构-

100 项与二氯化镭[223Ra] 相关的临床结果

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100 项与二氯化镭[223Ra] 相关的转化医学

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100 项与二氯化镭[223Ra] 相关的专利（医药）

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964

项与二氯化镭[223Ra] 相关的文献（医药）

2025-06-01·CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

The role of radium-223 in the evolving treatment landscape of metastatic castration-resistant prostate cancer: A narrative review

Review

作者: Pinto, Álvaro ; Domínguez, Mario ; Rodriguez-Vida, Alejo ; Gómez-Iturriaga, Alfonso ; Castro, Elena ; Vallejo-Casas, Juan Antonio

The treatment of metastatic castration-resistant prostate cancer (mCRPC) has been rapidly evolving over the last two decades. The advent of new androgen receptor pathway inhibitors (ARPIs) such as abiraterone acetate or enzalutamide marks a great advance for treating mCRPC patientd in the pre- and post-docetaxel settings. The subsequent approval of ARPIs in early stages-i.e., metastatic hormone-sensitive (mHSPC) or nonmetastatic CRPC-led to a realignment of subsequent treatment choices upon progression to mCRPC, given the possibility of cross-resistance between ARPIs. Therapies with mechanisms of action different from those of ARPIs are now the focus of new treatment developments. Also, this anomalous situation brings the focus back to well-known treatments currently used later in the treatment sequence. This is the case of radium-223 which, when administered with enzalutamide, has recently been shown to prolong radiographic progression-free survival vs. enzalutamide alone in the first line in asymptomatic or mildly symptomatic patients with no known visceral metastases. In this narrative review, we summarize the treatment landscape for mCRPC, both from a historical and practical point of view, to understand the new potential of radium-223 as a treatment option in this setting.

2025-04-26·JAPANESE JOURNAL OF CLINICAL ONCOLOGY

Evaluation of optimal timing and therapeutic efficacy of radium-223 therapy for metastatic castration-resistant prostate cancer: a multicenter collaborative study

Article

作者: Kimura, Takahiro ; Urabe, Fumihiko ; Miki, Jun ; Yamamoto, Toshihiro ; Goto, Yuma ; Taneda, Yuki ; Fujiwara, Kensuke ; Kawano, Shota ; Shimomura, Tatsuya ; Imai, Yu ; Tashiro, Kojiro ; Ito, Kagenori ; Atsuta, Mahito ; Kadena, Soshi ; Iwatani, Kosuke ; Nakano, Juria ; Iwamoto, Yuya ; Fukuokaya, Wataru ; Tokuoka, Kenichi ; Tsuzuki, Shunsuke ; Yanagisawa, Takafumi ; Murakami, Masaya

Abstract:

Background:

Despite its demonstrated efficacy in prolonging overall survival (OS) and delaying skeletal-related events in the ALSYMPCA trial, the optimal timing of radium-223 initiation remains unclear. This study investigated factors influencing radium-223 treatment outcomes, including completion rates and survival.

Methods:

This retrospective, multi-institutional study included 164 patients with metastatic castration-resistant prostate cancer (CRPC) who received radium-223 therapy. The primary endpoint was OS following radium-223 initiation. Secondary endpoints included factors associated with incomplete radium-223 treatment (< six cycles) and poor OS. Multivariate Cox regression and multivariate logistic regression analyses were conducted to identify prognostic factors.

Results:

The median OS times after CRPC diagnosis and radium-223 initiation were 39 and 12.5 months, respectively. Kaplan–Meier analysis showed that the OS of patients who completed six cycles of radium-223 treatment was longer than that of those who did not (18 vs. 5 months; P < .001). Multivariate Cox analysis identified Eastern Cooperative Oncology Group performance status (ECOG-PS) ≥ 1 (hazard ratio [HR] = 1.74, P = .046), PSA > 17 ng/ml (HR = 2.93, P < .001), and radium-223 incompletion (HR = 3.23, P < .001) as independent predictors of poor OS. The radium-223 completion rate was 68.3%, and incompletion was significantly associated with prior docetaxel use (odds ratio [OR] = 5.97, P = .001), bone pain (OR = 2.64, P = .024), and PSA > 17 ng/ml at the start of radium-223 treatment (OR = 3.12, P = .013).

Conclusions:

Completion of all six cycles of radium-223 treatment were associated with favorable survival outcomes in metastatic CRPC patients. Prior docetaxel use, bone pain, and elevated PSA levels were significant risk factors for radium-223 incompletion. These findings suggest the importance of initiating radium-223 earlier in the treatment course for patients with favorable clinical profiles to maximize the therapeutic benefits.

2025-04-01·Revista espanola de medicina nuclear e imagen molecular

State of the art and future perspectives of new radinuclides in Nuclear Medicine: Part III

Article

作者: Domínguez, María Luz ; Ramos, Rocío ; Quincoces, Gemma ; Roteta, Ana ; de Arcocha, María ; Torres, Irene ; Rosales, Juan J ; Sancho, Lidia ; Prieto, Elena

In this third installment of the continuing education series, the clinical and therapeutic applications of zirconium, astatine and thorium are analyzed in depth. Although they are not described as theragnostic pairs, each of these radionuclides plays a fundamental role in precision medicine, which is rapidly advancing within Nuclear Medicine. We begin by analyzing zirconium-89, a positron emitter whose long half-life makes it particularly suitable for labeling large molecules with slow kinetics, such as antibodies, playing a crucial role in immunotherapy. The use of astatine-211, an alpha-emitting radionuclide with a simple decay scheme and chemical behavior similar to iodine, is also discussed. Its main challenge lies in its production, as it requires cyclotrons capable of generating highly energetic alpha particle beams. Furthermore, thorium-227, a 100% alpha emitter, is reviewed. This radionuclide exhibits excellent chelation properties, enabling its conjugation with tumor-targeting molecules to produce thorium-labeled conjugates. While this technique is yielding promising preclinical results, the use of thorium faces challenges, including the potential separation of radium-223 from the molecule and the dependence of activity measurements on the time of production. Since it takes 100 days to reach equilibrium, activity assessment is based on photons emitted by its daughter radionuclides. Despite these challenges, these radionuclides are driving the evolution of precision medicine, expanding therapeutic and diagnostic possibilities within Nuclear Medicine.

128

项与二氯化镭[223Ra] 相关的新闻（医药）

2025-05-06

·药时代

诺华、AZ、礼来、BMS、拜耳——5家核药巨头布局全盘点

撰文：幻目放射性药物是一类利用放射性核素释放的辐射（如α、β粒子或俄歇电子）选择性杀伤病变组织的药物。近年来，这一领域发展迅速，预计到2033年，该领域的价值将超过130亿美元。通过5家制药巨头（诺华、阿斯利康、百时美施贵宝、礼来和拜耳）在核药领域布局情况或许可以预测放射性药物的未来前景。1诺华寻求保持核药的领导地位代表药物：Lutathera、Pluvicto诺华是放射性药物竞赛中的领跑者。目前已有两种商业产品：Lutathera，适用于胃肠胰神经内分泌肿瘤（GEP-NET），以及Pluvicto，用于转移性去势抵抗性前列腺癌（mCRPC）。尽管处于领先地位，但诺华继续加强其放射性药物产品管线。2024年5月2日，诺华宣布收购核药生物技术公司Mariana Oncology，诺华支付10亿美元预付款，以及7.5亿美元里程碑付款。图1. Mariana Oncology Inc和诺华收购协议相应款项，来源：药渡数据-全球药物库Mariana的首发管线MC-339，是用于治疗小细胞肺癌的靶向核药。该候选药物由一种肽类小分子组成，经设计可携带放射性锕（Ac）有效载荷。通过使用小分子将有效载荷输送到一个未公开的靶点，输送的剂量是小细胞肺癌细胞的致死剂量，但不会对健康组织造成难以承受的伤害。诺华最近还启动了下一代放射疗法AAA817的两项关键试验，该疗法正在开发中，应用于治疗前列腺癌。与Pluvicto一样，AAA817靶向前列腺特异性膜抗原（PSMA），但携带基于锕的有效载荷，可以提供更高的杀伤效力。除了建立新管线外，诺华还在寻求扩大其当前产品的适应症。2025年3月28日，FDA批准了Pluvicto®（177Lu-PSMA-617），用于前列腺特异性膜抗原（PSMA）阳性的转移性去势抵抗性前列腺癌（mCRPC）患者化疗前的早期治疗。这一批准是前列腺癌治疗领域的重大突破，极大地扩展了Pluvicto®的适用范围，允许在一次雄激素受体途径抑制剂（ARPI）后和化疗前使用Pluvicto®，使更多患者能够在疾病早期受益于这一创新疗法，患者群体预计扩大约三倍。这些战略举措使公司处于有利地位，可以将放射配体疗法从前列腺和神经内分泌肿瘤拓展到患者需求未得到满足的其他领域，比如乳腺癌和肺癌。2阿斯利康将重点放在放射性偶联物上代表药物：FPI-2265、AZD2068阿斯利康于2024年3月以高达24亿美元的价格收购了Fusion Pharmaceuticals，进入了放射性药物领域。尽管是该领域的新人，但阿斯利康将目标定得很高。预计到2030年及以后，放射性偶联物将成为其业务的强大驱动力。阿斯利康的放射性药物管线以FPI-2265（Fusion收购的核心）为基础，该药物由一种靶向PSMA的小分子药物组成，并携带一种可对癌细胞造成无法修复的损害的锕225放射性同位素。FPI-2265正在PSMA阳性mCRPC患者的II期AlphaBreak研究中进行评估，预计将于2025年下半年公布。阿斯利康还在研究AZD2068，这是Fusion的另一种放射性偶联物，旨在靶向表达EGFR和cMET标志物的细胞。该药物目前处于晚期实体瘤的I期研究中，预计最早将于2026年公布结果。除此外，阿斯利康还在研究分子成像和计算病理，这将加强放射性偶联物的递送和监测，最终目标是为患者提供精准的治疗。3BMS:在基于锕的放射治疗领域处于领先地位代表药物：RYZ-101、RYZ-801百时美施贵宝于2023年12月以41亿美元的价格收购了RayzeBio及其基于锕225的平台，从而在放射性制药领域大展拳脚。通过收购RayzeBio，BMS获得了该生物技术公司核药RYZ-101的所有权，该药物靶向2型生长抑素受体，这是一种通常在某些实体瘤上表达的蛋白质。BMS正在进行RYZ-101的三项临床试验：GEP-NETs的III期研究和不可切除的转移性乳腺癌和广泛期SCLC的I期研究。SCLC研究将于今年晚些时候公布，而GEP-NET的关键数据预计将于2026年公布。如果成功，RYZ101可能是第一个在FDA获得批准的基于锕255的放射性药物疗法。BMS还在推进RYZ-801，它由一种与锕225放射性有效载荷结合专有肽的偶联物，靶向GPC3蛋白。RYZ-801于2024年底进入肝细胞癌临床，目前正在招募中。除了这两项临床资产外，对RayzeBio的收购还为BMS提供了多种候选治疗药物。目前正在进行临床前的研究。除了加强放射性药物研发管线外，BMS还在建立生产能力。目前，公司在印第安纳波利斯的生产设施已全面投入运营，可以为临床供应核药。BMS还在在努力扩大该生产点的规模以支持商业生产。4礼来以交易狂潮进入核药领域代表药物：PNT2001和PNT2002在BMS和阿斯利康之前，礼来于2023年10月以14亿美元收购Point Biopharma进入放射性药物领域，该交易于当年12月正式完成。不到一年后，即2024年5月，礼来与Aktis Oncology达成了一项价值高达11亿美元的协议，加大了对放射性药物的投入。这笔交易使礼来能够使用AktisOncology的专有药物发现平台，以开发针对某些癌症靶点的新型放射药物。但礼来并没有就此止步。2024年7月，该公司与Radionetics Oncology达成了另一个战略联盟，预付款为1.4亿美元。致力于针对小分子G蛋白偶联受体的放药开发，用于治疗各种实体瘤。根据该协议，礼来还拥有以10亿美元收购Radionetics的独家权利。通过收购Point，礼来获得了这家生物技术公司的主要资产PNT2002的所有权，这是一种基于PSMA靶向镥177的疗法，旨在为激素治疗后疾病进展的mCRPC患者提供治疗。然而，2023年12月PNT2002的III期读数令人失望：与雄激素受体阻断相比，该药物将死亡或疾病进展的风险降低了29%——这一效果达到统计显著性，但低于分析师的预期。尽管如此，礼来还在其他几个放射性候选药物上押注，包括PNT2001，它靶向PSMA蛋白并携带225锕放射性同位素有效载荷。该药物目前处于前列腺癌的I期开发阶段。除此外，礼来公司还拥有一种使用225-锕的临床前放射性药物候选药物。另一种PNT2003递送镥177并靶向生长抑素受体以治疗GEP-NETs。5拜耳：Xofigo之外建立放射性药物管线代表药物：Xofigo、225Ac-Pelgifatamab、225Ac-PSMA-Trillium除了诺华之外，5家巨头中另一家拥有FDA批准的放射性药物的公司是拜耳。Xofigo是一种镭223二氯化物放射性药物，于2013年被FDA批准用于治疗有症状的骨转移且没有已知内脏转移性疾病的去势抵抗性前列腺癌。然而，与诺华的Lutathera和Pluvicto不同，Xofigo不包含靶标药物。Xofigo利用了镭的化学性质，使其能够与骨矿物质结合，从而帮助将药物定位到骨转移部位。Xofigo的市场表现一直不尽如人意，在2017年达到4.08亿欧元的峰值。拜耳去年没有报告Xofigo的具体销售情况。但这家制药巨头仍试图在当今的放射性制药领域开辟一席之地，2023年5月拜耳与Bicycle Therapeutics达成战略合作。凭借4500万美元的预付款和高达17亿美元的里程碑，拜耳获得了Bicycle的专有肽，用于开发针对几个未公开的癌症靶点的靶向放射疗法。根据其官网，拜耳至少有两种临床阶段的放射性药物疗法正在开发中：225Ac-Pelgifatamab和225Ac-PSMA-Trillium，这两种基于锕的候选药物都处于晚期前列腺癌的早期研究中。参考资料：1.https://www.biospace.com/drug-development/5-big-pharmas-push-boundaries-in-radiopharmaceuticals2.各公司官网图片来源：123rf3718.5亿美元！全球50款最畅销的重磅药物泽布替尼已具上榜实力可排第49名2025-05-0538笔！596亿美元！跨国药企2025年重磅交易达成，中国公司贡献很大2025-05-02【直击现场】「星起点」宣讲会直播：50万资金+专家辅导，寻找下一个代谢病创新药突破者！2025-04-30版权声明/免责声明本文为授权转载文章。本文仅作信息交流之目的，不提供任何商用、医用、投资用建议。文中图片、视频、字体、音乐等素材或为药时代购买的授权正版作品，或来自微信公共图片库，或取自公司官网/网络，部分素材根据CC0协议使用，版权归拥有者，药时代尽力注明来源。如有任何问题，请与我们联系。衷心感谢!药时代官方网站:www.drugtimes.cn联系方式:电话:13651980212微信:27674131邮箱:contact@drugtimes.cn点击这里，查看更多精彩!

放射疗法并购临床3期

2025-04-30

·药智网

核药五霸的厮杀

一个新的百亿美元药物市场正在形成。Precedence Research发布的报告显示，2024年全球放射性药物市场规模为67.4亿美元，预计到2033年，这个数字将以8.2%的复合增长率，达到136.7亿美元。图片来源：同写意虽然该赛道涌现出一批Biotech，凭借创新的技术和管线，正把这种先进疗法带向更广阔的应用市场，可最后的故事不太可能由它们来主导——以诺华、拜耳为代表的制药巨头环伺左右，摩拳擦掌。过去几年，资金越发频繁地流向这片蓝海：不仅是风投机构，还包括来自药企的钱。MNC通过参与Biotech的融资，或者直接引进管线，买下公司，深度参与到这场创新竞赛里。由此，行业格局似乎也逐渐呼之欲出。下文，将梳理五家制药巨头在放射性药物上的布局。它们采取各种策略，希望建立起自己的话语权。1拜耳：先驱不易作为最早一批押注放射性药物的MNC，拜耳2009年就与Algeta达成合作，获得Xofigo的全球独家销售权。Xofigo不包含靶向部分。相反，该药物利用镭的化学性质，使其能够与骨矿物质结合，从而帮助将药物定位到骨周转率高的部位。2013年，FDA批准Xofigo上市，作为全球首款α粒子放射性药物，用于治疗晚期骨转移型去势抵抗性前列腺癌。次年，拜耳顺势斥资29亿美元并购Algeta，完全将Xofigo收入囊中。通过这次收购，拜耳希望借此提振其药物部门。Algeta曾预计，到2018年，Xofigo全球销售额将超过10亿美元，但事实上，它在2017年达到的峰值是4.08亿美元。问题出在临床数据。2017年底，拜耳公布Xofigo与强生的Zytiga、类固醇联合使用的III期出现死亡和骨折事件后，该药物的销售额一直在下降。拜耳2024年财报并未披露Xofigo的销售额。GlobalData预计，Xofigo在2024年的销售收入仅为2.44亿美元，到2030年将降至1.61亿美元。不过，这家巨头正试图重铸自己的荣光。2021年，拜耳收购Noria Therapeutics和PSMA Therapeutics，获得一款靶向PSMA的小分子α粒子疗法的开发权益，进一步扩展其靶向α疗法的肿瘤学产品组合。2023年，通过战略合作，拜耳以4500万美元的预付款和高达17亿美元的里程碑付款，从Bicycle Therapeutics获得专有肽的使用权，计划将之用于开发针对几种未公开的癌症靶点的靶向放射疗法。根据其管线信息，拜耳至少有两种临床阶段的放射性药物正在开发中：225Ac-Pelgifatamab和225Ac-PSMA-Trillium，这两种都是针对晚期前列腺癌的早期研究中的候选药物。2诺华：一骑绝尘有目共睹，当前在放射性药物领域最为成功的MNC，非诺华莫属。跟拜耳相似，这家瑞士制药商通过并购快速建立起自己的版图：2017年，以39亿美元收购的Advanced Accelerator Applications，获得Lutathera——2024年营收同比增长20%，达到7.24亿美元；2018年，以21亿美元收购Endocyte，获得Pluvicto——2024年营收同比增长42%，达到13.92亿美元。Pluvicto以及即将突破“重磅炸弹”门槛的Lutathera证明，监管、制造复杂的放射性药物，同样有自己的广阔市场前景。诺华放射性配体治疗实体瘤战略副总裁Geoff Towle认为，与竞争对手相比，诺华在全球范围内建设了“行业领先的放射性配体研究和生产基地”。这一定程度促成其商业化产品飞速放量。尽管遥遥领先，诺华仍在持续投资放射性药物领域，加强自己的管线组合。2024年，该公司斥资10亿美元收购Mariana Oncology及其前景看好的产品线，其中最有潜力的产品线是MC-339，这是一种正在研究用于治疗小细胞肺癌的放射性疗法。Towle透露，诺华最近还启动了下一代放射疗法AAA817的两项关键试验，用于治疗前列腺癌。与Pluvicto一样，AAA817靶向PSMA，但携带的是基于锕的有效载荷，可以提供更高的效力。除了拓展产品线，另一大被诺华采用的策略，是扩大商业化产品的适应症。例如，3月底，诺华赢得FDA对Pluvicto的关键批准，使该药的潜在患者人数增加三倍，允许其在紫杉烷类化疗之前治疗PSMA阳性转移性去势抵抗性前列腺癌（mCRPC）。诺华介绍，化疗前mCRPC是Pluvicto实现50亿美元峰值销售额的最重要的适应症。现阶段，诺华还在尝试将放射性药物从前列腺和神经内分泌肿瘤，推向患者需求尚未得到满足的其他领域，例如乳腺癌和肺癌。3阿斯利康：抗癌新篇肿瘤治疗业务长期是阿斯利康的“现金牛”。2024年，该板块营收同比增长24%，达到223.53亿美元，占据阿斯利康总营收的41%。而随着产品的迭代，放射性疗法逐渐进入这家英国制药巨头的视野。它透露，核素偶联药物（RDC）已经成为公司肿瘤学研发战略的重要组成部分，也是多元化产品组合的关键——预计RDC将在2030年之后成为阿斯利康业务的强大推动力。2024年，阿斯利康以高达24亿美元收购Fusion Pharmaceuticals，正是进入放射性药物市场。Fusion为其带来了一款候选药物FPI-2265。阿斯利康生物工程和肿瘤靶点发现高级副总裁Puja Sapra透露，FPI-2265针对PSMA阳性mCRPC患者的II/III期试验，预计在2025年下半年获得读数。不过，距离获批上市可能尚需时日。GlobalData认为，该疗法最早将于2028年商业化，到2030年的销售收入也仅为1.82亿美元。阿斯利康还在研究AZD2068，这同样是Fusion开发的另一种RDC，旨在靶向表达EGFR和cMET标记的细胞。目前，AZD2068正处于针对晚期实体肿瘤的I期临床。根据管线规划，预计该研究最早在2026年就会有结果。产品管线之外，阿斯利康也对“分子成像和计算病理学”饶有兴趣。Sapra表示，这将“增强放射性结合物的输送和监测”，最终目标是“为正确的患者提供正确的治疗”。4BMS：锕系先锋诺华的重磅产品虽然正在跑马圈地，但并非没有薄弱环节。例如，Pluvicto、Lutathera选择镥-177这种β核素放射性同位素，就没有α粒子那样能提供更高的能力——比β粒子高400倍，进而引起更频繁的双链DNA断裂，实现高效、精确杀灭肿瘤细胞。理论上，利用锕-225的放射性药物，有可能比已经批准的Lutathera带来更佳的疗效。BMS正着手打造自己的锕系元素产品矩阵。2023年，BMS以41亿美元收购了RayzeBio及其基于锕-225的平台，在放射性药物赛道迈出重大一步。虽然成立时间尚短，RayzeBio却在锕系元素放射性药物治疗方面占据领先地位，拥有多个潜在First-in-Class和Best-in-Class项目。其中，RYZ-101靶向生长抑素受体2（SSTR）的RDC，这是一种通常在某些实体肿瘤中表达的蛋白。围绕RYZ-101，BMS开展了三项临床试验：一项针对胃肠胰神经内分泌肿瘤（GEP-NET）的III期研究，以及一项针对不可切除的转移性乳腺癌和广泛期SCLC的I期研究。BMS透露，针对SCLC的研究结果将于2025年晚些时候公布，而GEP-NET的关键数据预计在2026年对外揭晓。如果一切顺利，RYZ101有望成为美国首个获批的基于锕-255的放射性药物。RYZ-801则是另一款值得关注的候选产品。该药由一种肽与锕-225放射性有效载荷结合而成。据悉，RYZ-801靶向GPC3蛋白，已经在2024年底进入临床，用于治疗肝细胞癌，目前正在招募患者。此外，收购RayzeBio还为BMS带来了“IND生成引擎”，可以在未来几年内产生“几种候选治疗药物”。相关负责人称，BMS正在推进多个临床前项目。而生产制造能力方面，BMS位于美国印第安纳波利斯的工厂已全面投入运营，可以支持临床样品供应。BMS还打算扩大该工厂，以支持商业规模运营。5礼来：全线出击对于治疗用放射性药物，即眼下投资关注的主要细分领域，礼来可谓是刚进“新手村”。2023年10月，通过一笔14亿美元的收购，该MNC真正下场。礼来肿瘤学部门总裁Jacob Van Naarden称，他们对这种新兴治疗方式的潜力感到非常兴奋，并将收购Point Biopharma视为“投资开发多种治疗癌症的放射性药物的开始”。与Point的交易披露时，礼来获得PNT2002、PNT2003这两款处于III期临床的药物，以及几个处于早期阶段项目。不过，PNT2002、PNT2003与诺华两款商业化产品适应症存在重合，意味着它们的上市和销售道路可能并不容易走。2023年12月，PNT2002的III期结果令人失望：与雄激素受体阻断相比，该药物将死亡或疾病进展的风险降低了29%——符合统计学显著性，但低于分析师的预期。这笔14亿美元巨额收购的更大价值，或许是让礼来拥有一个工厂平台。Point是自带生产能力的Biotech，18万平方英尺的园区，属于世界上最大的放射性药物制造工厂之一。并且，陆空交通区位的优势，让货物可以快速进出，覆盖欧美等主要市场。但作为后来者，礼来不打算将鸡蛋放在一个篮子里。相反，它要发挥自己的体量优势，多次下注，尤其是在靶点技术方面，以此提高成功概率。2024年，礼来加快了进军放射性药物的步伐。5月，它从Aktis Oncology引进新型小蛋白技术平台生产放射性药物。7月，礼来又跟Radionetics Oncology签署投资协议，有机会以10亿美元的价格后者收购。此外，作为放射性药物的重要一环，核素的布局也没有被礼来落下。Point已与德国Lu-177生产商ITM Isotope Technologies Munich签订并扩大供应协议，一定程度减轻了礼来在核素方面的压力。2024年8月，礼来还通过可转换贷款方式，向一家名为Ionetix的同位素供应商投资了1000万美元。Ionetix位于美国的工厂运行着一台回旋加速器，该机器通过用质子束轰击镭-226来生产锕-225。来源 | 同写意（药智网获取授权转载）撰稿 | 写意君责任编辑 | 八角声明：本文系药智网转载内容，图片、文字版权归原作者所有，转载目的在于传递更多信息，并不代表本平台观点。如涉及作品内容、版权和其它问题，请在本平台留言，我们将在第一时间删除。合作、投稿 | 马老师 18323856316（同微信）阅读原文，是受欢迎的文章哦

放射疗法并购临床3期财报

2025-04-29

·PipelineReview

Bayer Initiates Phase I Study Targeting GPC3 With Actinium-225 Radiopharmaceutical in Patients With Advanced Hepatocellular Carcinoma

WHIPPANY, NJ, USA I April 29, 2025 I Bayer announced today initiation of a Phase I clinical trial with 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. 1,2 The first-in-human, dose escalation study ( NCT06764316 ) will evaluate the safety, tolerability and preliminary efficacy of BAY 3547926 alone, and as a combination therapy in patients with advanced HCC. “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 225 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. “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.” 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, many doctors are not satisfied with the therapeutic benefits from the currently available treatments. 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. 225 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 225 Ac-Pelgifatamab and 225 Ac-PSMA-Trillium, which are currently in Phase I clinical trials in patients with advanced metastatic castration resistant prostate cancer. On April 28, 2025 Bayer introduced 225 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 in vivo models. Recognition in this special symposium highlights the company’s commitment for precision oncology development portfolio. About 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 ( 225 Ac). 225 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. About Targeted Alpha Therapy 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. 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 About Oncology at Bayer 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. 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. About Bayer 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. 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. R&D expenses amounted to 6.2 billion euros. For more information, go to www.bayer.com . Find more information at https://pharma.bayer.com/ . Follow us on Facebook: http://www.facebook.com/bayer . SOURCE: Bayer

临床1期

100 项与二氯化镭[223Ra] 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	二氯化镭[223Ra]	V10XX03	DB08913

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
前列腺癌	中国	Institute For Energy Technology	2020-08-26
骨转移癌	欧盟	Bayer AG	2013-11-13
骨转移癌	冰岛	Bayer AG	2013-11-13
骨转移癌	列支敦士登	Bayer AG	2013-11-13
骨转移癌	挪威	Bayer AG	2013-11-13
去势抵抗性前列腺癌	美国	Bayer HealthCare Pharmaceuticals, Inc.	2013-05-15

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
去势敏感前列腺癌	临床3期	-	Bayer AG	2023-09-01
转移性前列腺癌	临床3期	-	Bayer AG	2023-09-01
转移性去势抵抗性前列腺癌	临床3期	中国	Bayer AG	2013-03-26
转移性去势抵抗性前列腺癌	临床3期	新加坡	Bayer AG	2013-03-26
转移性去势抵抗性前列腺癌	临床3期	韩国	Bayer AG	2013-03-26
转移性去势抵抗性前列腺癌	临床3期	中国台湾	Bayer AG	2013-03-26
转移性前列腺腺癌	临床2期	美国	Bayer AG	2022-04-28
转移性前列腺腺癌	临床2期	巴西	Bayer AG	2022-04-28
寡转移性前列腺癌	临床2期	美国	Bayer AG	2018-02-27
复发性多发性骨髓瘤	临床2期	美国	Bayer AG	2016-10-01

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临床结果

适应症

分期

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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


NCT04206319 (ASCO_GU2025)	临床2期	非转移性前列腺癌 PSMA+ \| NaF+	18	Radium 223	範壓糧選艱鹹鏇鬱膚顧(艱夢製憲範餘襯夢蓋艱) = Grade 2 toxicities have been rare and no Grade 1 or 2 changes in hemoglobin or platelets have occurred 鹽積醖積築鹽醖憲膚簾 (鹽鹹憲範窪襯壓構艱衊 ) 更多	积极	2025-02-13
ASCO_GU2025	N/A	转移性去势抵抗性前列腺癌	61	Radium-223 re-treatment	齋製襯鑰蓋鑰壓醖鬱構(衊鑰網壓製願鏇鏇選鑰) = 艱積顧醖製壓鬱艱鏇繭窪範廠襯壓鹽醖範艱鏇 (鑰築鹽膚窪鬱範範鏇簾, 11.9 ~ 21.9) 更多	积极	2025-02-13
NCT03002220 (EXCAAPE, CTgov)	临床2期	转移性去势抵抗性前列腺癌	52	radium-223	簾鏇網積選鏇夢憲齋鬱(壓願鏇窪膚範簾壓獵襯) = 範顧獵鑰夢窪網蓋選衊製憲築餘窪襯襯願顧艱 (選積構醖餘積選網繭願, 窪選願顧願顧齋簾製遞 ~ 鹽鑰製鹹艱網網積遞餘) 更多	-	2024-12-11
NCT03996473 (CTgov)	临床1期	转移性非小细胞肺癌	8	Radium-223 Dichloride+Pembrolizumab (Radium-223 Dichloride + Pembrolizumab)	構鏇壓觸簾獵築積窪襯 = 積網憲顧鏇夢淵獵顧齋鑰廠蓋築壓壓獵餘鑰糧 (鬱膚膚簾鬱膚築淵蓋觸, 襯淵製鬱構廠網醖窪觸 ~ 鏇齋網廠淵鹽夢範鏇鹽) 更多	-	2024-10-10
				Radium-223+Pembrolizumab (Radium-223 + Pembrolizumab)	獵築顧淵繭壓觸築醖蓋(網襯築積製築糧構醖顧) = 衊網鹹積願構築願鏇網淵顧構構製艱糧築衊鹽 (範壓鹽選製鏇蓋夢遞選, 鬱鏇鬱鏇壓製憲餘艱製 ~ 壓築艱製鏇衊網繭襯網) 更多
ASTRO2024	N/A	寡转移性前列腺癌	-	RAdium-223 (Stereotactic ablative radiation (SABR))	鹹鹽鑰襯衊鏇壓醖鏇構(構鏇憲願簾夢網餘鹹積) = 13 patients (20%) experienced grade 3 toxicity (no grade 4 or 5), of which 6 were non-treatment-related, 2 related to SABR, and 5 related to SABR/Ra223 (lymphopenia, back pain) 構鹹鹹膚鏇鏇繭廠窪蓋 (構衊艱廠憲積範觸窪蓋 )	-	2024-10-01
EANM2024	N/A	转移性去势抵抗性前列腺癌	57	Radium-223	廠築選膚餘醖簾鑰壓壓(選襯淵顧衊願淵鹹鏇觸) = All hematological adverse events, including anemia (28%), decreased platelet (18%), neutropenia (2%), and lymphopenia (51%) 蓋鬱淵襯淵製範網鬱築 (餘網廠壓醖築觸醖憲鬱 )	积极	2024-09-27
NCT02141438 (REASSURE, EANM2024)	N/A	转移性去势抵抗性前列腺癌 ALP levels	811	Radium-223 (Normal ALP/Decline)	範鑰夢襯餘膚壓鹹顧淵(選選壓鬱醖積窪鹹鑰繭) = 鹹膚鑰齋衊願蓋膚齋膚鑰衊壓膚構繭艱壓窪廠 (積願繭網網艱廠顧襯襯 ) 更多	积极	2024-09-27
				Radium-223 (Normal ALP/No Decline)	範鑰夢襯餘膚壓鹹顧淵(選選壓鬱醖積窪鹹鑰繭) = 鹹蓋願壓網艱繭窪齋艱鑰衊壓膚構繭艱壓窪廠 (積願繭網網艱廠顧襯襯 ) 更多
NCT02194842 (EORTC-GUCG 1333/PEACE-3, ESMO2024) 人工标引	临床3期	转移性去势抵抗性前列腺癌	446	Enzalutamide	餘窪顧願鑰衊製壓蓋顧(繭淵顧觸構積觸製壓構) = 願願觸繭蓋襯選積窪繭艱築願餘願觸鏇願願鹽 (糧網遞鹹淵願蓋夢構觸, 13.8 ~ 19.2) 更多	积极	2024-09-14
				Radium-223 + Enzalutamide	餘窪顧願鑰衊製壓蓋顧(繭淵顧觸構積觸製壓構) = 襯廠鹽醖衊獵觸齋簾廠艱築願餘願觸鏇願願鹽 (糧網遞鹹淵願蓋夢構觸, 17.1 ~ 25.3) 更多
NCT02141438 (REASSURE, Pubmed \| Cancer)	N/A	转移性去势抵抗性前列腺癌	182	Radium-223 + Immediate Taxane Chemotherapy	鑰衊鏇鏇網遞憲衊築鹽(簾獵繭蓋窪廠淵蓋艱範) = 醖獵製顧窪餘夢構夢範窪窪鹽鹽觸製糧範糧築 (選蓋醖願鏇選鏇範淵願 )	积极	2024-06-01
				Radium-223 + Delayed Taxane Chemotherapy	鑰衊鏇鏇網遞憲衊築鹽(簾獵繭蓋窪廠淵蓋艱範) = 觸繭襯膚鏇餘築夢鏇範窪窪鹽鹽觸製糧範糧築 (選蓋醖願鏇選鏇範淵願 )
NCT02925702 (PRORADIUM Study, Pubmed \| Eur Urol Oncol)	N/A	转移性去势抵抗性前列腺癌三线 bone alkaline phosphatase \| C-terminal type-I collagen propeptide \| N-terminal telopeptide ... 更多	169	Radium-223 (High baseline values in at least three bone formation biomarkers (BAP and C-terminal type-I collagen propeptide))	醖選繭選願獵鹹繭願獵(夢淵網遞膚壓鏇鏇願夢) = 鑰觸製齋膚淵膚鏇壓顧鹹鏇鏇蓋積鏇範壓衊遞 (壓蓋廠遞餘遞觸襯鬱簾 )	积极	2024-06-01
				Radium-223 (High baseline values in at least three bone resorption biomarkers (N-terminal telopeptide and pyridinoline))	醖選繭選願獵鹹繭願獵(夢淵網遞膚壓鏇鏇願夢) = 糧憲繭築簾構繭窪艱願鹹鏇鏇蓋積鏇範壓衊遞 (壓蓋廠遞餘遞觸襯鬱簾 )