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更新于：2025-08-02

Lutetium (177Lu) zadavotide guraxetan

更新于：2025-08-02

概要

概要

基本信息

药物类型

多肽偶联核素、治疗用放射药物

别名

177Lu-PNT2002、177Lu-PSMA-I&T、PNT-2002

+ [1]

靶点

PSMA

作用方式

抑制剂

作用机制

PSMA抑制剂(前列腺癌特异性膜抗原抑制剂)

治疗领域

肿瘤泌尿生殖系统疾病

在研适应症

转移性前列腺恶性肿瘤转移性去势抵抗性前列腺癌腺样囊性癌+ [3]

非在研适应症-

原研机构

Scintomics GmbH

在研机构

Lantheus Holdings, Inc.Curium US Holdings LLC

POINT Biopharma, Inc.

+ [4]

非在研机构

POINT Biopharma Corp.

Weill Medical College of Cornell University

权益机构

Lantheus Holdings, Inc.

Eli Lilly & Co.

Convergent Therapeutics, Inc.

+ [5]

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C63H85ILuN11O23

InChIKeyKRNMXHUBVUCLIL-KMPGELEWSA-G

CAS号2447131-70-4

使用我们的ADC技术数据为新药研发加速。

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关联

项与 Lutetium (177Lu) zadavotide guraxetan 相关的临床试验

NCT05896371

/ Not yet recruiting临床1/2期IIT

PROstate-specific Membrane Antigen DosImetry-Guided EndoradiotherapY: a Phase 1/2 Study of Personalized PSMA Radiopharmaceutical Therapy (PRODIGY-1)

The goal of this clinical trial is to study a personalized regime of lutetium-177 (177Lu) prostate-specific membrane antigen (PSMA) radiopharmaceutical therapy (RPT) in patients with progressive and/or symptomatic, inoperable PSMA-expressing cancers of prostatic or other origins.
The main questions it aims to answer are:
* To establish a dosimetry-based, personalized regime of 177Lu-PSMA
* To report on the efficacy of personalized 177Lu-PSMA
Participants (stratified by risk factors of toxicity) will receive up to 6 cycles of a personalized activity of 177Lu-PSMA based on renal dosimetry. In the phase 1, the prescribed absorbed dose to the kidney will be escalated, to determine the regime that will be administered in the phase 2. The best response within 12 months after the first cycle will be assessed. Salvage treatment of 3 cycles may be offered to responders after re-progression.

开始日期2028-03-01

申办/合作机构

Centre Hospitalier Universitaire (CHU) de Québec-Université Laval

[+1]

NCT07090369

/ Not yet recruiting临床1期IIT

Phase Ib Trial of 177Lu-PSMA-I&T Therapy in Combination With Olaparib and Pembrolizumab in Patients With Metastatic Castration Resistant Prostate Cancer

This phase 1b trial is designed to evaluate the safety and tolerability of olaparib in combination with 177Lutetium-Prostate Specific Membrane Antigen (177 Lu-PSMA) and pembrolizumab in patients with metastatic castration resistant prostate cancer (mCRPC).

开始日期2025-11-01

申办/合作机构

Peter MacCallum Cancer Institute

NCT06361810

/ Not yet recruiting临床1/2期IIT

A Phase 1/2 Open-label Study of Pembrolizumab Combined With PNT-2002 Radioligand Therapy in Patients With Metastatic Renal Cell Carcinoma

This is a multi-center, single arm open label phase 1b/2 study of pembrolizumab in combination with 177Lu-PNT2002 (also known as 177Lu-PSMA I&T) radiopharmaceutical therapy in patients with metastatic clear cell renal cell carcinoma (RCC) who have progressed after prior treatment with anti-programmed cell death protein 1 (PD1) or PD-L1 immune-checkpoint inhibitors (ICIs). The study comprises 2 phases: an open-label Phase 1b dose escalation portion followed by a Phase 2 dose expansion portion. Investigators hypothesize that pembrolizumab in combination with 177Lu-PNT2002 in in patients with metastatic clear cell RCC at a biologically active dose will result in tolerable safety profile and it will lead to improved radiological objective responses in patients who have progressed after prior treatment with standard anti-PD1 or anti- Programmed Cell Death Ligand 1 (PDL1) immune-checkpoint inhibitor containing regimen when compared to historic controls. Patients in both phases will have prostate-specific membrane antigen (PSMA), positron emission tomography (PET) imaging with the radiotracer (F-18)-DCFPyl, to help detect any spread of the cancer.

开始日期2025-05-01

申办/合作机构

The Sidney Kimmel Comprehensive Cancer Center

[+2]

100 项与 Lutetium (177Lu) zadavotide guraxetan 相关的临床结果

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100 项与 Lutetium (177Lu) zadavotide guraxetan 相关的转化医学

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100 项与 Lutetium (177Lu) zadavotide guraxetan 相关的专利（医药）

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项与 Lutetium (177Lu) zadavotide guraxetan 相关的文献（医药）

2025-04-01·JOURNAL OF NUCLEAR MEDICINE

Preclinical Evaluation of¹⁷⁷Lu-rhPSMA-10.1, a Radiopharmaceutical for Prostate Cancer: Biodistribution and Therapeutic Efficacy

Article

作者: Foxton, Caroline ; O'Neill, Edward ; Simón, Jaime Jim ; Cornelissen, Bart ; Veggerby Grønlund, Rikke ; Stevens, Daniel ; Waldron, Bradley

¹⁷⁷Lu-rhPSMA-10.1 is a novel radiohybrid prostate-specific membrane antigen (PSMA)-targeted radiopharmaceutical therapy for prostate cancer. We conducted preclinical analyses on non-tumor-bearing BALB/c mice and on prostate cancer human xenograft mouse models (LNCAP and 22Rv1 xenografts) to evaluate its biodistribution and therapeutic efficacy. Methods: Longitudinal biodistribution of ¹⁷⁷Lu-rhPSMA-10.1 was evaluated in BALB/c mice and 22Rv1 xenografts. Tissues of interest were harvested, and radioactivity was measured 1-168 h after injection of 1 MBq of ¹⁷⁷Lu-rhPSMA-10.1 (4 per time point). Longitudinal biodistribution was compared with ¹⁷⁷Lu-PSMA-I&T (1 MBq) in BALB/c mice and at a single time point (15 h) in 22Rv1 xenografts. The therapeutic efficacy of a single administration of 15, 30, or 45 MBq of ¹⁷⁷Lu-rhPSMA-10.1 in LNCaP xenografts and 30 MBq of ¹⁷⁷Lu-rhPSMA-10.1, ¹⁷⁷Lu-PSMA-617, or ¹⁷⁷Lu-PSMA-I&T in 22Rv1 xenografts (8 per group) was evaluated. Efficacy versus vehicle was evaluated on the basis of relative tumor volume and survival up to 49 d after administration. Statistical significance was evaluated with t testing (biodistribution data), 2-way repeated-measures ANOVA (tumor volume [analyzed until 3 per group remained]), or Kaplan-Meier log-rank analyses (survival). Results: Biodistribution of ¹⁷⁷Lu-rhPSMA-10.1 in the BALB/c and 22Rv1 xenografts showed rapid clearance from blood and other normal tissues within 48 h, with the kidney showing the highest normal-organ uptake. Kidney uptake and retention were lower for ¹⁷⁷Lu-rhPSMA-10.1 than for ¹⁷⁷Lu-PSMA-I&T (6.5-fold lower at 12 h in BALB/c mice and 6.4-fold lower at 15 h in 22Rv1 xenografts; P < 0.01). High and sustained ¹⁷⁷Lu-rhPSMA-10.1 tumor uptake was observed in 22Rv1 xenografts. This uptake was 2.3-fold higher than that of ¹⁷⁷Lu-PSMA-I&T (15 h; P < 0.05). When efficacy was evaluated, ¹⁷⁷Lu-rhPSMA-10.1 significantly suppressed tumor growth versus vehicle from day 11 (P < 0.05) in LNCaP xenografts in a dose-dependent manner and from day 18 (P < 0.05) in 22Rv1 xenografts and significantly prolonged median survival versus vehicle in both models. In 22Rv1 xenografts, ¹⁷⁷Lu-rhPSMA-10.1 suppressed tumor growth versus vehicle to a greater extent than did ¹⁷⁷Lu-PSMA-I&T (significant growth inhibition from day 25 [P < 0.05]) and similarly in extent to ¹⁷⁷Lu-PSMA-617 (from day 18 [P < 0.05]). Overall, compared with ¹⁷⁷Lu-PSMA-I&T, ¹⁷⁷Lu-rhPSMA-10.1 suppressed tumor growth for longer than ¹⁷⁷Lu-PSMA-617 (inhibition from day 39 onward [P < 0.05] versus on day 49 only [P < 0.05]). Conclusion: In preclinical models, ¹⁷⁷Lu-rhPSMA-10.1 shows a favorable tumor-to-kidney uptake ratio, and significant antitumor effects, indicating it to be a promising next-generation radiopharmaceutical therapy.

2024-11-01·ANNALS OF NUCLEAR MEDICINE

Comparative post-therapeutic dosimetry between 2D planar-based and hybrid-based methods for personalized Lu-177 treatment

Article

作者: Handayani, Wuri ; Phromphao, Benchamat ; Noipinit, Nut ; Khamwan, Kitiwat ; Chantadisai, Maythinee ; Pasawang, Panya

PURPOSE:

This study aims to compare the calculated absorbed dose in target organs and tumors obtained using the different imaging protocols and the calculation methodologies implemented by HERMES HybridViewer dosimetry software for ¹⁷⁷Lu-PSMA I&T and ¹⁷⁷Lu-DOTATATE therapy.

METHODS:

Multiple time-point whole-body planar images and one SPECT/CT image were acquired from 18 patients including ¹⁷⁷Lu-PSMA I&T (13 patients) and ¹⁷⁷Lu-DOTATATE treatment (5 patients) after administration of 3.80-8.58 GBq injected activity. The regions of interest were drawn in the whole body, kidneys, liver, urinary bladder, salivary glands, and tumors to determine the time-integrated activity (TIA) in source organs. Absorbed doses in target organs were calculated according to the Medical Internal Radiation Dose (MIRD) scheme using the HERMES HybridViewer dosimetry integrated with OLINDA/EXM V.2.1 that utilizes the non-uniform rational B-splines (NURBS) for computational digital phantom.

RESULTS:

The planar-based dosimetry showed a higher dose per injected activity compared to the hybrid-based dosimetry, primarily due to organ overlap. The highest difference in absorbed dose between the imaging scenarios was observed in the spleen with a variation of up to 51.6%, while the difference for other target organs and tumors was less than 40%.

CONCLUSION:

The dosimetry calculation derived from the 2D planar-based method consistently demonstrates a significantly higher absorbed dose in organs and tumors compared with the hybrid-based method. However, the hybrid method outperforms the planar method in terms of tumor visualization and overlap-free organ delineation.

2024-09-01·Journal of Nuclear Medicine Technology

First-Strike Rapid Predictive Dosimetry and Dose Response for¹⁷⁷Lu-PSMA Therapy in Metastatic Castration-Resistant Prostate Cancer

Article

作者: Falzone, Nadia ; Pearson, Michael ; Kao, Yung Hsiang ; Sivaratnam, Dinesh

We devised and clinically validated a schema of rapid personalized predictive dosimetry for ¹⁷⁷Lu-PSMA-I&T in metastatic castration-resistant prostate cancer. It supersedes traditional empiric prescription by providing clinically meaningful predicted absorbed doses for first-strike optimization. Methods: Prostate-specific membrane antigen PET was conceptualized as a simulation study that captures the complex dosimetric interplay between tumor, marrow, and kidneys at a single time point. Radiation principles of fractionation, heterogeneity, normal-organ constraints (marrow, kidney), absorbed dose, and dose rate were introduced. We created a predictive calculator in the form of a free, open-source, and user-friendly spreadsheet that can be completed within minutes. Our schema achieves speed and accuracy by sampling tissue radioconcentrations (kBq/cm³) to be analyzed in conjunction with clinical input from the user that reflect dosimetric preconditions. The marrow-absorbed dose constraint was 0.217 Gy (dose rate, ≤0.0147 Gy/h) per fraction with an interfraction interval of at least 6 wk. Results: Our first 10 patients were analyzed. The first-strike mean tumor-absorbed dose threshold for any prostate-specific antigen (PSA) response was more than 10 Gy (dose rate, >0.1 Gy/h). The metastasis with the lowest first-strike tumor-absorbed dose correlated the best with the percentage decrease of PSA; its threshold to achieve hypothetical zero PSA was 20 Gy or more. Each patient's PSA doubling time can be used to personalize their unique absorbed dose-response threshold. The predicted mean first-strike prescription constrained by marrow-absorbed dose rate per fraction was 11.0 ± 4.0 GBq. Highly favorable conditions (tumor sink effect) were dosimetrically expressed as the combination of tumor-to-normal-organ ratios of more than 150 for marrow and more than 4 for kidney. Our schema obviates the traditional role of the SUV as a predictive parameter. Conclusion: Our rapid schema is feasible to implement in any busy real-world theranostics unit and exceeds today's best practice standards. Our dosimetric thresholds and predictive parameters can radiobiologically rationalize each patient's first-strike prescription down to a single becquerel. Favorable tumor-to-normal-organ ratios can be prospectively exploited by predictive dosimetry to optimize the first-strike prescription. The scientific framework of our schema may be applied to other systemic radionuclide therapies.

132

项与 Lutetium (177Lu) zadavotide guraxetan 相关的新闻（医药）

2025-07-11

·精准药物

只有【1个员工】的Biotech，A轮融了5.4亿

PREFACE前言2023年之前，核药还只是诺华和拜耳两家MNC重点谋划的方向，但在随后的两年，诸多MNC开始通过一系列合作、并购、投资强势入局，推动核药赛道热度不断飙升。随着竞争不断加剧，差异化的创新也成为了脱颖而出的关键，如在靶点方面，除了PSMA和SSTR等成熟靶点外，FAP、HER2、CD46、B7-H3等新兴靶点逐步成为关注焦点。近日，一家核药初创biotech公司Actithera宣布完成了7550万美元（约为5.4亿元）的A轮融资，为核药赛道再添了一把热火。从差异化层面来看，Actithera主要有两大创新，一是在靶点上，选择了成纤维细胞激活蛋白FAP，但目前靶向FAP的核药开发也存在肿瘤滞留时间不够理想，从而影响疗效的问题，因此，Actithera的第二个创新点便是希望通过引入共价结合的概念，解决这一问题。另外，令小编震惊的是，目前Actithera只有首席执行官Andreas Goutopoulos一名员工，这无疑也为Actithera的创新故事增添了一层传奇的色彩。01共价核药加入战场Andreas Goutopoulos在创立Actithera之前，曾在德国默克旗下的EMD Serono担任了约17年的药物化学家。大约在2018年的时候，Goutopoulos加入了德国默克的企业风投部门M Ventures，担任驻场企业家（EIR）。这一工作角色，也让Goutopoulos萌生了创业的想法——想在“激动人心的新领域”创办一家biotech。创业方向来得很快。2018年，Endocyte启动了Pluvicto治疗转移性去势抵抗性前列腺癌的临床3期VISION研究，并且公布的初步临床数据也非常亮眼，这引起了Goutopoulos的关注。随着Pluvicto在前列腺癌适应症上不断取得突破，以及Goutopoulos对核药领域的研究不断深入，2021年，在M Ventures和Arkin Bio Ventures II的支持下，Actithera正式成立。Actithera的创新方向也来源于Goutopoulos对于Pluvicto的深入研究——一方面，Pluvicto在血液循环中的半衰期非常短，这对于避免毒性至关重要；另一方面，它在肿瘤中的滞留时间却可以长达一周甚至更久，大致匹配了177Lu的半衰期（6.65天），这是最理想的状态。但事实证明，想在其他靶点上复制Pluvicto的PK特征非常困难，这也成为了Actithera创立之初想解决的关键科学问题之一。循着这一思路，Goutopoulos认为利用共价化学有望解决这一难题。共价核药示意从机制上来看，通过放射性配体共价、不可逆地结合肿瘤特异性靶标，可以提高核素在肿瘤组织的摄取并延长其滞留时间，同时确保其在肿瘤组织的特异性结合。目前Actithera已有一款靶向FAP的共价核药处于临床前阶段，在A轮融资的支持下，Actithera将尽快启动临床研究。在核素的选择方面，由于供应的问题，目前Actithera的首选是Lu-177，但Goutopoulos也表示，随着供应的改善，未来也将开发Ac-225版本的FAP共价核药。02靶向FAP的核药到了爆发前夕Actithera想通过“共价”的方式，解决靶向FAP的核药在肿瘤组织的有效滞留时间较短的问题，这也从另一个角度证明了FAP靶点的潜力巨大。从靶点的特性来看，FAP在肿瘤相关成纤维细胞CAF中过表达，后者是肿瘤基质的重要组成部分，存在于包括胰腺癌、结肠癌和乳腺癌等在内的90%以上的上皮性肿瘤中，因此FAP可作为理想的靶标来杀伤CAF而抑制肿瘤细胞的生长。此外，还有证据表明FAP在部分肿瘤细胞上表达，有望对肿瘤产生双重打击。因此在核药领域，FAP已经成为了非常热门的靶点之一。核药龙头诺华已经对FAP进行了一系列布局。通过合作与收购，目前诺华的AAA614（177Lu-FAP-2286）已经处于治疗实体瘤的2期临床，用于诊断的68Ga-FAP-2286也在同步开发中。核药新入局者礼来也通过收购进行了相应的布局。2023年10月，礼来以14亿美元收购核药企业POINT Biopharma，这笔交易最核心的是已经处于临床3期的PNT2002和PNT2003，但同时POINT的管线中也有两款靶向FAP的治疗性核药，分别是177Lu-PNT6555（临床1期）和225AC-PNT6555（临床前），配套的诊断用核药也在开发者。除两家MNC之外，SOFIE的两款诊断用FAP核药处于临床2期，全球权益已经转让给了GE HealthCare；Lantheus也有一款诊断用FAP核药64Cu-LNTH-1363S处于临床1/2期；Ratio Therapeutics有一款治疗用FAP-Rx核药处于临床1期，拟用于治疗软组织肉瘤。在国内药企方面，东诚药业控股子公司烟台蓝纳成生物基于诊疗一体化思路，开发了靶向FAP的诊断用药物氟[18F]纤抑素注射液，于2022年末在国内获批临床，以及靶向FAP的治疗用药物177Lu-LNC1004，已经在2023年分别取得了美国、新加坡和中国的临床批件，并在近期获得了FDA授予的快速通道资格；法伯新天也有一款靶向FAP的诊断用药物锝[99mTc]-H7ND处于临床阶段；另外，恒瑞医药靶向FAP的RDC药物，在2025年初获批临床，用于治疗实体瘤。SUMMARY小结放眼整个赛道，FAP作为覆盖广泛实体瘤、蕴含“双重打击”潜力的明星靶点，其初步价值已被诺华、礼来等巨头重金押注以及众多国内外药企的积极布局所验证，正处于爆发性增长的前夜。Actithera选择在此刻加入FAP的竞争，以差异化技术寻求破局，时机与策略都极具看点。随着资本持续涌入、巨头深度布局、技术迭代加速，核药领域已驶入发展的快车道。可以预见，未来几年将是核药创新成果密集涌现、临床应用场景极大拓展的关键时期。核药革命的浪潮，正奔涌向前。声明：发表/转载本文仅仅是出于传播信息的需要，并不意味着代表本公众号观点或证实其内容的真实性。据此内容作出的任何判断，后果自负。若有侵权，告知必删！长按关注本公众号粉丝群/投稿/授权/广告等请联系公众号助手觉得本文好看，请点这里↓

并购临床3期

2025-06-23

·同写意

核药浪潮汹涌而至，BMS、诺华重金押注

同写意年度巨献！！大会特设“核药全产业链开发”分会，7月25-26日，邀您相聚金鸡湖畔，与5000人一起为中国医药创新“同写意”！近日，BMS子公司RayzeBio豪掷13.5亿美元引进前列腺癌核药OncoACP3，诺华同步在华启动SSTR2靶向药Lutathera治疗晚期胃肠胰神经内分泌瘤的III期临床。两大巨头重金加码与关键进展齐发，标志着全球核药行业进入加速发展的新阶段，全球核药浪潮来袭。TONACEA01核药的全球浪潮全球医疗产业正迎来治疗性核药的爆发性增长，这一领域凭借其精准靶向和诊疗一体化的独特优势，重塑肿瘤等重大疾病的治疗范式。据Precedence Research数据，2024年全球放射性药物市场规模达67.4亿美元，并以8.2%的复合年增长率加速扩张，预计2034年将突破144.4亿美元。这一增长主要源于放射性核素偶联药物（RDC）的技术突破与商业化落地。RDC的结构与抗体偶联药物（ADC）类似，但作用机理截然不同，其通过靶向配体引导放射性核素（如镥-177、锕-225）精准定位病灶，实“体内精准放疗”，而非ADC的细胞毒性杀伤。2024年-2034年放射性药物市场规模/图片来源：Precedence Research其中，诺华的两款RDC药物Pluvicto和Lutathera成为行业标杆。2024年，靶向PSMA的前列腺癌疗法Pluvicto销售额达13.92亿美元，同比增长42%，成为核药领域首个“重磅炸弹”。为了巩固Pluvicto地位，诺华正在进行Pluvicto的适应证拓展。2025年3月，Pluvicto获批用于更早期的前列腺癌治疗的新适应证，根据诺华在2025 JPM大会上预测，其销售峰值预计超50亿美元；而另一款靶向SSTR的神经内分泌肿瘤药物Lutathera在2024年收入7.24亿美元，同比增长20%。两者合计贡献21.16亿美元，验证了治疗性核药的商业潜力。另外，诊断性核药增长势头同样喜人，2024年两款PSMA-PET显影剂Plarify和Illuccix销售额合计16亿美元，同比增长33%，美国医保支付改革将进一步推动诊断核药的市场扩容，据Lantheus预测，2025年PSMA PET诊断规模有望超25亿美元，预计到2030年其市场规模有望超过35亿美元。2025年-2030年美国PSMA PET诊断市场预测/图片来源：LantheusTONACEA02MNC争相入局随着诺华旗下Pluvicto和Lutathera的商业化成功，核药赛道已成为MNC战略布局的新焦点。2024年至2025年初，礼来、BMS、阿斯利康等巨头通过高溢价收购和战略合作加速布局。礼来成为最活跃的投资者，2023年10月以14亿美元收购Point Biopharma，获得其PSMA靶向疗法PNT2002；2024年先后与Aktis Oncology、Radionetics Oncology达成合作；2025年2月又与AdvanCell扩大合作，整合后者领先的Pb212生产技术，共同开发靶向α核素疗法。BMS以41亿美元收购RayzeBio，创下核药领域最高交易纪录，核心资产为225Ac靶向药物RYZ101，意图挑战诺华的Lutathera。2025年6月10日，BMS全资子公司RayzeBio又以13.5亿美元的潜在总金额引进一款临床在研前列腺癌治疗和诊断药物OncoACP3，其野心可见一斑。主要MNC布局核药情况汇总/图片来源：平安证券研报阿斯利康从试水转向全面投入，2020年与Fusion Pharmaceuticals合作后，2024年3月以24亿美元直接收购该公司，获得其FastClear linker技术平台及4款在研核药，包括靶向PSMA的225Ac疗法FPI2265，同年还投资CDMO企业Nucleus RadioPharma完善产业链。诺华在巩固先发优势的同时，2024年5月以17.5亿美元收购礼来曾投资的Mariana Oncology，加码放射性配体疗法（RLT）管线，并加速推进225AcPSMA617等新一代药物。近些年，拜耳也持续布局核药领域。2021年，拜耳收购Noria Therapeutics和PSMA Therapeutics，扩展了基于Ac-225的核药产品研发管线。2023年5月，拜耳与Bicycle Therapeutics达成战略合作，开发RDC。截至2024年末，其研发管线中已拥有7款处于临床前研究阶段、2个进入早期临床开发的RDC项目。TONACEA03国内商业化征程已然开启近年来，国内核药产业同样迎来实质性突破，从研发阶段迈入商业化价值兑现期。2020年2025年初，国内共获批5种新型核药，其中远大医药的钇[90Y]微球注射液表现最为亮眼，2024年实现收入近5亿港元，同比增长140%。后续伴随着2025年商保推出及落地，钇[90Y]微球注射液有望放量。此外，2025年成为国内核药商业化进程的关键节点。其中，安迪科的氟[18F]化钠已于5月底获NMPA批准上市。同时，诺华围绕PSMA靶点的前列腺癌治疗药镓[68Ga]戈泽肽及配套诊断药镥[177Lu]特昔维匹肽于2024年11月获CDE优先审评，2025年有望双双获批。值得一提的是，2025年6月10日，诺华还在中国启动了SSTR2靶向核药Lutathera在1级和2级晚期胃肠胰神经内分泌瘤（GEP-NET）患者III期临床研究。与此同时，国内企业的研发与管线布局同样进入收获期。远大医药核药抗肿瘤诊疗板块目前已储备12款创新产品，3款RDC产品处于III期临床阶段，其中前列腺癌诊断药物TLX591-CDx计划2025年递交上市申请。远大医药还提出“自研核药出海”战略，目标是自2025年起每年向FDA递交一个产品申请，2028年-2029年首个产品完成临床试验并向FDA递交上市申请。远大医药介入治疗和RDC管线/图片来源：远大医药2024年财报东诚药业则聚焦诊断核药商业化，旗下产品氟[18F]化钠已于2025年5月底获批上市，锝[99mTc]-GSA等产品有望年内提交新药申请；治疗性核药中，其FAP靶点药物177Lu-LNC1004获FDA快速通道资格，全球进度领先。结语：随着国内外企业加速布局与商业化破局，核药必将引爆下一个百亿美元级的蓝海市场。精准“核爆”，未来已来！

并购抗体药物偶联物临床3期放射疗法

2025-06-11

·BioSpace

BMS Expands Radiopharma Presence With $1.35B Biobucks Deal for Philochem

iStock, hapabapa Instead of homing in on PSMA—currently the most validated target in prostate cancer—BMS and Philochem will instead collaborate on an early-stage molecule that binds to a novel marker called ACP3. Bristol Myers Squibb is trying to unlock an alternative pathway to treating prostate cancer. The company’s radiopharma-focused subsidiary RayzeBio has fronted $350 million to partner with Italian-Swiss biotech Philochem to advance an early-stage small-molecule radiotherapeutic targeting a novel biomarker. BMS is also promising up to $1.35 billion in development, regulatory and commercial milestones, plus mid-single to low-double-digit royalties on global net sales. BMS and Philochem expect to close the transaction in the third quarter, pending customary clearances and approvals. Philogen, Philochem’s parent company, surged 20% on Wednesday morning. The star of Wednesday’s agreement is OncoACP3, a small-molecule radiotracer that targets a biomarker called ACP3. According to Philochem, ACP3 is highly expressed in prostate cancer—but not in healthy tissue—and at levels that match or exceed that of PSMA, which is currently the prevailing target of choice for prostate cancer therapies. “A side-by-side comparison between ACP3 and PSMA . . . has shown that ACP3 is more abundantly expressed in prostate cancer than PSMA,” the biotech wrote on its website. OncoACP3 is a small-molecule ligand that has high affinity for the ACP3 protein. Notably, it can carry both Lutetium-177 and Actinium-225—both currently the most common payloads for radiopharmaceuticals. In a statement on Wednesday, RayzeBio president Ben Hickey said that by potentially opening an alternative pathway to PSMA, the Philochem partnership “provides a differentiated entry” for BMS “into the prostate cancer arena.” The decision to zero in on a novel prostate cancer target could also help BMS distinguish itself in a radiopharma field that is becoming increasingly crowded . Currently leading the pack is Novartis, which owns two FDA-approved therapies: Lutathera, indicated for gastroenteropancreatic neuroendocrine tumors, and Pluvicto, which targets PSMA and is approved for prostate cancer. Another pharma trying to catch Novartis is AstraZeneca, which entered the ring in March 2024 with the $2.4 billion acquisition of Fusion Pharmaceuticals, which gave the pharma its lead radiopharma asset FPI-2265, an actinium-based radioconjugate that is being developed for prostate cancer—and targets PSMA. Also in the running is Eli Lilly, which spent $1.4 billion to buy Point Biopharma in October 2023 and $1.1 billion for Aktis Oncology in May 2024. Anchoring its radiopharma pipeline is PNT2002, another PSMA-targeting candidate for prostate cancer.

并购上市批准引进/卖出

100 项与 Lutetium (177Lu) zadavotide guraxetan 相关的药物交易

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研发状态

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
转移性前列腺恶性肿瘤	临床3期	美国	Curium US Holdings LLC	2022-02-14
转移性前列腺恶性肿瘤	临床3期	法国	Curium US Holdings LLC	2022-02-14
转移性前列腺恶性肿瘤	临床3期	意大利	Curium US Holdings LLC	2022-02-14
转移性前列腺恶性肿瘤	临床3期	西班牙	Curium US Holdings LLC	2022-02-14
去势抵抗性前列腺癌	临床3期	美国	POINT Biopharma Corp.	2021-02-25
转移性去势抵抗性前列腺癌	临床3期	美国	Lantheus Holdings, Inc.	2021-02-25
转移性去势抵抗性前列腺癌	临床3期	美国	POINT Biopharma Global, Inc.	2021-02-25
转移性去势抵抗性前列腺癌	临床3期	加拿大	POINT Biopharma, Inc.	2021-02-25
转移性去势抵抗性前列腺癌	临床3期	法国	POINT Biopharma, Inc.	2021-02-25
转移性去势抵抗性前列腺癌	临床3期	荷兰	POINT Biopharma, Inc.	2021-02-25

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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


NCT04886986 (ASCO_GU2025) 人工标引	临床1期	晚期前列腺癌	18	225Ac-J591 + PNT2002	願簾齋構膚醖衊糧鬱壓(製網選壓鑰齋膚艱顧淵) = 35 KGBq/kg 艱選鹽蓋壓蓋積積壓願 (蓋鹽鹽醖艱淵鑰廠膚積 ) 更多	积极	2025-02-13
NCT04647526 (SPLASH, Pubmed \| Front Oncol) 人工标引	临床3期	转移性去势抵抗性前列腺癌	27	[177Lu]Lu-PNT2002 6.8 GBq/cycle	積製醖獵遞夢獵蓋鬱鏇(鏇襯淵壓艱繭顧窪蓋窪) = 艱鹹簾獵選積鏇製繭襯繭構遞範廠觸顧餘顧遞 (鬱艱築積願鬱選製廠淵, 9.2 ~ 19.1) 更多	积极	2025-01-07
NCT05204927 (PipelineReview) 人工标引	临床3期	转移性去势抵抗性前列腺癌	-	177Lu-PSMA-I&T	夢範淵衊選觸鑰簾淵網(構築鹽壓鹹憲願選選鹽) = 齋觸夢製窪築醖願範襯蓋淵壓窪選鏇網鹹襯艱 (願衊窪淵遞淵獵憲壓淵 )	积极	2024-11-13
NCT05204927 (PipelineReview) 人工标引	临床3期	转移性去势抵抗性前列腺癌	-	Hormone therapy	夢範淵衊選觸鑰簾淵網(構築鹽壓鹹憲願選選鹽) = 觸襯壓糧憲夢淵衊顧繭蓋淵壓窪選鏇網鹹襯艱 (願衊窪淵遞淵獵憲壓淵 )	积极	2024-11-13
VISION trial (EANM2024)	N/A	转移性去势抵抗性前列腺癌	112	7.4 GBq [177Lu]Lu-PSMA-I&T	憲艱齋鹽糧餘範淵憲壓(獵壓願糧餘獵網膚齋窪) = CTCAE grade 3 anaemia was seen in four patients 襯獵齋網淵醖築憲鹽廠 (艱選艱醖夢壓膚糧鬱簾 ) 更多	积极	2024-09-27
NCT04647526 (SPLASH, ESMO2024) 人工标引	临床3期	转移性去势抵抗性前列腺癌 FOLH1 Positive	412	177Lu-PNT2002	蓋衊衊廠鬱壓夢製網膚(範選願網積製製簾鏇鹽) = 糧築糧憲積膚襯膚獵齋餘簾餘憲齋鏇夢鹹獵膚 (衊淵鬱築遞壓範顧膚觸, 7.4 ~ 10.0) 更多	积极	2024-09-15
NCT04647526 (SPLASH, ESMO2024) 人工标引	临床3期	转移性去势抵抗性前列腺癌 FOLH1 Positive	412	Alternate ARPI	蓋衊衊廠鬱壓夢製網膚(範選願網積製製簾鏇鹽) = 獵簾壓醖醖觸鬱夢製夢餘簾餘憲齋鏇夢鹹獵膚 (衊淵鬱築遞壓範顧膚觸, 4.7 ~ 7.9) 更多	积极	2024-09-15
SNMMI2024	N/A	-	-	[177Lu]Lu-PSMA I&T	願蓋鑰糧鬱膚醖選獵艱(網積窪簾淵糧築網鬱觸) = No CTC grade ≥III occurred after RLT 醖鬱積鏇糧築餘觸觸壓 (願艱鏇襯遞簾繭鑰廠艱 ) 更多	-	2024-06-09
NCT04647526 (SPLASH, Biospace) 人工标引	临床3期	去势抵抗性前列腺癌	-	177Lu-PNT2002	淵獵製蓋繭膚壓鹽製範(鹹糧繭艱壓夢願蓋鹽蓋) = 繭觸鏇簾鹹繭選願獵鬱鹹衊廠願網窪獵艱顧糧 (鑰遞鹹憲獵壓廠觸憲築 ) 更多	积极	2023-12-18
NCT04647526 (SPLASH, Biospace) 人工标引	临床3期	去势抵抗性前列腺癌	-	ARPI	淵獵製蓋繭膚壓鹽製範(鹹糧繭艱壓夢願蓋鹽蓋) = 淵積艱醖淵觸窪簾鑰獵鹹衊廠願網窪獵艱顧糧 (鑰遞鹹憲獵壓廠觸憲築 )	积极	2023-12-18
NCT04886986 (ASCO 12023 \| ASCO 22023) 人工标引	临床1/2期	前列腺癌	18	225Ac-J591+PNT2002	繭製獵網築遞齋觸鏇築(選餘夢選蓋積積鹽顧觸) = 2 of 6 pts with DLT at 40 KBq/Kg (Gr 2 or 3 thrombocytopenia delaying cycle 2 by >3 wk); no DLT observed in other cohorts. 簾艱衊鹽網糧膚窪觸簾 (膚鏇選簾醖蓋膚廠鹽築 ) 更多	积极	2023-05-31
NCT05496959 (LUNAR, Pubmed) 人工标引	临床2期	激素依赖性前列腺癌	100	177 Lu-PNT2002+SBRT	鹽遞餘觸顧膚網顧艱夢(鏇網鹽構遞簾醖鑰鑰淵) = The addition of 177 Lu-PNT2002 to metastasis-directed therapy alone may potentially further forestall disease progression. 廠廠餘壓鏇繭築簾夢襯 (選範壓簾簾積襯淵遞製 )	积极	2023-03-02
NCT05496959 (LUNAR, Pubmed) 人工标引	临床2期	激素依赖性前列腺癌	100	SBRT		积极	2023-03-02
NCT04647526 (SPLASH, ESMO2022 \| Corporate Publications) 人工标引	临床3期	转移性去势抵抗性前列腺癌	27	177Lu-PNT2002	繭鹹襯顧壓襯繭鏇鹹壓(齋遞襯襯鏇繭膚齋網製) = 壓夢鹹製糧選齋簾鏇蓋製衊膚鹹壓廠顧網選窪 (鹽艱製遞糧築鏇觸網顧 ) 更多	积极	2022-09-10