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更新于：2026-06-06

Lutetium (177Lu) zadavotide guraxetan

更新于：2026-06-06

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PSMA阳性去势抵抗性前列腺癌+ [3]

非在研适应症

腺样囊性癌

原研机构

Scintomics GmbH

在研机构

Curium US Holdings LLC

Lantheus Holdings, Inc.

Curium Holding France SASU

+ [4]

非在研机构

POINT Biopharma, Inc.POINT Biopharma Corp.

Progenics Pharmaceuticals, Inc.

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)临床申请批准

特殊审评快速通道 (美国)

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结构/序列

使用我们的ADC技术数据为新药研发加速。

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查看完整样例数据

Sequence Code 3937

来源: *****

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

/ Withdrawn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2025-10-01

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）

2026-02-01·NUCLEAR MEDICINE COMMUNICATIONS

Concordance between single-time-point and multiple-time-point dosimetry in 177Lu-PSMA-I&T therapy for metastatic castration-resistant prostate cancer

Article

作者: Zuluaga, Clarena ; Pulido, Edwin ; Barbosa, Nathaly ; Granados, Carlos

Purpose:

To quantify concordance between single-time-point (STP) and multiple-time-point (MTP) dosimetry for organs-at-risk (OARs) and lesions in 177 Lu-PSMA-I&T.

Methods:

Thirteen men with metastatic castration-resistant prostate cancer underwent quantitative SPECT/CT at ~20, ~48, and ~120 h posttherapy. Lesions <3.0 cc were excluded. Time-activity curves (TACs) were fit with automatic model-order selection (parameters ≤ data points); accepted fits required R2 > 0.90. STP activity–time integrals were estimated with the Hänscheid formalism. Agreement metrics included paired median differences, Lin’s concordance, and Bland–Altman bias/limits of agreement.

Results:

For OARs, STP at ~48 h matched MTP with minimal bias (parotids Δ = 0.00 Gy/GBq, P = 0.475; kidneys Δ = 0.02, P = 0.157). Lesion concordance improved with later imaging (STP2–STP3), whereas ~20 h STP underestimated lesion dose coefficients (all lesions Δ = +0.36 Gy/GBq; +57.4%). TAC modeling favored mono-exponential kinetics in most lesions (83%) and kidneys, with mixed behavior in parotids.

Conclusion:

A single quantitative scan at ~48 h provides OAR dosimetry concordant with MTP, while lesion estimates are best captured at ~48–120 h. Early STP imaging (~20 h) should not be used alone for lesions. Findings support a pragmatic, concordance-oriented dosimetry workflow for routine 177 Lu-PSMA-I&T care.

2025-11-01·LANCET ONCOLOGY

Lutetium-177 [177Lu]Lu-PSMA-I&T plus radium-223 in patients with metastatic castration-resistant prostate cancer (AlphaBet): an interim analysis of the investigator-initiated, single-centre, single-arm, phase 1/2 trial

Article

作者: MacFarlane, Lisa ; Buteau, James P ; Au, Lewis ; Cardin, Anthony ; Hamilton, Anthony J ; Garcia, Quinn ; Hofman, Michael S ; Haskali, Mohammad B ; Emmerson, Brittany ; Saghebi, Javad ; Alipour, Ramin ; Parker, Belinda S ; Tran, Ben ; Chin, Kwang Y ; Kong, Grace ; Jackson, Price A ; Kostos, Louise ; Murphy, Declan G ; Ravi Kumar, Aravind S ; Kashyap, Raghava K ; Xie, Jing ; Furic, Luc ; Azad, Arun A ; Wang, Yang ; Chan, Joanna ; Akhurst, Tim

BACKGROUND:

Lutetium-177 [¹⁷⁷Lu]Lu-PSMA-I&T (¹⁷⁷Lu-PSMA-I&T) and the bone-seeking α-emitter radium-223 (²²³Ra) are established life-extending therapies for patients with metastatic castration-resistant prostate cancer; however, resistance and progression are inevitable. We aimed to evaluate the safety and preliminary antitumour activity of ¹⁷⁷Lu-PSMA-I&T combined with ²²³Ra in this patient group.

METHODS:

We conducted an investigator-initiated, single-centre, single-arm, phase 1/2 trial (AlphaBet) at the Peter MacCallum Cancer Centre in Melbourne, Australia. Adults (aged ≥18 years) with a diagnosis of progressive, metastatic castration-resistant prostate cancer, an Eastern Cooperative Oncology Group performance status score of 0-2, at least two visible bone metastases not treated with radiotherapy, previous exposure to an androgen receptor pathway inhibitor, prostate-specific membrane antigen (PSMA)-positive disease (defined by maximum standardised uptake value ≥20 at a site of disease), and no discordant sites (ie, avid on 2-[¹⁸F]fluoro-2-deoxy-D-glucose-PET-CT with minimal PSMA expression and no uptake on bone scintigraphy) were eligible for inclusion. Phase 1 dose-escalation assessed two dose levels of ²²³Ra (27·5 kBq/kg and 55·0 kBq/kg) combined with 7·4 GBq ¹⁷⁷Lu-PSMA-I&T, administered intravenously every 6 weeks for up to six cycles. Phase 2 dose expansion continued with the recommended phase 2 dose. Co-primary endpoints were the maximum tolerated or administered dose and the recommended phase 2 dose (phase 1), and the PSA response rate (phase 2), analysed in all patients treated at the maximum tolerated or administered dose in either phase. Safety was assessed in all patients who received at least one dose of either protocol treatment in phase 1 or 2. Herein, we report the results of an interim analysis, which was added to the protocol following an amendment on May 30, 2024. This trial is registered at ClinicalTrials.gov (NCT05383079) and follow-up is ongoing.

FINDINGS:

Between Nov 3, 2022, and Nov 5, 2024, 37 patients were enrolled, of whom 36 (97%; median age 72·5 years [IQR 67·0-78·0]) were included in the safety analysis and 33 (89%) were included in the preliminary activity analysis. No dose-limiting toxicities were observed. The recommended phase 2 dose of ²²³Ra was 55·0 KBq/kg combined with 7·4 GBq ¹⁷⁷Lu-PSMA-I&T, administered every 6 weeks. With a median follow-up of 13·3 months (IQR 8·7-17·1), 11 (31%) patients completed all six cycles of both treatments. 18 (50%) patients discontinued treatment early, primarily due to unequivocal disease progression (11 [61%]) or adverse events (three [17%]). A reduction in PSA of at least 50% was observed in 18 (55%; 95% CI 36-72) patients. Grade 3 or higher treatment-related adverse events occurred in five (14%) of 36 patients, including anaemia (four [11%]) and neutropenia (three [8%]), with no treatment-related deaths. Non-clinically significant grade 3 lymphopenia occurred in ten (28%) patients.

INTERPRETATION:

The combination of ¹⁷⁷Lu-PSMA-I&T and ²²³Ra is safe and feasible in patients with metastatic castration-resistant prostate cancer and bone metastases. These findings warrant further evaluation of combined α-emitting and β-emitting approaches.

FUNDING:

Prostate Cancer Foundation, Bayer, and National Health and Medical Research Council.

2025-11-01·JOURNAL OF NUCLEAR MEDICINE

Preclinical Evaluation of [ ²¹² Pb]Pb-ADVC001: A Prostate-Specific Membrane Antigen–Targeted α-Therapy for Prostate Cancer

Article

作者: Horsfall, Aimee ; Kryza, Thomas ; Hammond, Edward ; Li, Kwong Ching ; Liu, Feifei ; Fletcher, Nicholas ; Shakti, Stelle ; Soderholm, Amelia T ; Prior, Amber ; Koehbach, Johannes ; Monterosso, Melissa E ; Kuan, Kevin ; Sydes, Abby ; Rose, Stephen ; Tieu, William ; Akhter, Dewan ; Kim, Chanwoo ; Thurecht, Kristofer ; Puttick, Simon ; Kumar, Saawan ; Boucher, Didier ; Li, Gary ; Karmann, Anna

Prostate-specific membrane antigen (PSMA)-directed radiopharmaceutical therapies continue to improve treatment outcomes in patients with metastatic castration-resistant prostate cancer. Here, we report the in vitro and in vivo characterization of a PSMA-targeted therapy (ADVC001) specifically designed for targeted α-therapy with ²¹²Pb. Methods: The binding affinity to PSMA was determined by PSMA enzymatic assays and by radioligand binding assays using PSMA-high prostate cancer (PC) cells. In vitro cytotoxicity against PC cell lines with high and medium PSMA expression was evaluated using clonogenic, metabolic, and imaging-based cytotoxic assays. Pharmacokinetics and biodistribution were assessed using PSMA-high subcutaneous tumor xenografts. In vivo single-dose and multidose efficacy was assessed in subcutaneous PC xenograft models expressing various levels of PSMA. Results: A high binding affinity to PSMA was observed for ADVC001 with nanomolar inhibitory concentration of 50% values. In cellular assays, [²¹²Pb]Pb-ADVC001 (²¹²Pb-ADVC001 hereafter for simplicity) exhibited specific cytotoxic activity against PSMA-expressing cells with nanomolar effective concentration of 50% values. In vivo biodistribution of ²¹²Pb-ADVC001 in the PC3-PIP xenograft model revealed rapid and persistent tumor uptake, fast renal clearance, and low retention in normal tissues. Single-dose efficacy studies of ²¹²Pb-ADVC001 (0.46 MBq) showed improved survival compared with [¹⁷⁷Lu]Lu-PSMA-I&T (¹⁷⁷Lu-PSMA-I&T hereafter for simplicity) (20 MBq) treatment. In a multidose experiment, 2 doses of ²¹²Pb-ADVC001 (0.5 MBq) significantly increased median survival (86 d vs. 45.5 d, P < 0.05) compared with 2 doses of ¹⁷⁷Lu-PSMA-I&T (15 MBq). Treatment with ²¹²Pb-ADVC001 (0.5 MBq) after initial ¹⁷⁷Lu-PSMA-I&T (15 MBq) relapse showed an enhanced survival benefit (59.5 d). In a C4-2 xenograft model with medium-level PSMA expression, single doses of 0.3, 0.8, and 1.1 MBq of ²¹²Pb-ADVC001 significantly extended median survival to 34, 57, and 62.5 d, compared with untreated cohorts (16 d). All treatments were well tolerated. Conclusion: The preclinical results support the clinical development of ²¹²Pb-ADVC001 as a targeted α-therapy for the treatment of patients with PC.

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

2026-06-01

·BioSpace

Curium Announces a Strategic Investment of Over €32 million in Saclay, France

Curium’s strategic investment of over €32 million will establish a European production line for 177 Lu-PSMA-I&T, a therapeutic agent for patients with metastatic castration-resistant prostate cancer This investment positions France at the forefront of this innovative cancer treatment technology and is part of broader industrial commitments in France, covering European demand for targeted prostate cancer therapy PARIS, June 01, 2026 (GLOBE NEWSWIRE) -- Curium, a global leader in nuclear medicine, today announced at the Choose France summit in Versailles, a major industrial investment program in France to the value of €32 million. This investment will strengthen its production capabilities for radiopharmaceuticals through the creation of a new production line, and 20 highly skilled jobs. This will supply the European market with ¹⁷⁷Lu-PSMA-I&T, a targeted radioligand therapy (RLT) for patients with metastatic castration-resistant prostate cancer (mCRPC). With this development, Curium is positioning itself as a theranostic player, combining its longstanding expertise in diagnostics with a growing therapeutic portfolio built around RLT. This commitment is part of a broader strategy to reinforce France’s position at the heart of the European nuclear medicine value chain. In France, Curium employs over 750 employees and operates 13 production sites that are serving more than 200 nuclear medicine centers every day. Saclay, France is Curium’s historic site, drawing on a world-class scientific ecosystem and notably rooted in the legacy of the French Atomic Energy Commission (CEA). By investing in the facility in Saclay, Curium is strengthening the care pathway in France and will help meet growing European demand for innovative radiopharmaceutical treatments, particularly for advanced prostate cancer through targeted ¹⁷⁷Lu-PSMA-I&T therapies. Curium has launched an ambitious investment program in France, investing more than €50 million over the past 5 years, underscoring its sustained confidence in France’s global industrial strength, and positioning the company to scale up rapidly in a market expected to grow tenfold by 2035, alongside a fast-expanding diagnostic and therapeutic pipeline. Ciril Faia, Curium International’s Chief Executive Officer, said: “France is a key production hub for Curium and accounts for more than 20% of Curium’s global revenue Nuclear medicine, and radioligand therapy in particular, is set to become an essential component of the modern therapeutic arsenal against cancer by providing innovative and highly targeted solutions for patients with cancer.”. Isabelle Rouzou, SVP Quality and Operations, Curium International, said: “France was chosen for this strategic investment because of the quality of its scientific, industrial, and hospital ecosystem, as well as its historic expertise in the field of nuclear medicine, making it a leading location for the development of radiopharmaceuticals. This investment creates new opportunities for highly skilled workers and critically, will help increase access to the radioligand therapy for patients with cancer.” About Nuclear Medicine Nuclear medicine is undergoing a profound transformation in healthcare, evolving from a primarily diagnostic role to a targeted treatment - radioligand therapy (RLT) represents one of the major innovations driving this transformation. It combines a molecular vector capable of specifically targeting tumor cells with a radioactive isotope, enabling treatment to be delivered directly to the core of the tumor while minimizing effects on healthy tissue. The growth prospects for these therapies are considerable. In France, the number of patients eligible for RLT could increase more than tenfold by 2035, reflecting a structural evolution in cancer care. About Curium Curium Pharma is a leading global radiopharmaceutical company with proven expertise in the development, manufacturing and supply of radiopharmaceuticals that transform the way cancer is diagnosed and treated. Headquartered in Boston with offices around the world, Curium’s mission is to find new and better ways to diagnose and treat cancer. With a global footprint that extends to more than 70 countries, a skilled and dedicated team of over 5,000 employees, and four manufacturing sites, Curium is uniquely qualified to meet the significant supply and distribution of established products that underlie success in the radiopharmaceuticals market. Curium’s global leadership is embodied in a diverse and extensive portfolio of over 45 products, that advance patient care for a wide range of cancers. Curium’s pioneering legacy in nuclear medicine is the foundation of the company’s dedication to innovation and portfolio expansion to cancer therapeutics, particularly in neuroendocrine tumors and with a late-stage pipeline exploring opportunities in prostate cancer. To learn more, visit . Inquiries: Curium Group Camilla Campell VP, Head of Global Communications Camilla.campbell@curiumpharma.com

放射疗法

2026-05-25

·药时代

70亿美元！核药赛道最大并购来了？

出海机会来了！现征集天然免疫领域的口服小分子创新药，适应症为炎症或免疫，要求中美已申报IND或处于I期临床。需机制新颖、靶点明确、差异化显著，知识产权清晰，数据完整可快速推进临床。欢迎感兴趣的药企立即联系药时代BD团队！ BD@drugtimes.cn 2026年5月22日，据彭博社援引知情人士报道，由私募股权基金CapVest Partners控股的放射性药物企业Curium Pharma，已向纳斯达克上市公司Lantheus Holdings提出收购要约，交易估值高达约70亿美元。若这笔交易最终落地，将一举刷新2023年百时美施贵宝以41亿美元收购RayzeBio的纪录，成为全球核药行业史上规模最大的并购案。消息传出后，资本市场迅速作出反应。截止当日收盘，Lantheus股价应声上涨9.03%，股价强势突破100美元大关，总市值攀升至67。06亿美元。来源：雪球网尽管目前双方尚未公开表态，但这桩潜在的收购案已然引发了行业对核药赛道格局重塑的深度遐想。值得注意的是，去年国际投资公司CapVest Partners LLP对Curium Pharma的估值为70亿美元，与Lantheus的市值相近。为何Lantheus能值70亿美元？首先是因为Lantheus手中握着王牌PYLARIFY®，全球首个年销售额突破10亿美元的放射性诊断药物。这款靶向前列腺特异性膜抗原（PSMA）的PET显像剂，自2021年5月获FDA批准以来，便以惊人的速度占领市场。截至2025年9月，已累计开展超过50万例扫描；2025年第一季度净销售额达2.577亿美元，同比增长约25%，持续领跑PSMA PET显像剂市场。除了现金牛产品，Lantheus在创新管线与商业化布局上也动作频频。今年3月，FDA批准了其新型前列腺癌PET显像剂Pylarify TruVu上市。这款新制剂具备更高的放射性浓度，能支持生产更大批次的PET扫描用示踪剂，有望显著提升先进诊断检查在供应不足地区的可及性。此外，Lantheus通过一系列精准收购不断拓宽护城河：2025年1月，斥资7.5亿美元收购Life Molecular Imaging，获得了阿尔茨海默病β-淀粉样蛋白斑块检测的明星产品Neuraceq；同月，又签署协议以最高超10亿美元的总对价收购Evergreen Theragnostics，不仅补充了针对神经内分泌肿瘤（NET）的注册阶段PET诊断剂OCTEVY，更极大地增强了其在放射性药物开发和生产端的复杂能力。当然，Lantheus的发展并非一帆风顺。其寄予厚望的治疗性药物PNT2002因临床试验中患者交叉导致总生存期数据模糊，最终不得不终止开发。在诺华Pluvicto已率先占据治疗市场主导的背景下，这一挫折曾让外界对其治疗管线的商业化前景蒙上阴影。但即便如此，Lantheus在诊断领域的龙头地位依然稳固，这也正是Curium最为看重的战略资产。估值70亿美元的Curium Pharma凭何收购？抛出橄榄枝的Curium Pharma同样来头不小。作为全球医用同位素的核心供应商，Curium大规模供应镥-177、锕-225等关键核素，同时也是放射性药物领域的CDMO（合同研发生产组织）巨头。2025年上半年，Curium完成了对Monrol的收购，这不仅大幅增强了其Lu-177的生产能力，帮助继续扩大其创新治疗诊断产品的投资组合和生产线，更将其在全球的PET工厂网络从西欧、亚洲延伸至东欧及中东地区，进一步夯实了其垂直整合的全球供应链。在创新药布局上，Curium同样不遑多让。2026年1月，其研发的1类放射性治疗药物177Lu-PSMA-I&T注射液的临床试验申请已获中国CDE受理（受理号为JXHL2600006），正式叩响中国市场大门，准备与诺华等巨头在RLT（放射性配体疗法）治疗市场正面交锋。那么，一家估值70亿美元的非上市公司，如何收购另一家市值相近的上市公司？资金从何而来？解开这个谜题的关键，在于Curium独特的资本结构。2025年11月，Curium完成了一项规模高达70亿美元的资本重组。这并非传统的融资，而是由控股股东CapVest设立“延续基金”，引入ICG、TPG、CVC等顶级机构接盘老股并注入新资金。这次资本重组对Curium的估值约为70亿美元，创下全球核医学领域最大规模交易纪录。换言之，Curium账面上虽无70亿现金，但其背后站立的私募资本拥有调动庞大资金池的能力。用资本运作吸引来的资金去收购一家拥有成熟商业化网络的上市公司，正是私募股权基金“买入、整合、增值、退出”的经典打法。70亿美元的要约相对于Lantheus目前市值，包含了合理的控制权溢价，完全符合市场逻辑。倘若本次交易落地，两家核药企业的结合或碰撞出“核爆级”影响。首先，业务上完美互补。Curium拥有强大的上游核素原料和Lu-177治疗管线，而Lantheus手握全球最成功的PSMA诊断产品PYLARIFY及强大的医生资源网络。二者结合，将打通从前列腺癌筛查、诊断到治疗的完整闭环，真正实现“诊疗一体化”。再者，私募资本的退出路径清晰。对于CapVest等投资机构而言，将Curium与Lantheus整合后，打造一个估值更高、业务更完整的核药巨头，无论是未来让这个新巨头独立上市（IPO），或者以更高的价格整体卖给诺华、礼来等更大的跨国药企，都将获得极其丰厚的回报，完成一次完美的投资闭环。这正是资本愿意为此买单的根本原因。核药收并购热潮，席卷而来当然，交易仍面临反垄断审查等诸多变数。但无论结果如何，这桩潜在的重磅并购案已经清晰地折射出核药赛道的产业趋势：它正在从“小而美”的细分领域，走向“大而强”的资本竞技场。回顾历史，核药的发展经历了漫长的蛰伏。从20世纪40年代放射性碘治疗甲状腺癌，到2013年拜耳氯化镭[223Ra]打开治疗大门，核药曾因原料获取难、监管严等问题长期不温不火。真正的爆发始于2018年至2022年间，随着诺华Lutathera和Pluvicto两款放射性配体疗法的相继上市，尤其是Pluvicto成为核药领域首个“十亿美元分子”，彻底印证了核药技术的临床与商业价值。此后， MNC掀起了疯狂的扫货模式。诺华、拜耳、礼来、阿斯利康、BMS、默沙东、强生等巨头均通过并购、引进、股权投资等方式入局核药，单笔交易金额动辄数十亿美元。这股热潮同样席卷了中国，2026年1月，湖南中晟全肽与诺华就RLT领域一款多肽资产达成全球授权合作，中晟全肽将获得5000万美元首付款，这标志着中国核药创新已开始融入全球主流产业链。创下中国RDC（多肽核素偶联药物）创新药授权出海第一单！ Curium对Lantheus的要约，正是这一宏大背景下的缩影。当诊断与治疗在核药领域交汇，当上游原料与下游市场在整合中碰撞，一个全新的核药巨头有望诞生。这笔收购案能否成交，核药的发展又将走向何方？药时代将持续关注。参考资料： 1.https://sa.marketscreener.com/news/lantheus-weighs-potential-7-billion-sale-after-curium-s-offer-bloomberg-news-reports-ce7f5adcd88ef127 2.https://be.marketscreener.com/beursnieuws/lantheus-overweegt-mogelijke-verkoop-van-7-miljard-dollar-aldus-bloomberg-news-c e7f5adcd88cfe26 3.https://www.capvest.com/news/curiumrecap 4.核药领袖Lantheus角逐核药赛道的生意经（夸克医药） 5.https://mrem.bernama.com/viewsm.php?idm=50703 6.https://db.yaozh.com/zhuce?comprehensivesearchcontent=177lU 7.https://www.gurufocus.com/news/2841497 8.公开资料封面图来源：即梦AI 首款！FDA批准吉利德丁肝疗法 2026-05-23 疗效堪比手术！礼来三靶点减肥药平均减重28.3% 2026-05-22 再鼎医药总裁兼COO离职！ 2026-05-22 百家药企联名力挺仍遭婉拒！FDA局长之位竟是“烫手山芋”？ 2026-05-21 版权声明/免责声明本文为原创文章。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 点击查看更多精彩内容！

2026-05-11

·小核说核药

225Ac-PSMA I&T：全球首个前瞻性Ⅰ期剂量递增研究结果

01. 背景简介 2026年4月，荷兰鹿特丹伊拉斯姆斯大学医学中心（Erasmus MC）放射科与核医学科Sui Wai Ling教授为通讯作者在《Journal of Nuclear Medicine》期刊上正式发表名为“Phase 1 Dose-Escalation Study of [²²⁵Ac] Ac-PSMA I&T in Patients with Metastatic Castration-Resistant Prostate Cancer: An Analysis of Safety, Tolerability, and Dosimetry”的研究论文，该研究是全球首个前瞻性Ⅰ期剂量递增研究，系统评估了 [²²⁵Ac]Ac-PSMA I&T 用于 mCRPC 的安全性、耐受性与剂量学结果。相关往期： JNM：[225Ac]Ac-PSMA-I&T临床前研究 PSMA核药的近期碎片笔记 02. 研究内容尽管以¹⁷⁷Lu‑PSMA-617为代表的PSMA靶向放射性配体疗法已获批用于转移性去势抵抗性前列腺癌（mCRPC），但现有治疗手段仍无法避免最终的耐药与疾病进展。相较于β核素，α核素²²⁵Ac‑PSMA凭借高高传能线密度及短射程的物理特性，展现出更强的抗肿瘤潜能。然而，目前尚缺乏关于[²²⁵Ac]Ac‑PSMA I&T的前瞻性I期剂量递增及全面的辐射剂量学研究数据，其最大耐受剂量（MTD）与体内生物分布特征仍有待明确。本研究为一项单中心、开放标签的Ⅰ期剂量递增临床试验（ClinicalTrials.gov 编号：NCT05902247；欧洲 EudraCT 编号：2020-001089-13），研究纳入9例mCRPC患者，分为8、10、12 MBq（0.216、0.270、0.324 mCi）三个队列，接受[²²⁵Ac]Ac‑PSMA I&T治疗。治疗计划为每个周期间隔8周，共计2个周期。研究的主要终点为评估药物的安全性、耐受性及确定Ⅱ期推荐剂量（RP2D）；次要终点包括通过全身平面显像、SPECT/CT及生物样本分析，测定红骨髓、肾脏、唾液腺及肿瘤的吸收剂量，并探索其对PSA应答、影像学疗效、总生存期（OS）及疼痛缓解的影响。本图是本研究的试验流程与剂量学采集方案时间轴图，清晰展示了从基线检查、两周期 [²²⁵Ac]Ac‑PSMA I&T 治疗给药、多时间点血/尿样本采集、全身平面与 SPECT/CT 显像，到疗效评估 PET/MRI 检查的完整时序与操作节点，表明该研究采用规范的Ⅰ期剂量递增设计，通过系统化、多时点的生物样本与影像采集完成安全性监测与精准剂量学评估，同时明确不同剂量组的检测差异，为剂量推荐与数据可靠性提供流程依据。本图是接受 [²²⁵Ac]Ac‑PSMA I&T 治疗患者的剂量学示例图，包含治疗前⁶⁸Ga‑PSMA PET/MRI 定位、治疗后全身平面显像靶器官勾画，以及基于子核素²¹³Bi（440keV）、²²¹Fr（218keV）检测得到的血液、尿液放射性活度‑时间曲线，表明药物在体内呈双相清除特征，尿液可快速排出大部分放射性，血液清除相对缓慢，为体内辐射剂量计算与临床辐射防护提供了关键依据。本图为接受 2 个周期 8 MBq [²²⁵Ac]Ac‑PSMA I&T 治疗患者的 [⁶⁸Ga]Ga‑PSMA PET/MRI 对比影像，直观展示了治疗后患者骨转移灶数量显著减少、腹膜后淋巴结转移灶明显消退的变化，是疗效的直接影像证据，表明 [²²⁵Ac]Ac‑PSMA I&T 对转移性去势抵抗性前列腺癌具有明确的抗肿瘤效果，可实现病灶的影像学部分缓解。本表是按 8、10、12 MBq 三个剂量组分别统计的 PSA 应答与 RECIST 1.1 影像学疗效数据，本图是 [²²⁵Ac]Ac‑PSMA I&T cycle1 治疗后患者的 Kaplan–Meier 总生存曲线，二者共同表明该药物对转移性去势抵抗性前列腺癌具有一定治疗活性，44% 的患者实现 PSA 下降≥50%，仅 8 MBq 组出现 1 例部分缓解（PR），10/12 MBq 组无 PR，稳定/进展各占 1/3；中位总生存期达 15 个月，但不同剂量组间疗效无明显梯度差异，整体疗效呈现个体化差异。安全性方面：[²²⁵Ac]Ac‑PSMA I&T 整体安全可耐受，89% 患者出现不良反应，最常见为口干（89%）、贫血（44%）与乏力（44%），12 MBq 组出现 2 例剂量限制性毒性（≥2 级口干），确定 Ⅱ 期推荐剂量为 10 MBq；表2显示关键器官中位吸收剂量，暗示肿瘤吸收剂量远高于正常器官，唾液腺、肾脏是剂量限制器官（±误差较大）；表4是本研究实测吸收剂量与既往 [²²⁵Ac]Ac‑PSMA‑617、[²¹³Bi]Bi‑PSMA‑617 估算剂量的对比结果。 03. 小结总之，本研究首次报道了针对mCRPC的[²²⁵Ac]Ac‑PSMA I&T前瞻性Ⅰ期剂量递增试验结果：推荐Ⅱ期剂量（RP2D）为10 MBq、主要毒性为口干及血液学毒性、肿瘤吸收剂量显著高于正常器官、因成像限制未能实现SPECT/CT定量剂量学、证实该疗法在mCRPC中具有可控的安全性和潜在的抗肿瘤活性。 ●【CDE核药简讯】：阿斯利康、礼来 ●【CDE核药简讯】：先通医药氟 [18F] 妥司特注射液 ●【CDE核药简讯】：诺宇 ●新核药[68Ga]BED003临床转化研究声明：本文观点仅代表小核本人，欢迎批评指正；如需转载请注明来源；小核始终秉持客观中立原则，不发布主观评述或倾向性引导，建议读者结合原文及多方信息独立研判。小核 | xiaoheshuoheyao777（微信） Copyright © 小核说核药 All Rights Reserved.

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

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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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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT04647526 (SPLASH, CTgov)	临床3期	转移性去势抵抗性前列腺癌	455	[Lu-177]-PNT2002 (Randomization Phase: [Lu-177]-PNT2002 (Arm A))	膚鬱壓積遞蓋鏇艱鏇壓(築鏇膚糧願膚夢鹹願簾) = 繭選襯選範選鏇繭夢網鹹膚網顧鏇餘鑰積鬱繭 (糧膚艱鹽願窪選網糧襯, 膚鏇艱鹽淵窪餘積鑰網 ~ 積顧餘顧簾鹹壓積願積) 更多	-	2026-01-13
				Enzalutamide+Abiraterone+[Lu-177]-PNT2002 (Randomization Phase: Abiraterone or Enzalutamide (Arm B))	膚鬱壓積遞蓋鏇艱鏇壓(築鏇膚糧願膚夢鹹願簾) = 築鹹憲網醖構鬱襯鬱範鹹膚網顧鏇餘鑰積鬱繭 (糧膚艱鹽願窪選網糧襯, 構鏇網廠製鬱獵遞鑰憲 ~ 遞齋蓋醖簾獵憲壓膚網) 更多
NCT04886986 (ASCO_GU2025) 人工标引	临床1期	晚期前列腺癌	18	225Ac-J591 + PNT2002	鏇構襯築選鑰壓鏇選膚(遞製願鬱鬱蓋鏇獵憲壓) = 35 KGBq/kg 壓憲鬱齋鬱遞憲築廠範 (鏇齋蓋製積鹹衊網簾觸 ) 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	簾鬱夢製襯齋獵醖築獵(蓋鹹廠築積繭製窪蓋襯) = 願糧鏇製衊艱積鬱艱鏇壓網餘鬱齋餘襯艱積廠 (襯醖蓋艱夢簾簾構範鹹, 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	積鹽醖窪積積繭壓鹽鹹(願簾壓網製鹽顧齋觸齋) = 網繭選淵顧淵窪遞襯夢壓獵願築製憲獵夢艱願 (憲廠顧憲簾繭艱鏇願遞 )	积极	2024-11-13
				Hormone therapy	積鹽醖窪積積繭壓鹽鹹(願簾壓網製鹽顧齋觸齋) = 網夢艱鬱鬱範鏇齋觸壓壓獵願築製憲獵夢艱願 (憲廠顧憲簾繭艱鏇願遞 )
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	窪廠網範艱襯蓋襯積築(繭觸選鏇膚艱壓築齋壓) = CTCAE grade 3 anaemia was seen in four patients 鏇壓鹽襯築願簾衊糧壓 (鏇艱夢網鬱築襯糧窪範 ) 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	範衊繭壓簾鏇壓選鹹選(糧遞鬱構壓壓顧製壓構) = 顧醖襯簾憲獵憲壓範鏇淵獵醖選觸願鹽繭齋積 (構遞獵積廠鹹網憲選積, 7.4 ~ 10.0) 更多	积极	2024-09-15
				Alternate ARPI	範衊繭壓簾鏇壓選鹹選(糧遞鬱構壓壓顧製壓構) = 構鑰艱憲艱選齋製襯壓淵獵醖選觸願鹽繭齋積 (構遞獵積廠鹹網憲選積, 4.7 ~ 7.9) 更多
SNMMI2024	N/A	-	-	[177Lu]Lu-PSMA I&T	繭餘簾衊襯鑰蓋糧網遞(衊網蓋餘膚構製膚鹽鹽) = No CTC grade ≥III occurred after RLT 願醖膚築淵壓壓鏇製願 (顧襯淵餘鏇壓顧簾膚廠 ) 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	蓋築膚艱蓋蓋憲範繭壓(窪築窪簾簾鬱憲淵願襯) = 糧積範積蓋壓選艱積範蓋襯衊憲獵衊繭鑰齋糧 (醖膚製獵醖鹹膚餘鬱範 ) 更多	积极	2023-12-18
				ARPI	蓋築膚艱蓋蓋憲範繭壓(窪築窪簾簾鬱憲淵願襯) = 憲夢選糧範鹹範鑰鑰餘蓋襯衊憲獵衊繭鑰齋糧 (醖膚製獵醖鹹膚餘鬱範 )
NCT04886986 (ASCO 12023 \| ASCO 22023) 人工标引	临床1/2期	前列腺癌	18	225Ac-J591+PNT2002	憲獵廠鑰鹹憲鬱積憲構(憲顧鏇餘膚鬱蓋鏇構齋) = 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. 膚夢遞艱窪糧鬱觸選窪 (蓋鹹膚衊淵艱鹹獵繭網 ) 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	鹽艱遞齋鑰範廠選鹹製(顧壓壓鹹糧窪齋繭衊餘) = The addition of 177 Lu-PNT2002 to metastasis-directed therapy alone may potentially further forestall disease progression. 廠夢壓願簾顧廠獵願願 (簾膚積範廠蓋糧鏇鏇衊 )	积极	2023-03-02
				SBRT