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更新于：2026-02-27

Lutetium (177Lu) zadavotide guraxetan

更新于：2026-02-27

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.

POINT Biopharma, Inc.

+ [5]

非在研机构

POINT Biopharma Corp.

Progenics Pharmaceuticals, Inc.

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)临床申请

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

/ 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.

150

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

2026-02-26

·GlobeNewswire-Health Care

Curium Announces Pharmacokinetics and Dosimetry Data for Investigational Lutetium-177 Zadavotide Guraxetan in Metastatic Castration-Resistant Prostate Cancer at ASCO GU 2026

Dosimetry data from the Phase 3 ECLIPSE substudy demonstrated favorable organ radiation absorbed doses supporting administration of 7.4 GBq for up to six cycles BOSTON, Feb. 26, 2026 (GLOBE NEWSWIRE) -- Curium, a world leading nuclear medicine company dedicated to using cutting-edge technology and innovative science to personalize diagnoses and treatments for patients with cancer, today announced the first dosimetry and pharmacokinetics (PK) data from a substudy of the ongoing pivotal Phase 3 ECLIPSE clinical trial (NCT05204927). The Phase 3 ECLIPSE clinical trial evaluates lutetium-177 (Lu-177) zadavotide guraxetan (a proprietary formulation of 177Lu-PSMA-I&T), an investigational prostate-specific membrane antigen (PSMA)-targeted radioligand therapy, for the treatment of patients with metastatic castration-resistant prostate cancer (mCRPC) who have progressed on prior androgen receptor pathway inhibitor (ARPI). The data will be presented in a poster at the American Society of Clinical Oncology Genitourinary Cancers Symposium (ASCO GU) taking place 26-28 February, 2026, in San Francisco, California. The nonrandomized PK/dosimetry substudy (n=26) was conducted as part of the ECLIPSE trial to evaluate the biodistribution and radiation absorbed dose of Lu-177 zadavotide guraxetan to organs of interest. Sakir Mutevelic, MD, Curium’s Chief Medical Officer said: “These data represent the first published dosimetry data for our investigational formulation of Lu-177 zadavotide guraxetan, with projected mean cumulative renal doses remaining low for a six-cycle treatment regimen, thus supporting a protocol amendment to increase from a maximum of four doses to six in the ECLIPSE trial. We will continue to evaluate the ECLIPSE clinical trial data with the goal of bringing this potential therapy to market for those living with mCRPC. This reinforces our long-term vision to treat 80 percent of cancers within the next 10-15 years.” Frankis Almaguel, MD, PhD, Assistant Professor, Medicine, Hematology/Oncology, Loma Linda University Health Cancer Center, and presenting author said: “These data reinforce the clinical utility of using dosimetry data to inform clinical trial protocol design, as well as identify organs at highest risk of radiation exposure.” A poster, Pharmacokinetics and Dosimetry of Lutetium Lu 177 Zadavotide Guraxetan in Patients With Metastatic Castration-Resistant Prostate Cancer (mCRPC): Results From the ECLIPSE Sub-study (Abstract #174), will be presented on Thursday, 26 February in Poster Session A: Prostate Cancer. The abstract is available here. ASCO GU attendees can learn more about Curium by visiting booth 11 during the symposium. About Curium Curium is a world 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 3,000 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 www.curiumpharma.com. Inquiries: Camilla CampbellVP, Head of Global Communicationscommunications@curiumpharma.com

临床3期临床结果ASCO会议

2026-02-18

·同写意

核药告别“小众”标签

100+全球先锋领袖现场开讲、50+顶尖新基建机构抢先入驻、1000+产业精英面对面链接，中国ADC和核药产业界规格最高、影响力最大、汇聚创新力量最全的年度品牌盛会！ 2026年伊始，放射性药物领域即以一场备受瞩目的IPO拉开序幕。 1月，Aktis Oncology完成扩大规模的首次公开募股，融资总额约3.18亿美元，发行价每股18美元，礼来公司作为锚定投资者承诺投入约1亿美元。这是本年度首批规模可观的生物技术IPO之一，也彰显了资本市场对放射性药物领域的高度信心。 Aktis在IPO招股说明书中，特别强调了其同位素供应链布局，包括获取锕-225的稳定供应渠道。这一细节，再次印证了材料获取与生产能力在放射性药物研发战略中的核心地位。此外，Aktis与礼来保持战略合作，礼来有权将部分合作项目推进至后期开发与商业化阶段。单一IPO事件尚不足以断言生物科技融资市场的全面回暖，但此次融资的规模与大型药企的深度参与，至少表明放射性药物领域仍在持续吸引优质资本的关注。 TONACEA 01 “进攻”前线放射性配体疗法通过将小分子配体、多肽或抗体等靶向分子，与放射性同位素结合，实现对肿瘤部位的精准辐射递送，同时最大限度减少对正常组织的损伤。该领域普遍采用诊疗一体化策略：首先通过影像学检查确认靶点摄取情况，随后仅对显像阳性的患者实施治疗。早在20世纪40年代，放射性碘就已用于甲状腺疾病治疗，但在肿瘤学领域的重大突破发生在数十年后。肽受体放射性核素疗法（PRRT）在神经内分泌肿瘤治疗中的应用，标志着该领域的重要进展。通过使用放射性标记的生长抑素类似物靶向表达生长抑素受体的肿瘤细胞，最终促成2018年镥-177 dotatate（Lutathera）在美国获批上市。此后，前列腺癌治疗领域也迎来突破，针对前列腺特异性膜抗原（PSMA）的疗法相继问世，PSMA作为一种在前列腺肿瘤中高表达的蛋白，成为理想的治疗靶点。到2025年，放射性配体疗法的版图很大程度得以整合巩固，最重大的结构性变化，并非验证放射性配体疗法的有效性，而是其治疗线序的显著前移。 Pluvicto适应症的扩展，标志着该疗法不再局限于末线治疗场景，正式进入更早期的治疗梯队。换言之，放射性配体疗法正逐步探索其主流肿瘤治疗手段的地位。 PSMAdition临床试验的结果进一步印证这一趋势。该研究探索了Pluvicto联合标准激素治疗在转移性激素敏感性前列腺癌（mHSPC）中的应用价值。诺华公布的数据显示，在预设的中期分析中，联合治疗组在影像学无进展生存期方面取得具有统计学意义和临床价值的显著改善。若该适应症最终获批，放射性配体疗法将与一线激素治疗并驾齐驱，而非仅作为后续补救措施。 2025年的另一个重要信号，在于资本流向的转变。投资者不再满足于追逐少数几个前景可期的候选药物，而是开始为更大规模的产业化布局铺路。当年完成的数起大规模私募融资，资金用途均明确指向同位素获取、生产网络建设和平台能力提升，而非仅仅用于推进单一临床项目。 • 瑞士放射性制药企业Nuclidium于7月完成7900万瑞士法郎（约9800万美元）B轮融资，旨在推进其铜基诊疗一体化项目的同时，扩建欧美地区的生产基础设施。 • 仅一日之隔，Actithera获得超额认购的7550万美元A轮融资，用于推进靶向成纤维细胞活化蛋白（FAP）的放射性配体项目及其发现平台建设。 • ARTBIO随后完成1.32亿美元B轮融资，明确将资金用于α放射性配体管线开发及同位素供应与生产能力建设。 • AdvanCell也在2025年初完成1.12亿美元C轮融资，同步推进临床项目与靶向α疗法生产能力的规模化建设。 TONACEA 02 巨头争锋核药市场的特殊性，决定了这是一个高门槛的游戏。与传统药物不同，放射性药物研发需要跨越核物理、放射化学、肿瘤学和药物研发多个领域，且涉及严格的放射性物质管理规范。根据Evaluate Pharma的数据，全球核药市场在2023年已达到约100亿美元规模，预计到2030年将增长至300亿美元。其中，用于癌症治疗的放射性药物占据最大份额，特别是前列腺癌、神经内分泌肿瘤和淋巴瘤等适应症领域。诺华无疑是这场竞赛的领头羊，通过一系列精心策划的收购，构建了核药领域的完整版图。2017年，诺华以39亿美元收购Advanced Accelerator Applications，获得了Lutathera；2018年，又以21亿美元收购Endocyte，获得了后来成为重磅产品的Pluvicto。这些投资正在产生丰厚回报。2025年，Pluvicto全年销售额达19.9亿美元，同比增长42%；Lutathera销售额为8.16亿美元。诺华预计，Pluvicto的销售峰值可能超过50亿美元，有望成为历史上最成功的核药产品。诺华一边持续推进Pluvicto适应症拓展，继2025年3月扩至化疗前mCRPC人群后，近期mHSPC III期研究传来捷报；一边布局α核素领域，推进β核素与α核素协同治疗研发。近年来，诺华通过收购多家核药研发企业，丰富多癌种管线，将RLT技术拓展至肺癌、乳腺癌等高发实体瘤领域。阿斯利康则选择了一条差异化的追赶路径。 2024年3月，阿斯利康宣布以约24亿美元的总交易价值收购Fusion Pharmaceuticals，一举获得了包括FPI-2265在内的多款在研核药。FPI-2265是一种针对PSMA的放射性偶联药物，采用了锕-225这一α核素，与诺华Pluvicto使用的β核素镥-177形成技术差异。 α核素与β核素的不同选择代表了核药研发的两条技术路线。α粒子质量更大，能量更高，能更有效地造成DNA双链断裂，但同时也面临更大的安全性挑战。阿斯利康押注α核素技术，试图在下一代核药技术上建立领先优势。礼来的入局则更加激进。通过收购Point Biopharma，礼来获得了PNT2002等候选药物，快速补齐PSMA靶向核药管线，同时兼顾多癌种、多技术路线探索。2025年2月，礼来与AdvanCell达成战略合作，整合其Pb212生产技术与核素开发设施，共同推动靶向α放射性核素疗法研发。目前，礼来核药管线已覆盖RLT、α核素、RDC等多个领域，涉及多种癌种，快速从核药“新手”成长为有力竞争者。除了上述巨头，拜耳凭借其已上市产品Xofigo（镭-223）也在核药市场占有一席之地。Xofigo主要用于去势抵抗性前列腺癌骨转移治疗，凭借显著疗效占据全球相关市场重要份额。 TONACEA 03 2026年，值得关注 01 监管审批节点 ITM公司的Lu-edotreotide-177（ITM-11）用于胃肠胰神经内分泌肿瘤（NETs）的审评进程值得关注，FDA已设定目标审批日期为2026年8月28日。若顺利获批，该产品将打破镥-177 dotatate（Lutathera）自2018年以来在该领域的独占格局，为神经内分泌肿瘤患者提供更多PRRT治疗选择。 02 数据更新继Pluvicto适应症前移之后，业界目光转向更早期治疗数据的成熟度。诺华在PSMAdition研究中公布的影像学无进展生存期获益引发广泛关注，但总生存期数据尚不成熟。2026年若有进一步数据披露，将有助于明确该疗法在转移性激素敏感性前列腺癌一线治疗策略中的定位及其获益持久性。 03 α核素疗法的临床验证大型药企的战略布局已明确指向α核素疗法领域，BMS收购RayzeBio、阿斯利康收购Fusion均彰显了其对这一技术路线的高度认可。RayzeBio的RYZ101与Fusion的FPI-2265，都已进入后期临床开发阶段。 2026年的关键看点不仅在于早期应答率的提升，更在于耐受性数据的积累、重复给药的可行性验证以及α核素规模化供应能力的实际落地。上述证据的完善将为α核素疗法的广泛临床应用奠定基础。 — 写在最后 — 放射性配体疗法能否突破PSMA与生长抑素受体这两大成熟靶点的局限，是衡量该领域发展潜力的重要指标。值得关注的是，新兴靶点能否在大规模临床试验中展现出可靠的影像学筛选能力、稳定的肿瘤摄取特征以及可控的安全性谱。放射性配体疗法对同位素半衰期的敏感性，决定了其规模化发展必然受制于生产与配送网络的完善程度。随着更多项目进入后期开发阶段并向更早期治疗线序推进，跨中心的药物配送能力将日益成为影响临床应用的关键因素。预计2026年将涌现更多聚焦于产业链配套能力的战略合作与投资布局。参考文章： 1、Will radioligand therapies keep the momentum going in 2026? ；labiotech 2、硬“核”破局，Aktis敲钟前夜；同写意

2026-02-05

·汇佳生物

放射性药物的淘金热潮：为何大型药企豪掷数十亿美元押注靶向放射性疗法

抗体与小分子药物风头暂歇！肿瘤治疗领域迎来新的主力军—— 靶向放射性疗法，其携放射性 “杀伤力” 强势登场。当下，跨国药企正掀起一场耗资数十亿美元的放射性药物淘金热潮，企业接连开展收购、斥巨资布局这一技术，而该技术有望彻底改写肿瘤治疗的格局。这并非传统的放射治疗，我们所说的是被称作“智能炸弹” 的靶向放射性配体疗法（RLT）。这类疗法如同精准制导导弹，主动寻找肿瘤细胞并直接向其释放致死剂量的放射线，同时最大程度保护健康组织。为何药企突然大举转型布局？数十年来，放射治疗一直以体外射线照射或全身性治疗为主，伴随显著的副作用。而多重因素的叠加改变了这一局面，让制药巨头们对放射性药物产生了前所未有的兴趣： 1. 诊疗一体化革命：所见即所治放射性药物最具吸引力的特质之一，便是其诊疗一体化的能力。一款药物平台，便能实现癌症的精准诊断与治疗双重目标。临床中，医生会先为患者注射低能放射性标记的同款药物，这一“诊断剂量” 的药物在体内游走，特异性结合肿瘤细胞，使肿瘤在 PET 显像中清晰显影。借助这一手段，临床医生能精准为癌症分期、定位所有肿瘤病灶，更关键的是，可确认患者的肿瘤是否表达该药物的靶向靶点，彻底告别治疗中的盲目试错。一旦靶点得到确认，医生会为患者注射高能放射性标记的同款药物，这一“治疗剂量” 的药物将致死性辐射直接作用于已定位的肿瘤细胞，在提升疗效的同时，最大程度降低脱靶损伤。这正是精准医疗的实际落地应用。 2. 攻克耐药难题：物理作用的独特优势肿瘤细胞的耐药性向来令人棘手，它们能进化出复杂的生物学机制，对化疗、免疫治疗甚至靶向治疗产生抵抗。但肿瘤细胞很难对纯粹的物理作用产生耐药性。放射性药物通过释放高能粒子（如β 粒子或 α 粒子）从物理层面破坏肿瘤细胞的 DNA，造成不可逆的损伤并最终导致细胞死亡。这一核心作用机制，为攻克其他疗法难以奏效的耐药肿瘤，提供了一款强有力的新型武器。 3. 重磅药物的成功验证：Pluvicto 的临床与商业双重答卷 Novartis 旗下前列腺癌治疗药物 Pluvicto（Lu-177 vipivotide tetraxetan）的问世，无可辩驳地证明了靶向放射性配体疗法的商业价值与临床疗效。自获批上市以来，Pluvicto 已成为重磅炸弹级药物，年销售额近 10 亿美元，这一成果也印证了患者、医生与医保支付方对这一创新疗法的接受度。这一成功案例，彻底点燃了整个行业对放射性药物的布局热情。收购狂潮：数百亿资金涌入赛道在过去 24 个月里，肿瘤领域的头部药企纷纷争抢放射性药物赛道的布局机会，一系列金额达数十亿美元的收购案接连落地： ·2024 年，AstraZeneca 以 24 亿美元收购 Fusion Pharmaceuticals，斩获新一代以锕 - 225 为核心的 α 射线疗法研发管线； ·2023 年，Eli Lilly 以 14 亿美元收购 Point Biopharma，核心看中其极具潜力的前列腺癌候选药物 PNT2002； ·2023 年末，Bristol Myers Squibb 以高达 41 亿美元的价格收购 RayzeBio，为其管线新增胃肠胰神经内分泌肿瘤治疗方案； ·作为赛道先行者的 Novartis，2024 年初再以 17.5 亿美元收购 Mariana Oncology，进一步布局下一代靶向放射性配体疗法研发管线； ·就连 Sanofi 也在 2024 年加入战局，与 Orano Med 达成合作，联合开发针对罕见癌症的放射性配体药物。这并非单纯的并购传闻，而是这些制药巨头在战略层面的根本性重新布局。下一个前沿：α 射线疗法时代当前，以 Pluvicto 为代表的成功药物均采用 β 粒子发射体（如Lu-177），而行业的下一波创新浪潮，正聚焦于 α 粒子发射体（如Ac-225）。 β 粒子的作用模式如同霰弹枪射击：辐射射程约数毫米，虽能发挥治疗作用，但可能对周围健康细胞产生 “旁观者效应” 损伤；而 α 粒子则如同狙击枪子弹：携带的能量远高于 β 粒子，辐射射程却仅为几个细胞的直径。这一特性让 α 粒子能在高效杀伤肿瘤细胞的同时，对邻近健康组织的影响降至最低，有望实现疗效与安全性的双重提升。未来数年，多款 α 射线疗法的关键临床试验数据结果将陆续公布。独特挑战：错综复杂的物流体系与可在货架上存放数年的口服药片不同，放射性药物面临着一个独特且复杂的难题—— 它们会过期。多数放射性药物的半衰期极短，药效会快速衰减，部分药物的有效期甚至仅有数天乃至数小时。这一特性，迫使制药企业转型为专业的物流与生产运营机构。也正因如此，Novartis 才在 2026 年 1 月宣布一项高达 230 亿美元的美国投资计划，拟在佛罗里达州和印第安纳州打造专业化的放射性药物生产网络。企业需要在靠近医院与患者的区域生产这类前沿药物，才能避免珍贵的放射性有效成分在运输途中衰变。这一套精密的物流运作流程，为药物研发与生产增添了新的复杂度和成本，但制药巨头们显然愿意迎接这一挑战。未来展望放射性药物领域的发展充满活力且日新月异，人类对这类靶向放射性疗法的全部潜力，仍处于初步探索阶段。随着研究的不断推进，我们有望看到： ·除前列腺癌外，更多新的治疗靶点被发现； ·连接子技术持续优化，进一步提升药物的靶向特异性与递送效率； ·靶向放射性配体疗法与免疫治疗、其他靶向药物联用的联合治疗方案落地； ·药物生产与供应链体系不断升级，实现药物递送的最优化。这场放射性药物的淘金热潮，并非昙花一现的行业趋势，而是肿瘤治疗理念的根本性变革。对患者而言，这意味着未来将迎来更精准、更高效且潜在毒性更低的治疗方案；对制药行业而言，这是一场耗资数十亿美元的豪赌，赌的是一个全新的未来—— 放射线不再是治疗肿瘤的 “钝器”，而是一款调校精准、能挽救生命的精密武器。往期回顾大阪大学与 Sumitomo Heavy Industries 合作研发砹类放射性药物英国首批患者接受 Blue Earth Therapeutics 研究性放射性药物疗法 ——Lu-177 rhPSMA-10.1 注射液治疗转移性去势抵抗性前列腺癌新型诊疗一体化放射性药物组合有望攻克上消化道肿瘤汇佳生物专注于转化医学领域的前沿研究及临床转化应用技术，业务涵盖生物标志物和药物靶标技术，新型诊断试剂及治疗药物的研发，相关仪器设备的开发及临床转化技术的应用，实现了产、医、研的融合发展。媒体合作/科研宣传/产品咨询长按二维码，联系我们

放射疗法并购抗体药物偶联物

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

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研发状态

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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))	憲積壓壓憲構觸齋齋獵(艱糧壓餘築糧壓壓壓蓋) = 願憲鑰餘願艱憲齋鏇製膚窪築衊鬱網繭夢鑰齋 (選糧積鹽鏇簾淵製齋遞, 鏇鹽獵衊鏇夢鏇築遞鬱 ~ 選構夢願構蓋鬱鹹淵繭) 更多	-	2026-01-13
				Enzalutamide+Abiraterone+[Lu-177]-PNT2002 (Randomization Phase: Abiraterone or Enzalutamide (Arm B))	憲積壓壓憲構觸齋齋獵(艱糧壓餘築糧壓壓壓蓋) = 醖選簾憲淵鏇鬱觸憲獵膚窪築衊鬱網繭夢鑰齋 (選糧積鹽鏇簾淵製齋遞, 艱鹽遞鹽淵網簾遞鑰淵 ~ 鬱憲壓衊鏇顧蓋獵顧網) 更多
NCT04886986 (ASCO_GU2025) 人工标引	临床1期	晚期前列腺癌	18	225Ac-J591 + PNT2002	製夢鏇鏇淵構鏇遞製艱(壓網獵範夢艱餘壓壓鬱) = 35 KGBq/kg 餘淵壓網網餘淵鹹簾積 (糧窪築築衊鏇襯醖鑰繭 ) 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	構構選窪選窪糧遞構顧(醖糧鏇積築窪衊構築鬱) = 襯衊鏇顧遞蓋鏇糧餘鏇膚窪鑰膚齋鹽膚簾獵鹽 (艱簾積憲獵廠鑰糧鑰製, 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	夢膚膚艱繭簾鬱鑰範壓(鏇構顧鏇艱膚製選築窪) = 積構衊獵簾積積築築積積衊積鏇選齋遞積繭網 (願壓糧鬱鹽夢築鏇簾膚 )	积极	2024-11-13
				Hormone therapy	夢膚膚艱繭簾鬱鑰範壓(鏇構顧鏇艱膚製選築窪) = 鹽積觸艱窪壓蓋壓顧簾積衊積鏇選齋遞積繭網 (願壓糧鬱鹽夢築鏇簾膚 )
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	鬱積淵醖願艱選顧鏇鹽(憲選壓積顧構鑰鬱窪願) = CTCAE grade 3 anaemia was seen in four patients 願餘艱願廠餘網築積製 (網蓋衊蓋顧齋鹽構廠簾 ) 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	襯膚糧壓構鏇選醖鬱鹹(範窪顧範淵夢選憲鏇範) = 糧艱夢齋鏇顧簾選窪憲衊繭廠鑰蓋觸膚鬱夢顧 (顧鹽鬱醖繭範簾獵願膚, 7.4 ~ 10.0) 更多	积极	2024-09-15
				Alternate ARPI	襯膚糧壓構鏇選醖鬱鹹(範窪顧範淵夢選憲鏇範) = 製醖構積齋觸獵鏇夢願衊繭廠鑰蓋觸膚鬱夢顧 (顧鹽鬱醖繭範簾獵願膚, 4.7 ~ 7.9) 更多
SNMMI2024	N/A	-	-	[177Lu]Lu-PSMA I&T	蓋衊觸網艱願鏇鬱範糧(鬱繭願壓淵鹽願衊觸網) = No CTC grade ≥III occurred after RLT 淵顧鬱齋製醖觸願餘願 (淵齋遞淵蓋範廠廠獵鹽 ) 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	製糧築廠夢齋憲鏇糧淵(憲淵鏇範網糧鹹積壓積) = 觸糧衊鑰獵鑰鏇鹹鑰簾構製鬱窪醖積顧憲築襯 (觸顧願網獵鹹齋艱獵製 ) 更多	积极	2023-12-18
				ARPI	製糧築廠夢齋憲鏇糧淵(憲淵鏇範網糧鹹積壓積) = 顧淵願觸鑰顧糧艱蓋醖構製鬱窪醖積顧憲築襯 (觸顧願網獵鹹齋艱獵製 )
NCT04886986 (ASCO 12023 \| ASCO 22023) 人工标引	临床1/2期	前列腺癌	18	225Ac-J591+PNT2002	積鬱齋淵窪壓憲廠艱艱(觸築繭範醖窪選繭窪製) = 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. 鑰簾觸築齋艱襯網鏇鏇 (獵齋廠蓋顧網憲願憲構 ) 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	製廠鏇淵願廠構餘壓壓(網夢範鹽鑰範繭遞夢選) = The addition of 177 Lu-PNT2002 to metastasis-directed therapy alone may potentially further forestall disease progression. 窪積顧願觸鏇鑰範製願 (範選遞鑰鑰鏇膚淵簾顧 )	积极	2023-03-02
				SBRT