This phase II trial investigates how well 177Lu-DOTATATE works in treating patients with breast cancer that is stage IV or has come back (recurrent). 177Lu-DOTATATE may shrink or destroy the tumor or circulating breast cancer stem cells if they show evidence of the SSTR2. 177Lu-DOTATATE is a targeted therapy that uses DOTATATE, linked to a radioactive agent called 177Lu. DOTATATE attaches to tumor cells with SSTR2 and delivers 177Lu to kill them. Giving 177Lu-DOTATATE may help decrease the number and size of tumors and the number of circulating cancer stem cells in patient's blood for the treatment of patients with breast cancer positive for SSTR2.

开始日期2025-12-01

申办/合作机构

OHSU Knight Cancer Institute

[+3]

CTR20252270

/ Recruiting临床3期

一项评价 [177Lu]Lu-DOTA-TATE在新诊断为1级和2级（Ki-67 < 10%）晚期GEP-NET伴高疾病负荷患者中的有效性和安全性的III期、多中心、随机、开放性研究（NETTER-3）

本研究的目的是在新诊断为生长抑素受体阳性（SSTR+）、高分化1级和2级（G1和G2）（Ki-67 < 10%）晚期胃肠胰神经内分泌瘤（GEP-NET）伴高疾病负荷（高疾病负荷示例见第5.1节）的患者中，评价 [177Lu]Lu-DOTA-TATE + 奥曲肽LAR相比于奥曲肽LAR单药的有效性和安全性。

开始日期2025-10-14

申办/合作机构

Advanced Accelerator Applications (Italy) Srl

[+3]

NCT07150546

/ Not yet recruiting临床1期IIT

Combination External Radiation and 177Lu-DOTATATE for Large Gastrointestinal Neuroendocrine Tumors: A Single Arm Pilot Clinical Trial

This phase I trial tests the safety and effectiveness of stereotactic body radiation therapy (SBRT) followed by 177Lu-DOTATATE peptide receptor radionuclide therapy (PRRT) in treating patients with large well-differentiated grade 1-2 digestive system neuroendocrine tumors that cannot be removed by surgery (unresectable). SBRT is a type of external radiation therapy that uses special equipment to position a patient and precisely deliver radiation to tumors in the body. The total dose of radiation is divided into smaller doses given over several days. This type of radiation therapy helps spare normal tissue. 177Lu-DOTATATE is a radioactive drug. It binds to a protein called somatostatin receptor, which is found on some neuroendocrine tumor cells. 177Lu-DOTATATE builds up in these cells and gives off radiation that may kill them. It is a type of radioconjugate and a type of somatostatin analog. Giving PRRT after SBRT may reduce the chances of the disease returning or getting worse, compared to the standard treatment of PRRT alone.

开始日期2025-09-01

申办/合作机构

Emory University

[+1]

100 项与 (177镥)镥氧奥曲肽相关的临床结果

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100 项与 (177镥)镥氧奥曲肽相关的转化医学

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100 项与 (177镥)镥氧奥曲肽相关的专利（医药）

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1,141

项与 (177镥)镥氧奥曲肽相关的文献（医药）

2026-01-01·JOURNAL OF NEURO-ONCOLOGY

Efficacy of Intra-arterial [177Lu]Lu-DOTATATE monotherapy for treatment-refractory meningioma

Article

作者: Tolboom, N ; Lapa, C ; van der Schaaf, I C ; Snijders, T J ; Braat, A J A T ; Amerein, A ; El Ghalbouni, A ; Patt, M ; Maurer, C J

Abstract:

Purpose:

For meningiomas that are refractory after local treatments, there are no systemic evidence-based therapeutic options to date. In recent years, somatostatin-targeted radionuclide therapy has emerged as a promising new treatment modality. Recent studies have indicated that intra-arterial administration of [177Lu]Lu-DOTATATE may increase the tumor absorbed dose. This study aims to assess the efficacy of intra-arterial [177Lu]Lu-DOTATATE in a cohort of treatment-refractory meningiomas.

Materials and methods:

Retrospective cohort study including patients diagnosed with treatment-refractory meningioma (WHO grade 1–3), who had received at least one cycle of intra-arterial [177Lu]Lu-DOTATATE. Primary outcomes were progression-free survival (PFS) and overall survival (OS). Secondary outcomes included objective response, and safety and toxicity.

Results:

Seventeen patients with a median follow-up duration of 36 months (range: 1–57 months) were included. Six-month PFS was 65% (95% CI: 46–92%) and 6-month OS was 82% (95% CI: 66–100%). Regarding best objective response, disease control was found in 53% (95% CI: 28–77%); with an objective response rate of 24% (95% CI: 7–50%). In terms of safety, two patients developed grade 3 anemia, while one patient experienced local necrosis as a result of peripheral embolism, a complication related to angiographic intervention.

Conclusion:

In a treatment-refractory meningioma cohort, intra-arterial administration of [177Lu]Lu-DOTATATE is safe and effective, with an objective response rate of 24%, and survival data that exceed published benchmarks. Prospective controlled studies with larger cohorts and extended follow-up are needed, comparing intra-arterial [177Lu]Lu-DOTATATE to (historic) cohorts receiving intravenous administration are needed.

2025-12-01·NUCLEAR MEDICINE COMMUNICATIONS

Feasibility of real-time monitoring for administered activity during Lu-177 infusion by imaging the administration site using a pinhole gamma camera: a Monte Carlo study

Article

作者: Nishii, Ryuichi ; Fujita, Naotoshi ; Miwa, Kenta ; Nakanishi, Kohei ; Yamamoto, Seiichi

Objectives:

Using personalized treatment with Lu-177-labeled radiopharmaceuticals, rather than using a fixed activity of 7.4 GBq, the administered radioactivity is adjusted in each patient. Achieving precise control of the administered activity would be possible during Lu-177 infusion if real-time monitoring techniques were possible. However, these techniques are not currently available. In this study, we used Monte Carlo simulations to simulate imaging of the administration site in an arm phantom with a pinhole gamma camera to explore the feasibility of achieving real-time monitoring and control of the administered activity during infusion.

Methods:

We used the Geant4 toolkit to simulate a compact gamma camera. We simulated the basic performance of the camera within an energy window of 208 keV ± 10% and the imaging of an arm phantom to evaluate the feasibility of visualizing and quantifying the inflow of Lu-177-labeled radiopharmaceutical activity.

Results:

The spatial resolution with the 1.0-mm pinhole collimator for Lu-177 was 1.8 mm full width at half maximum (FWHM) at 50 mm, whereas it was 1.2 mm FWHM for the 0.5-mm pinhole collimator. Our gamma camera captured the activity of Lu-177 in a 3.0-mm diameter vessel within the arm phantom, achieving measurements in only 1 min. The maximum values among the mean estimation errors of the administered activity were 0.73% and −3.53% for the 1.0 and 0.5-mm pinhole collimators, respectively, both occurring within the initial 1 min.

Conclusion:

Monte Carlo simulations demonstrated the feasibility of real-time monitoring of administered activity during Lu-177 infusion by imaging the administration site with our pinhole gamma camera.

2025-12-01·Journal of Gastrointestinal Cancer

Mixed Neuroendocrine and Non-neuroendocrine Tumor of Pancreato-Biliary Origin Treated Successfully with Peptide Receptor Radionuclide Therapy

Article

作者: Luong, Tu Vinh ; Navalkissoor, Shaunak ; Krell, Daniel ; Paterson, Anna ; Caplin, Martyn ; Shekhda, Kalyan Mansukhbhai

PURPOSE:

Mixed neuroendocrine and non-neuroendocrine neoplasms (MiNENs) are rare neoplasms composed of morphologically distinguishable neuroendocrine (NE) and non-neuroendocrine components, each representing at least 30% of the tumor volume. The NE component must be substantiated by immunohistochemistry. MiNENs generally have a poor prognosis, with a more aggressive component dictating overall survival and prognosis. Owing to its rarity, there are no specific validated treatment guidelines available for these tumors, and they are generally treated with surgery if possible. However, surgically unresectable or advanced tumors are generally treated with chemotherapy.

METHODS:

We report a case of an elderly woman who was referred to the neuroendocrine tumor (NET) unit following incidental findings of liver lesions found on cardiac magnetic resonance imaging (MRI) performed for an asymptomatic heart murmur. Histology from the liver biopsy revealed MiNEN with up to 60% grade 2 (Ki67: 19%) well-differentiated NET and up to 30% well-differentiated to moderately differentiated adenocarcinoma of possible pancreato-biliary origin; intrahepatic ductal primary could not be excluded. Her 18-fluoro-deoxyglucose positron emission tomography (FDG-PET) revealed no FDG-avid lesions, and a ⁶⁸Gallium 1,4,7,10-tetraazacyclododecane-tetraacetic acid Tyr3-octreotate (⁶⁸ Ga-DOTATATE)-PET scan revealed multiple areas of intensely DOTATATE-avid liver lesions. Due to the absence of any primary imaging findings, the patient was diagnosed with MiNEN of possible pancreato-biliary origin.

RESULTS:

She was started on lanreotide 120 mg every 28 days for 6 months, with no response to the treatment. Subsequently, the patient was treated with four cycles of ¹⁷⁷Lutetium-DOTATATE (Lutathera®) peptide receptor radionuclide therapy (PRRT). She tolerated the treatment well, with no significant side effects. MRI at the end of treatment revealed a partial response to treatment.

CONCLUSION:

PRRT is currently not used in treatment protocols for the management of MiNENs; however, it could be considered a treatment option in patients with MiNENs, where there is a predominant component of well-differentiated NETs with ⁶⁸ Ga-DOTATATE avid lesions.

667

项与 (177镥)镥氧奥曲肽相关的新闻（医药）

2025-11-13

·百度百家

医药融资降温，巨头反向豪赌，这三大领域即将爆发

B轮死的魔咒还在生物医药圈游荡，听起来一片哀嚎，2025年第二季度全球生物医药一级市场融资事件数直接掉了四成多，融资总额也缩水了近三成。可真正的猎手，嗅觉总是格外灵敏，他们早就将子弹射向了那些能穿越周期的硬核地带。当所有人的目光还聚焦在诺和诺德和礼来两家公司瓜分了近97%的减重市场时，一些更深层的故事正在悄然上演。司美格鲁肽和替尔泊肽确实是现象级的，但如果你认为这就是医药创新的全部，那可就看偏了方向。真正的风暴，往往在更安静的深水区酝酿。比如肿瘤领域，过去那种追求重磅炸弹药物，一个药吃遍天的时代，正在慢慢褪去。现在，大型药企更痴迷于构建技术平台，这背后是赤裸裸的现实考量——专利悬崖的威胁迫在眉睫。与其押注单一的药物，不如掌握一个能不断孵化新产品的技术平台。这就像是，比起买一条鱼，不如直接建一个渔场。诺华就是个聪明的玩家，从2017年就开始收购布局，硬是把自己打造成了核药领域的领头羊，它那套诊断-治疗一体化的生态，让Lutathera和Pluvicto两款核药卖得风生水起。2025年上半年，Pluvicto的销售额就达到了8.25亿美元，同比增长了26%。这个逻辑延伸下去，AI驱动的药物发现平台自然就成了香饽饽。毕竟，能大幅缩短研发周期，降低成本的诱惑谁能抵挡？2025年，默克甩出3.49亿美元与Variational AI合作，而晶泰科技更是与DoveTree达成了高达59.9亿美元的超级合作，这种动辄数亿甚至数十亿美元的交易，清晰地表明了资本的态度。技术，尤其是平台型技术，才是穿越周期的硬通货。同样的故事也在自身免疫领域发生。这个仅次于肿瘤的第二大市场，规模将在2030年达到1767亿美元，市场的支付能力早已被验证。看看2024年全球十大畅销药榜单，自免药物就占了三席，数量上甚至超过了肿瘤药。赛诺菲的度普利尤单抗、艾伯维的利生奇珠单抗，都是年入百亿美元级别的存在。在这里，最热门的技术趋势叫T细胞衔接器，简称TCE。这东西听着复杂，说白了，就是给人体自身的免疫T细胞装上了一个精准的导航和武器，一头锁定致病的B细胞，另一头激活T细胞去清除它们。相比传统药物那种好坏通杀的免疫抑制，TCE要精准得多；相比流程复杂、价格昂贵的CAR-T疗法，TCE又是现成的药物，成本低，更容易普及。这种巨大的治疗潜力，自然引来了巨头们的争相布局。2025年6月，和铂医药就将其一款TCE授权给了日本大冢制药。资本的逻辑也很清晰，在靶点创新、形式优化和适应症拓展三个方向上持续深化。目前TCE的靶点还比较集中，但未来一定会向更多新靶点拓展。药物形式也在从双抗向三抗甚至多抗演进，目的就是为了提升疗效，克服耐药性。现在，我们再回头看GLP-1减重药，就能发现另一番景象。在诺和诺德与礼来的垄断下，新的入局者不再去硬碰硬，而是转向了差异化创新。口服制剂、超长效技术、多靶点药物、组合疗法，每一个细分方向都可能诞生新的机会。礼来的口服小分子药物Orforglipron进展最快，预计今年年底就能提交上市申请。而安进的Maridebart cafraglutide则把给药周期延长到了每月一次，二期数据显示其减重效果依然出色。更有意思的是组合疗法。GLP-1类药物减重的同时，往往伴随着肌肉流失，这显然不是理想状态。于是，联用能够保留甚至增加瘦体重的药物就成了新的研发方向。礼来通过收购Versanis获得了Bimagrumab这款单抗，其与GLP-1联用的临床试验正在进行中。这已经不是单纯追求体重下降了，而是追求更高质量的减脂增肌。你看，无论是肿瘤领域的平台化，自免领域的精准免疫，还是GLP-1领域的差异化创新，它们共同指向了一个事实：热闹是表面的，门道在深处。当大众还在为一个个神药惊叹时，资本和真正的玩家早已将目光投向了更底层的技术逻辑和更长远的未来布局。喧嚣是司美格鲁肽们的，但未来，可能属于那些在寂静中瞄准靶心的人。

免疫疗法细胞疗法并购

2025-11-12

·药明康德

同行致远 | 已有数款获批上市，这类新兴靶向疗法展现治疗潜力 | Bilingual

编者按：多肽偶联药物（peptide-drug conjugates，PDCs）作为新一代极具潜力的靶向治疗药物类型，将肽类分子的高精确性与小分子药物的强效活性进行结合。通过提升靶向递送能力并增强治疗效果，PDCs在肿瘤、感染性疾病及代谢性疾病等多个领域展现治疗潜力。然而，由于其结构复杂，对稳定性、可扩展性及质量控制提出了更高要求，也意味着PDCs的开发需要专业技术与先进平台的有力支撑。为应对这些挑战，药明康德旗下WuXi TIDES一体化CRDMO平台，凭借在多肽合成、小分子化学及偶联技术领域的深厚积累，可为全球合作伙伴提供覆盖从早期研究到商业化生产的全流程一站式解决方案。多肽偶联药物是精准肿瘤治疗领域中极具前景的创新药物类型之一。PDCs与抗体偶联药物（ADCs）基于相同原理，即通过靶向载体递送细胞毒性药物。不同之处在于，PDCs采用短小、可合成的肽链替代大型抗体。这些细胞靶向肽（CTPs）分子量仅为数千道尔顿，赋予PDCs卓越的组织穿透力、低免疫原性及高度设计灵活性。此外，PDCs通过肾脏途径代谢清除，从而减轻系统性负担。其小巧且具构象可塑性的结构还能引入非天然氨基酸、环状结构及多种化学修饰，进一步提升稳定性和靶向特异性。因此，PDCs正逐步成为靶向治疗领域中发展迅速、潜力突出的新型治疗模式。每一个PDC的核心都由三个相互依存的关键部分组成，共同协作以扩大药物的治疗窗口。首先是细胞靶向肽，可通过纳摩尔级亲和力识别疾病细胞上高表达的受体，常采用环状或缚合（stapled）结构，以维持二级结构并增强结合力，如针对整合素的RGD基序及针对CD13的NGR序列。其次是连接子（linker），决定药物释放的时间与位置。连接子可设计为可裂解型（对pH、谷胱甘肽或肿瘤相关酶敏感）或不可裂解型（依赖载体的胞内降解释放药物-连接子复合物）。最后是细胞毒性有效载荷，如多柔比星（doxorubicin）、紫杉醇（paclitaxel）或mertansine等。这些药物通过偶联可改善药代动力学、循环稳定性与肿瘤选择性，同时保持强效活性。PDCs的模块化结构从分子识别、可控释放到精准杀伤，形成了高效且清晰的药物递送路径。目前，已有数款治疗用PDC疗法获全球监管机构批准。Lutathera（Lutetium Lu-177 Dotatate）结合了生长抑素受体靶向肽与β射线放射性核素Lu-177，用于治疗生长抑素受体阳性的胃肠胰神经内分泌肿瘤（GEP-NETs），可实现局部放射治疗，并在安全可控的前提下维持持久疗效。Pepaxto（melphalan flufenamide）是一种肽偶联烷化剂，旨在靶向复发/难治性多发性骨髓瘤中升高的氨基肽酶活性。进入细胞后，经酶切反应释放melphalan，在恶性浆细胞内发挥杀伤作用。这些疗法的成功上市，验证了PDCs作为临床可行新型药物形式的潜力。随着研究的不断深入和合成技术的日趋成熟，PDCs有望在肿瘤、代谢性疾病及感染性疾病等多个领域拓展其临床应用。由于PDCs兼具肽与小分子药物的双重特性，其复杂的结构对药物研发生产能力提出了更高要求。依托全面的多肽技术平台与小分子化学能力，药明康德的WuXi TIDES平台可为多肽偶联药物的项目提供一站式解决方案，涵盖从发现合成、工艺开发到生产的一体化支持。展望未来，作为值得信赖的合作伙伴，药明康德将持续赋能全球肽类药物创新，助力客户加速研发进程，更快将高质量的创新药物带给患者，早日实现“让天下没有难做的药，难治的病”的愿景。 Peptide-Drug Conjugates: A New Frontier in Targeted Therapy Peptide-drug conjugates (PDCs) represent a promising new generation of targeted therapeutics that combine the precision of peptides with the potency of small molecules. By enhancing selective delivery and improving therapeutic efficacy, PDCs are showing strong promise across oncology, infectious diseases, and metabolic disorders. At the same time, their intricate architectures demand specialized expertise and advanced technology to ensure stability, scalability, and quality throughout development. Addressing these needs, WuXi TIDES, part of WuXi AppTec, has established an integrated CRDMO platform dedicated to peptide therapeutics. Leveraging deep expertise in peptide synthesis, small-molecule chemistry, and conjugation technologies, the platform delivers comprehensive end-to-end solutions for peptide conjugate discovery, development, and manufacturing, supporting partners from early research to commercial production. Peptide-drug conjugates are emerging as one of the most promising modalities in precision oncology. Built upon the same fundamental principle as antibody-drug conjugates (ADCs), PDCs distinguish themselves by using short, synthetically designed peptides in place of large antibodies. These cell-targeting peptides (CTPs), typically only a few kilodaltons in size, endow PDCs with remarkable tissue penetration, low immunogenicity, and high design flexibility. In addition, PDCs are cleared through renal pathways, minimizing systemic burden. Their small, conformationally adaptable structures also allow incorporation of non-natural amino acids, cyclic motifs, and chemical modifications that enhance stability and targeting selectivity. As a result, PDCs represent a fast-advancing platform in the landscape of targeted therapeutics. At the core of every PDC are three interdependent parts that work together to widen the therapeutic window versus the free drug: a cell-targeting peptide that recognizes receptors enriched on diseased cells with nanomolar affinity, often in cyclic or stapled formats that preserve secondary structure and strengthen binding (e.g., RGD motifs for integrins, NGR for CD13); a linker that governs when and where the payload is released, using cleavable chemistries responsive to pH, glutathione, or tumor-associated enzymes, or non-cleavable designs that rely on intracellular degradation of the carrier to liberate an active drug-linker complex; and a cytotoxic payload—such as doxorubicin, paclitaxel, or mertansine—whose conjugation improves pharmacokinetics, circulation stability, and tumor selectivity without sacrificing potency. This modular architecture creates a clear progression from molecular recognition to controlled release and, ultimately, targeted cell killing. To date, there are a few PDC therapeutics approved by global regulatory agencies. Lutathera (Lutetium Lu-177 Dotatate) couples a somatostatin-targeting peptide with the beta-emitting radionuclide Lu-177 to treat somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors, delivering localized radiotherapy and achieving durable disease control with a manageable safety profile typical of radioligand approaches. Pepaxto (melphalan flufenamide) is a peptide-conjugated alkylator designed to target elevated aminopeptidase activity in relapsed/refractory multiple myeloma; once internalized, enzymatic cleavage releases melphalan and exerts cytotoxic effects inside malignant plasma cells. These approvals demonstrate the PDCs' potential as a feasible new modality to benefit patients in clinics. As research advances and synthetic technologies mature, PDCs are poised to broaden their clinical applications across oncology, metabolic, and infectious diseases. Because PDCs integrate peptide targeting and cytotoxic payloads, their complex structures demand specialized development capabilities. Leveraging a comprehensive peptide platform integrated with small-molecule chemistry, WuXi TIDES provides a one-stop solution—spanning discovery synthesis, process development, and manufacturing—for peptide-conjugate discovery projects. As a trusted global partner, WuXi AppTec continues to empower innovation across peptide therapeutics. By enabling partners worldwide to accelerate development and bring high-quality candidates to patients faster, the company advances the vision that “every drug can be made and every disease can be treated.” 参考资料： [1] Xiao W, Jiang W, Chen Z, Huang Y, Mao J, Zheng W, Hu Y, Shi J. Advance in peptide-based drug development: delivery platforms, therapeutics and vaccines. Signal Transduct Target Ther. 2025 Mar 5;10(1):74. doi: 10.1038/s41392-024-02107-5. PMID: 40038239; PMCID: PMC11880366. [2] Peptide-Drug Conjugate Services. Retrieved October 16, 2025 from https://labtesting.wuxiapptec.com/peptide-drug-conjugate-services/ [3] Peptide Conjugate Discovery. Retrieved October 18, 2025 from https://tides.wuxiapptec.com/services-solutions/peptide/discovery/peptide-conjugate/ 免责声明：本文仅作信息交流之目的，文中观点不代表药明康德立场，亦不代表药明康德支持或反对文中观点。本文也不是治疗方案推荐。如需获得治疗方案指导，请前往正规医院就诊。版权说明：欢迎个人转发至朋友圈，谢绝媒体或机构未经授权以任何形式转载至其他平台。转载授权请在「药明康德」微信公众号回复“转载”，获取转载须知。分享，点赞，在看，聚焦全球生物医药健康创新

2025-11-11

·赛柏蓝

医药领域，这些潜力赛道即将爆发！

作者 | 草履虫编辑 | 郑瑶据公开资料，2025年第二季度，全球生物医药行业一级市场融资事件数同比下降41.1%，融资总额同比下降28.3%，不少明星项目也陷入“B轮死”的尴尬。然而，真正的猎手善于在寂静中寻找机会，将子弹射向那些能穿越周期、定义未来的硬核地带。 01肿瘤：放弃重磅炸弹，聚焦技术平台 2025年，推动药企收购或BD交易的动因已从追求短期收入增长的“重磅炸弹”药物，转向构建长期技术能力的平台型资产。这一转变背后的原因显而易见。一方面，大型药企需要抵御即将到来的专利悬崖风险；另一方面，监管机构日益认可那些具备灵活性与可扩展性的技术平台——这类平台更适用于联合疗法开发及适应性临床试验设计。与传统单一资产开发相比，技术平台具有“一对多”优势。多特异性支架、ADC连接子、RNA引导递送及降解剂化学等技术，能够为产品线注入可衍生出多个研发项目的潜力。诺华自2017年起通过收购Advanced Accelerator Applications和Endocyte等企业，快速建立核药领先地位，打造“诊断-治疗”一体化生态。2024年5月，其以10亿美元预付款收购Mariana Oncology，进一步强化布局。目前，诺华多款核药已实现商业化突破，Lutathera 2024年全球销售额达7.24亿美元，并已在中国提交临床申请；Pluvicto在2025年上半年销售额达8.25亿美元，同比增长26%。平台化策略正在成为应对专利悬崖的利器。其中，大幅缩短药物发现周期，降低研发成本的AI驱动药物发现平台备受青睐。 2025年，默克宣布与加拿大AI制药公司Variational AI达成协议，潜在交易总价值达3.49亿美元，默克将利用其AI药物发现平台设计和优化针对两个未公开靶点的小分子候选药物。 2025年，晶泰科技与DoveTree达成一项高达59.9亿美元的超级合作，专注于发现和开发新型小分子药物，该合作直接推动了公司2025年上半年的业绩爆发，彰显了AI驱动药物发现平台的巨大商业潜力。此外，精准靶向技术是另一个资本重点布局领域。放射性配体疗法（RLT）作为精准靶向的代表，正迎来快速发展期。一篇发表在Nature Reviews Drug Discovery上的文章显示，目前全球有超过60个RLT管线处于临床开发阶段（图1）。图1.临床阶段放射配体疗法中使用的放射性同位素；图片来源：Nature Reviews Drug Discovery 下一代RLT技术正在向多元化方向发展。在放射性同位素方面，除了已广泛应用的Lu-177外，Actinium-225和Lead-212等新型同位素显示出更好的疗效和安全性（图1）。在靶向配体方面，工程蛋白和抗体衍生物正在超越传统抗体，实现更好的肿瘤靶向性。值得注意的是，2025年，跨境并购成为肿瘤领域的显著特征，跨境合作能够利用不同市场间的估值差异实现战略收益。同时，通过获取不同地区的监管经验和市场入口，并加速全球同步申报的进程。德国BioNTech公司收购中国的普米斯生物与德国的CureVac公司、阿斯利康收购瑞士的EsoBiotec公司、大鹏药品收购Araris Biotech AG公司，每一笔交易都凸显出全球药企正积极布局，以获取临床试验渠道、生产基地以及区域性监管等优势，同时也反映了市场对跨境技术整合的高度认可。 02自免：新靶点、新形式、新适应症多线推进自免市场是仅次于肿瘤的第二大市场。据Frost & Sullivan数据统计，2022年全球自免市场规模为1323亿美元，到2030年，全球自免市场将达1767亿美元，其中生物药市场为1450亿美元，占比高达82.1%。图2.自免市场规模（亿美元）及增速（%）；图片来源：华创证券研报市场的支付能力已经过验证，在2024年全球十大畅销药中，自免药物占据三席，数量上超过了肿瘤药物。赛诺菲的度普利尤单抗、艾伯维的利生奇珠单抗和强生的乌司奴单抗，这三款“百亿美元俱乐部”成员，共同勾勒出一个高价值、高增长且需求持续旺盛的市场轮廓。当前，自免领域最引人注目的技术趋势是T细胞衔接器（TCE）的崛起。其通过“双靶点桥接”，一端靶向B细胞表面抗原，另一端结合T细胞表面的CD3分子，精准激活人体自身免疫系统来清除致病细胞。相较于传统药物无差别地抑制免疫系统，TCE能更精确地靶向异常活化的B细胞；与依赖毒性载荷的ADC药物相比，TCE依靠激活T细胞，理论上具有更好的安全性；相比流程复杂、价格高昂的CAR-T疗法，TCE作为一种现货型药物，成本更低，更易于推广。巨大的治疗潜力使TCE成为MNC争相布局的战略要地。2025年6月，和铂医药将其BCMAxCD3双特异性TCEHBM7020授权给日本大冢制药，HBM7020具备非对称结构，能够有效解决轻链错配挑战，展现出了良好的安全性与成药性。 2024年11月，维立志博与风险投资公司Aditum Bio宣布成立新药研发公司 Oblenio Bio，维立志博将其CD19/BCMA/CD3三特异性TCE LBL-051授权给OblenioBio，共同推进项目开发。另外，为构建长期竞争力并规避同质化风险，资本在自免领域的布局正沿着靶点创新、形式优化、适应症拓展三个方向深化。当前TCE的靶点主要集中在CD19、BCMA等成熟靶点上，未来的突破有赖于向新靶点拓展，借鉴CAR-T疗法在肿瘤领域的经验，CD22、BAFF-R等靶点也具备向自免领域转化的潜力。此外，药物形式正超越传统的双抗，向三抗甚至多抗TCE演进，以期通过多靶点协同提升疗效并克服耐药性。嘉和生物将其CD3/CD20双抗GB261授权给TRC，其“非对称”结构设计是通过降低CD3端亲和力，减少细胞因子风暴（CRS）发生率，同时保留抗体依赖的细胞介导的细胞毒作用；与此同时，自免药物的研发不再局限于类风湿关节炎、银屑病等传统领域，正迅速覆盖更多未被满足的临床需求。科伦博泰与和铂医药将联合开发的TSLP抗体HBM9378授权给Windward，用于治疗哮喘和慢性阻塞性肺疾病（COPD），通过拓展呼吸系统等新的自免疾病领域来挖掘市场潜力，交易金额达9.7亿美元。 03GLP-1：挖掘细分领域，追求差异化创新目前，减重市场已形成诺和诺德与礼来双巨头垄断格局，市占率接近97%。投资人正将目光从同质化竞争转向差异化创新，聚焦于口服制剂、超长效技术、多靶点药物、组合疗法及适应症拓展等细分方向（图4）。提高患者用药便利性与依从性，是GLP-1药物迭代的重要方向。目前，主流研发聚焦于“口服制剂”与“超长效制剂”。口服GLP-1药物主要包括小分子与多肽两类。礼来的Orforglipron在全球口服小分子中进展最快，预计今年年底递交上市申请（图3），国内企业如恒瑞医药、华东医药、闻泰科技等也在该领域积极布局，部分管线已进入临床中后期，展现出较强的出海潜力。图3.主要GLP-1小分子专利结构；图片来源：华泰证券研报在长效化方面，司美格鲁肽与替尔泊肽已实现每周给药，而下一代”超长效制剂”则致力于将给药周期延长至每两周甚至每月一次。安进的Maridebart cafraglutide（MarITide）作为每月一次给药的GLP-1/GIP双靶点药物，二期数据显示其52周减重效果可达约20%，且安全性良好。此外，随着市场对减重效果要求的提升，单一GLP-1靶点已难以满足“高质量减重”的需求。“多靶点激动剂”通过协同激活或抑制多个代谢相关受体，实现“抑制食欲+加速代谢+器官保护”的协同机制，在减重效果与代谢综合改善方面显著优于单靶点药物。图4.MNC下一代减重药物管线布局；图片来源：开源证券研报礼来的替尔泊肽（GLP-1/GIP）与Retatrutide（GLP-1/GIP/GCGR）、信达生物的玛仕度肽（GLP-1/GCGR）等是其中的代表。此外，GLP-1与FGF21的联用也在探索用于改善血脂异常和治疗MASH等适应症，华东医药的GLP-1/GCGR/FGF21三靶点药物DR10624即为FIC布局。 “组合疗法”是另一大创新方向，旨在实现“减脂增肌+代谢修复”。GLP-1类药物在减重的同时常伴随肌肉流失，而联用ActRII（激活素受体II）或MSTN（肌肉生长抑制素）靶点药物，有望在减重的同时保留甚至增加瘦体重。礼来通过收购Versanis获得了ActRIIA/B单抗Bimagrumab，其与GLP-1联用的临床试验正在进行中。国内来凯医药在ActRII靶点布局领先，其LAE102已进入临床阶段。此外，GLP-1与胰淀素（AMYR）类似物或外周限制性CB1拮抗剂的联用，也在探索增强疗效与改善安全性的潜力。 04结语在肿瘤、自免与GLP-1的深水区，技术平台、精准免疫与差异化疗法正悄然重塑全球医药领域未来。参考资料： [1] https://www.nature.com/articles/d41573-025-00096-w [2]华创证券研报、华泰证券研报、开源证券研报 [3]各企业官网及各种公开资料等 END 内容沟通：Xinmeitizhongxin- 商务合作：13810647732

并购抗体药物偶联物放射疗法

100 项与 (177镥)镥氧奥曲肽相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	V10XX04	DB13985

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
生长抑素受体阳性神经内分泌肿瘤	日本	Novartis Pharma KK	2021-06-23
生长抑素受体阳性神经内分泌肿瘤	日本	FUJIFILM Toyama Chemical Co., Ltd.	2021-06-23
SSTR阳性胃肠胰神经内分泌肿瘤	欧盟	Advanced Accelerator Applications SA	2017-09-26
SSTR阳性胃肠胰神经内分泌肿瘤	冰岛	Advanced Accelerator Applications SA	2017-09-26
SSTR阳性胃肠胰神经内分泌肿瘤	列支敦士登	Advanced Accelerator Applications SA	2017-09-26
SSTR阳性胃肠胰神经内分泌肿瘤	挪威	Advanced Accelerator Applications SA	2017-09-26

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
胃肠胰神经内分泌肿瘤	申请上市	美国	Curium Pharma UK Ltd.	2024-07-09
晚期神经内分泌肿瘤	临床3期	中国	北京先通国际医药科技股份有限公司	2024-06-11
神经内分泌癌	临床3期	中国	北京先通国际医药科技股份有限公司	2024-06-11
神经内分泌肿瘤	临床3期	中国	北京先通国际医药科技股份有限公司	2024-06-11
晚期胰腺神经内分泌肿瘤	临床3期	中国	江苏恒瑞医药股份有限公司	2023-07-06
大肠类癌	临床3期	美国	Advanced Accelerator Applications SA	2012-09-06
大肠类癌	临床3期	比利时	Advanced Accelerator Applications SA	2012-09-06
大肠类癌	临床3期	法国	Advanced Accelerator Applications SA	2012-09-06
大肠类癌	临床3期	德国	Advanced Accelerator Applications SA	2012-09-06
大肠类癌	临床3期	意大利	Advanced Accelerator Applications SA	2012-09-06

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临床结果

适应症

分期

评价

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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


NCT05459844 (XT-XTR008-3-01, Ann Oncol) 人工标引	临床3期	胃肠胰神经内分泌肿瘤	196	XTR008 four cycles every 8 weeks	範衊襯齋觸簾鑰鹹醖窪(簾衊衊鑰衊鹽積淵淵艱) = 觸積鑰選範範選廠築廠餘膚窪鬱醖簾構願網窪 (鹽選鑰獵壓醖衊遞鹽願, 16.13 ~ NE) 更多	积极	2025-10-18
				Octreotide 60 mg every 4 weeks	範衊襯齋觸簾鑰鹹醖窪(簾衊衊鑰衊鹽積淵淵艱) = 選積範觸鏇遞鏇積衊糧餘膚窪鬱醖簾構願網窪 (鹽選鑰獵壓醖衊遞鹽願, 5.65 ~ 8.41) 更多
NCT05459844 (XT-XTR008-3-01, ESMO2025)	临床3期	神经内分泌肿瘤	196	XTR008 (7.4 GBq q8w×4)	網獵淵膚廠選糧網選積(積鹽窪衊夢積觸壓構醖) = 廠鏇憲遞顧鏇鏇積憲廠廠襯繭襯觸餘襯膚糧遞 (廠網願構觸築蓋顧觸網, 22.14 ~ NE) 更多	积极	2025-10-17
				LAR (60 mg q4w)	網獵淵膚廠選糧網選積(積鹽窪衊夢積觸壓構醖) = 鬱廠醖範繭窪獵窪餘夢廠襯繭襯觸餘襯膚糧遞 (廠網願構觸築蓋顧觸網, 5.65 ~ 8.41) 更多
JPRN-UMIN000054127 (ESMO2025)	N/A	神经内分泌肿瘤	383	Lu-DOTATATE	鹹積構艱廠襯餘醖壓獵(淵鏇艱觸醖選範鏇膚壓) = 餘簾齋憲憲淵憲製鑰襯構構窪襯蓋願鹹膚製鬱 (遞簾構網餘鏇齋鏇襯製 ) 更多	积极	2025-10-17
ASCO2025	N/A	嗅神经母细胞瘤一线 \| 二线 somatostatin receptor (SSTR)	-	177Lu-dotatate	夢獵糧窪鑰餘窪觸齋遞(鹽憲範齋顧範夢蓋網窪) = 夢衊蓋艱餘選膚衊繭積遞願廠簾壓淵糧淵夢簾 (願壓衊鑰製繭餘願築夢, 8.29 ~ NE)	积极	2025-05-30
NCT03972488 (NETTER-2, CTgov)	临床3期	胃肠胰神经内分泌肿瘤	226	Sandostatin LAR+Lys-Arg+Octreotide long acting repeatable+Lutathera (Lutathera® Plus Octreotide LAR 30 mg (Investigational Arm))	糧遞夢積壓鑰簾顧獵憲(廠鑰願築齋鬱夢齋膚顧) = 顧鬱觸蓋醖襯遞願鹹觸簾齋製積淵製製醖蓋積 (壓選觸餘憲廠齋膚鏇獵, 繭願膚積範鹹積淵範網 ~ 窪鬱網鹹觸觸醖襯鑰糧) 更多	-	2024-10-10
				octreotide (Octreotide LAR 60 mg (Control Arm))	糧遞夢積壓鑰簾顧獵憲(廠鑰願築齋鬱夢齋膚顧) = 願鑰鹹壓窪築簾淵積鑰簾齋製積淵製製醖蓋積 (壓選觸餘憲廠齋膚鏇獵, 夢範遞衊壓鬱糧鬱夢窪 ~ 範廠製憲鹽構鏇顧壓構) 更多
NCT02743741 (OZM-067, ASTRO2024)	N/A	-	33	177Lu-DOTATATE	窪構艱艱鏇廠蓋壓夢襯(鏇鹹壓繭壓壓選鬱繭壓) = 齋壓選繭鬱夢獵鑰願構觸簾顧衊顧齋鏇餘鏇鑰 (積窪選製膚壓壓壓鏇醖, 0.87) 更多	积极	2024-10-01
				68Ga-DOTATATE	窪構艱艱鏇廠蓋壓夢襯(鏇鹹壓繭壓壓選鬱繭壓) = 淵鏇襯鏇糧範製鑰顧鬱觸簾顧衊顧齋鏇餘鏇鑰 (積窪選製膚壓壓壓鏇醖, 0.87) 更多
ASTRO2024	临床2期	神经内分泌肿瘤	195	177 Lu-DOTATATE (177Lu-D >880 mCi)	觸鏇願鑰鹽鏇艱衊構蓋(遞壓憲築積憲網鹹積鏇) = 膚網獵醖蓋鏇憲選選齋鹽齋憲繭獵簾襯淵憲願 (艱鑰鏇鹽艱構醖繭醖顧, 90 ~ 100) 更多	不佳	2024-10-01
				177 Lu-DOTATATE (177Lu-D 800 Â± 10%)	觸鏇願鑰鹽鏇艱衊構蓋(遞壓憲築積憲網鹹積鏇) = 願積網鏇鹹鑰窪淵糧艱鹽齋憲繭獵簾襯淵憲願 (艱鑰鏇鹽艱構醖繭醖顧, 73 ~ 100) 更多
ASTRO2024	N/A	胃肠胰神经内分泌肿瘤	-	<sup>177</sup>Lu-DOTATATE	積膚遞壓積積襯製範窪(選構齋網衊網衊糧鹽醖) = 顧積壓醖鑰鹹範蓋築窪願繭窪壓網願壓齋淵淵 (鹹廠窪夢蓋鑰顧蓋鹽選 )	-	2024-10-01
ASTRO2024	临床2期	脑膜瘤 somatostatin receptors	20	177Lu-Dotatate 7.4 GBq	醖製壓觸膚鬱鏇艱選蓋(淵醖構鬱製襯醖簾鹽壓) = 選憲醖餘繭蓋夢廠製蓋憲鬱襯鑰餘遞築鏇願襯 (憲夢築憲齋壓積繭壓憲, 52 ~ 94) 更多	积极	2024-10-01
Biospace 人工标引	临床2期	脑膜瘤	20	Lutathera	願構築糧糧觸鬱夢獵範(醖觸窪餘憲壓鑰窪衊鬱) = 蓋蓋積鹹齋鹹願遞艱窪網糧膚齋製餘製顧構獵 (鬱構築範鏇衊選醖鏇衊 ) 更多	积极	2024-09-30