The goal of this research is to determine if DetectnetTM PET/CT can be used to make Lutathera therapy safer for patients with neuroendocrine cancer.
Participants will:
* Complete two phases involving 6 visits
* Undergo additional research PET/CT, and possibly SPECT/CT scans

开始日期2025-03-07

申办/合作机构

University of Wisconsin Madison

NCT04529044

/ Not yet recruiting临床2期IIT

A Phase II Pilot Study of (Lutetium (177Lu)-DOTATATE in Patients with Metastatic Breast Cancer

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2025-01-01

申办/合作机构

OHSU Knight Cancer Institute

[+3]

NCT06663072

/ Recruiting临床1期IIT

A Phase I Study of Fulvestrant in Combination With Lu-DOTATATE for Advanced Pancreatic Neuroendocrine Tumors

This is a phase I, open-label study to assess the safety and preliminary efficacy of Fulvestrant in combination with 177Lu-DOTATATE for advanced pNETs.

开始日期2024-12-13

申办/合作机构

The University of Chicago

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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953

项与 (177镥)镥氧奥曲肽相关的文献（医药）

2025-04-16·BIOCONJUGATE CHEMISTRY

Choice of an Optimal Modular Strategy for the Synthesis of DOTA-Containing Heterobivalent Agents Targeting PSMA and GRPr

Article

作者: Orlov, Grigory A. ; Prach, Anastasia ; Plotnikov, Evgenii ; Bodenko, Vitalina ; Grishin, Yuri K. ; Beloglazkina, Elena K. ; Zyk, Nikolay Y. ; Grigoriev, Gleb P. ; Roznyatovsky, Vitaly A. ; Machulkin, Aleksei E. ; Larkina, Mariia S. ; Beloglazkina, Maria A. ; Petrov, Stanislav A. ; Petrova, Juliana V. ; Yusubov, Mekhman S. ; Varvashenya, Ruslan

Heterodimeric approaches have emerged as a promising method for simultaneously targeting multiple receptors on tumor cells using a single molecule. Simultaneous targeting of the prostate-specific membrane antigen (PSMA) and the gastrin-releasing peptide receptor (GRPr) holds the potential to improve the accuracy of prostate cancer diagnosis. The aim of this study was to develop a convenient and simple modular strategy for the creation of heterobivalent (HBV) conjugates targeting PSMA/GRPr receptors. For this purpose, we developed and compared six alternative routes for the stereoselective synthesis of HBV conjugates designed to deliver the chelating agent DOTA to PSMA/GRPr receptors. The comparison of these alternative synthetic pathways took into account such factors as efficiency, complexity, synthesis, and purification details, as well as yields of the target compounds. Optimal conditions for the stereoselective synthesis of HBV ligands to PSMA and GRPr, which could serve as molecular platforms for the targeted delivery of therapeutic or diagnostic agents to these receptors, were revealed. For synthesized HBV ligand 26^x and its HBV conjugate with DOTA 27, the complete signal assignment in ¹H, ¹³C, and ¹⁵N NMR spectra was achieved using 2D NMR techniques. Based on these data, comprehensive signal assignments were provided for all final compounds in their NMR spectra. The final HBV conjugate 27 was labeled with Lu-177, with yields >99%, and the obtained radiotracer was studied in vitro for its binding specificity, with determining of the K_D and B_max using LNCaP (PSMA+) and PC-3 (GRPr+) cell lines.

2025-04-01·CANCER BIOTHERAPY AND RADIOPHARMACEUTICALS

Generalized Seizure as an Acute post-[¹⁷⁷Lu]Lu-DOTATATE Side Effect in a Case of Recurrent Meningioma

Article

作者: Yazdani, Babak ; Alipour, Abdolmajid ; Ghaedian, Tahereh ; Ghaedian, Mehrnaz ; Rakhsha, Abbas

[¹⁷⁷Lu]Lu-DOTATATE is a newly trending acceptable therapy in recurrent/residual meningioma with good safety. However, recognizing any possible side effects in this special population would be helpful for better management and individualization of this useful treatment. Although the seizure has been previously reported in a few cases after [¹⁷⁷Lu]Lu-DOTATATE therapy in recurrent meningioma, the acute onset of seizure in these patients, early after therapeutic radioligand administration, is not reported to the best of our knowledge. This report presents a case with the progression of residual meningioma after previous surgery in 2016 who developed with generalized tonic-clonic seizure, a few hours after administration of 200 mCi [¹⁷⁷Lu]Lu-DOTATATE. The patient was taking prophylactic doses of the lacosamide, although no previous history of seizure was reported.

2025-04-01·SUPPORTIVE CARE IN CANCER

Navigating care: understanding cancer patients’ experiences with systemic radionuclide therapy

Article

作者: Griessler, Erich ; Winkler, Florian ; Starkbaum, Johannes ; Thircuir, Solenn

Abstract:

Neuroendocrine tumors (NETs) are widely considered to be a rare disease, often diagnosed at a late stage due to the variety of symptoms. Systemic radionuclide therapy (SRT) with Lutathera (177Lu-Dotatate) is a promising treatment for this disease. However, little is known about patients’ experiences with this approach and the radioactivity involved. Based on seven semi-structured interviews, this qualitative study explores how cancer patients perceive their journey to SRT, and the treatment and care they receive in clinics specialized in the delivery of 177Lu-Dotatate to target tumors. The interviews were conducted in France between 2020 and 2021. Six interviews included patients receiving SRT, and one was held with a patient representative for NETs. Three key themes emerged from the analysis: challenges in accessing SRT, including geographic and institutional barriers; the psychological and social impact of radiation-related isolation; and the role of patient-centered care in fostering trust and well-being. Patients reported difficulties navigating the healthcare system, emotional distress due to isolation during treatment, and the importance of support in mitigating these challenges. These findings highlight the need for increased access to SRT, as well as of patient-centered approaches to the various challenges directly and indirectly associated with SRT.

495

项与 (177镥)镥氧奥曲肽相关的新闻（医药）

2025-04-22

·PRNewswire

SHINE Expands Global Footprint with UAE Distribution Partnership For Cancer-Fighting Isotopes

Strategic agreement with Modawina Medical Company strengthens SHINE's presence in EMEA region and advances access to Ilumira, n.c.a. lutetium 177 JANESVILLE, Wis., April 22, 2025 /PRNewswire/ -- SHINE Technologies, LLC, a nuclear fusion company with a platform of medical isotope products, today announced a strategic distribution partnership with Modawina Medical Company to bring Ilumira, SHINE's non-carrier-added lutetium-177 (n.c.a. Lu-177), to patients in the United Arab Emirates. This first-of-its-kind agreement for SHINE in the UAE extends the company's global reach and reinforces its position as a key supplier of cancer-fighting isotopes across the EMEA region. Strategic partnership to serve Middle East patients Continue Reading MMC will distribute Ilumira to its network of radiopharmaceutical manufacturers and nuclear medicine centers in the UAE. Post this Through this long-term agreement, MMC will distribute Ilumira (Lu-177) to its extensive network of radiopharmaceutical manufacturers and nuclear medicine centers in the UAE, increasing access to this important cancer-fighting isotope. Modawina Medical Company (MMC) is dedicated to equipping healthcare providers across the UAE with advanced medical technologies. Through this long-term agreement, MMC will distribute Ilumira to its extensive network of radiopharmaceutical manufacturers and nuclear medicine centers in the UAE, increasing access to this important cancer-fighting isotope. "We're proud to partner with SHINE to bring its high-quality Ilumira to healthcare providers throughout the UAE," said Ahmed Aboufaroukh, Founder and CEO of MMC. "Our mission has always been to provide cutting-edge medical solutions to the region, and this partnership allows us to address the growing demand for targeted radiotherapies that can transform cancer care." Supporting global growth in precision medicine SHINE produces Ilumira at its Cassiopeia facility in Janesville, Wisconsin, one of the highest-capacity Lu-177 production sites in North America. With the ability to support up to 100,000 doses annually, SHINE's proprietary production process ensures a reliable, high-quality supply of this important isotope, crucial given its 6.7-day half-life and need for rapid distribution. This agreement marks another step in SHINE's mission to make advanced cancer care accessible to more patients around the world. As SHINE continues to expand its global network, strategic partnerships like this one will play a vital role in strengthening the supply chain for medical isotopes and supporting the future of targeted radiopharmaceutical therapies. "The Middle East represents an exciting growth region for advanced cancer therapies, and we're proud to help lead that growth," said Greg Piefer, Founder and CEO of SHINE. "What's most exciting about expanding into the UAE with MMC, a partner with deep relationships with healthcare providers across the region, is the opportunity to deliver breakthrough cancer treatments for patients who may not have had access before." Ilumira is a critical medical isotope used in targeted cancer therapies that precisely delivers radiation to cancer cells while minimizing damage to surrounding healthy tissue. These therapies are gaining global momentum and offer powerful new options for patients with limited alternatives. Recently, the FDA expanded the approved indications for Lu-177-based radiopharmaceuticals in treating metastatic prostate cancer. About SHINE Headquartered in Janesville, Wisconsin, SHINE is an industry leader in next-generation fusion, developing innovative fusion-based technology that combines safety, cost-efficiency and environmental responsibility. SHINE has successfully commercialized fusion across multiple applications, including neutron testing markets such as neutron radiography, radiation-effects testing and fusion material research. It has commercialized and is scaling its proprietary medical isotope production processes, supplying high-quality radioisotopes essential for procedures including diagnosing heart disease and cancer as well as cancer therapy. Beyond these applications, SHINE is pioneering nuclear waste recycling to make nuclear energy more sustainable. Its long-term purpose is to change the way humans make energy by commercializing fusion energy. Unlike other fusion companies, SHINE takes a commercially driven path mirroring successful deep-tech industries. Through this visionary approach, SHINE is advancing technology, healthcare, and sustainable energy, making a lasting impact across multiple sectors. Learn more at About Modawina Medical Company Modawina Medical Company (MMC) was established in 2010 to meet the growing demands of healthcare services in the United Arab Emirates. As a trusted partner of leading global medical equipment manufacturers, MMC provides premium healthcare solutions with exceptional after-sales service. The company's comprehensive product portfolio includes advanced equipment for Radiology, Nuclear Medicine, Surgical Instruments, Medical Oncology, Laboratory and Physiotherapy used in hospitals throughout the region. A private enterprise dedicated to serving healthcare providers across the Middle East, MMC is committed to supplying superior equipment while maintaining the highest standards of patient care. The company continuously expands its product offerings to fulfill market demands, ensuring healthcare facilities have access to the best-known brands in the medical field. Through its commitment to quality and service excellence, MMC continues to support the advancement of healthcare delivery throughout the UAE and beyond. Learn more at SOURCE SHINE Technologies, LLC WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

放射疗法

2025-04-22

·创药网

【技术剖析】技术革新驱动核药产业系统性创新（一）

近年来，核药领域迎来爆发式增长。在精准医疗与诊疗一体化理念驱动下，核药创新技术加速升级，呈现出"核素迭代、靶标拓展、平台创新"等创新趋势。新型α核素药物、新功能靶向分子、智能开发平台等技术突破正重塑核药研发范式。本文概述了核药重磅交易和代表性RDC上市和在研药物，供研发人员参考。近年来，核药领域迎来爆发式增长。据统计，2024年核药市场规模达175亿美元，复合增长率13.48%，全球临床阶段核药管线超600项。在精准医疗与诊疗一体化理念驱动下，核药创新技术加速升级，呈现出"核素迭代、靶标拓展、平台创新"等创新趋势。新型α核素药物、新功能靶向分子、智能开发平台等技术突破正重塑核药研发范式。随着诺华Pluvicto在转移性去势抵抗性前列腺癌治疗中的成功，核药产业竞争焦点已从同位素选择转向系统性技术革新。一、α核素开启精准杀伤新时代靶向α治疗（Targeted Alpha Therapy，TAT）疗法是近年来核药领域的突破性方向，主要利用高能α粒子对肿瘤细胞进行精准杀伤。相比传统的β射线核素，α粒子具备更短的穿透深度和更高的线性能量转移（LET），能够在细胞层面实现高效破坏，同时降低对周围正常组织的损伤。其中，锕225（225Ac）凭借多阶段杀伤拓展难治瘤种，铅212（212Pb）以“短平快”的α治疗重塑临床范式，硼10（10B）则通过诊疗精准性开辟实体瘤新路径。创新性核素应用推动核药从“广谱杀伤”向“精准放疗2.0”升级。值得注意的是，同位素供应短缺是核药行业面临的最大挑战之一。在生产方面，现有创新技术包括原料替代，如212Pb用228Th替代铀矿，225Ac用核废料替代纯钍矿，10B开发新型前驱体；同时，使用模块化热室（212Pb）、在线辐照（225Ac）、超低温精馏（10B）等工艺革新技术；另有Telix公司构建"钍矿-分离-制剂"全链条，中核集团实现"反应堆-精馏-应用"闭环等产业协同创新流程，不断推动创新核素在核药开发中的精准诊疗应用（表1）。表1：创新α核素与传统核素对比核药的精准打击优势和技术迭代潜力持续吸引资本与产业资源（表2）。2024年2月，由诺贝尔化学奖得主Michael Welch教授创立的AlphaThera Bio宣布完成8500万美元A轮融资，致力于开发基于225Ac和镭223（223Ra）的TAT平台，并解决放射性核素稳定性和体内清除的挑战。自2023年以来，核药领军企业诺华分别与Bicycle Therapeutics、3B Pharmaceuticals、PeptiDream、Mariana Oncology等多家公司达成收购或药物开发合作，总金额近70亿美元。2024年7月，Novartis宣布与Radiomedix达成合作协议，开发TAT治疗方案，前期支付2000万美元，合作总金额超过10亿美元。2024年11月，诺华再与Ratio Therapeutics公司达成合作，共同开发针对生长抑素受体2（SSTR2）的放射性治疗药物，利用Ratio公司在放射配体治疗（RLT）发现和开发方面的专业知识及其两个专有研发平台——Trillium和Macropa，Trillium是一种药代动力学调控平台，能够针对任何特异性抗原靶标进行调控；Macropa是一种同位素225Ac螯合剂，这些平台均能够提升α粒子的肿瘤杀伤力。其中，国内药企东诚药业、远大医药等通过技术引进和合作加速国产替代。表2：近两年核药的重磅交易列举二、精准靶向及诊疗一体化1RDCRDC（Radionuclide Drug Conjugates）是一类创新的放射性药物，将精准靶向分子（单抗或多肽/小分子，Ligand）和强力杀伤因子（核素，Radioisotope）用连接臂（Linker）螯合剂（Chelator）偶联在一起而设计开发的药物形态；得益于其特殊的作用机制，RDC可实现高精度诊断及在治疗疾病的过程中具有不易耐药等优点，成为临床实操中唯一能够实现诊疗一体化的药物，也被认为是目前核药靶向治疗领域最具潜力的发展方向之一。当前，全球已获批RDC药物11个，其中9个为诊断用，2款来自诺华公司分别为针对神经内分泌瘤的Lutathrea与前列腺癌Pluvicto为治疗性用药（表3）。Pluvicto是首个靶向前列腺特异性膜抗原（PSMA）的治疗性RDC药物，通过β射线精准杀伤肿瘤细胞，2024年销售额13.92亿美元。Lutathera是全球首款治疗性RDC，针对SSTR2阳性肿瘤，Ⅲ期试验显示疾病进展风险降低79%，2024年销售额7.24亿美元。两款治疗性RDC的良好市场表现，让整个市场对核药赛道展现出强劲信心。表3：已获批RDC诊疗法当前管线中，RDC药物研发较活跃，临床前及早期临床候选药物较丰富（图1）。进入临床后期的管线中，目前已递交上市申请的RDC候选药共有8个，其中有2个治疗性RDC的上市申请进展较为艰难，131I-Omburtamab（靶向B7-H3）的上市申请经历了多次波折，目前尚未在全球主要市场获批；131I-Apamistamab（商品名Iomab-B）作为一种靶向CD45的RDC，在复发/难治性急性髓系白血病（R/R AML）治疗中展现了突破性潜力，但其上市申请因监管要求未完全获批，目前处于战略合作调整阶段。进入Ⅲ期临床的RDC药物进展较为积极的治疗性RDC有8个（表4）。以225Ac-PSMA-617、RYZ101和177Lu-Edotreotide为代表的全球首创药物具备较强的市场竞争力。图1：全球RDC研发管线布局表4：处于Ⅲ期临床的RDC药物2PRC根据靶向配体的不同，RDC可细分为抗体偶联核素药物（ARC）、小分子偶联核素药物（SMRC）和多肽偶联核素药物（PRC）。PRC利用多肽将放射性同位素靶向递送至癌细胞中，通过“靶向多肽+核素”的精准设计，结合技术创新（如环肽、诊疗一体化），在实体瘤治疗中展现出独特优势。与抗体相比，多肽在组织渗透、药代动力学性质等方面优势独特，同时多肽蛋白的特异性表达与偶联功能可以满足RDC的技术突破方向要求。此外，通过环化改造（如形成环肽）或引入非天然氨基酸，可增强多肽的抗酶解能力和靶标亲和力。美国FDA已经批准多款靶向多肽核药，如Lutathera用的多肽是Octreotide（奥曲肽），证明了基于多肽分子开发RDC的可行性。2024年5月，诺华与PeptiDream公司开展多肽发现合作，利用其独有的多肽发现平台系统（PDPS），根据诺华指定的靶标，发现和优化创新大环肽。同月，诺华以17.5亿美元收购Mariana Oncology公司，该公司聚焦开发靶向肽核药，其主导项目MC-339是一种针对小细胞肺癌的在研的新型PRC，其携带的放射性同位素为锕系元素。本文其它内容请见创药网https://www.iddds.cn

并购临床研究

2025-04-21

·抗体圈

创新药10年变天

资本寒冬，一家上市Biotech也没有挂掉。18A生物科技七年之痒，70家公司（含摘B）仍然整整齐齐，一家没少，即使市值最小的北海康成账上现金仅剩1亿元，但管理层认为2025年有足够的营运资金，即使诺辉健康复牌暂时没有进展，但离生死大限还有5个月。中国创新药处于少年时代，（在上市公司层面）有着足够的容错率和包容度，如同《百年孤独》中初创的“马孔多”，这里全是年轻人，没有死亡，自然没有墓地。然而，站在中国创新药10年节点之上，两大蜕变还是发生了。今非昔比，《创新药供给侧改革》（2021年7月）指出的内卷和泡沫，如今都不再严重。一是行业主要矛盾的蜕变，从同质化竞争的内部矛盾，转为中国生物科技快速崛起与美国维持生物科技创新领域领导地位之间的外部矛盾。二是创新模式的蜕变，大部分Biotech转向纯粹的研发型企业，以BD为导向，以早研管线为重心，而且同靶点药物争取国内前三，甚至全球前三。01 超长续航模式据青侨阳光，2024年港股18A生物科技的合计可持续业务营收达到598亿元，同比增长48%，相比2019年的44.5亿元增加超12倍，相比2021年的143亿元增加3倍以上。预计2026年，18A合计可持续业务营收将接近或超过1000亿元。但这还不是最激动人心的预期差。据Wind数据，2024年港股18A生物科技板块，70%的企业研发费用为同比下降，而且研发费用超过5亿元的仅有13家。在节衣缩食的情况下，研发管线却出现大规模的迭代重塑，创新性和差异化前所未有。这到底发生了什么？据药明生物披露的综合项目现况图，早期项目费用比后期项目低得多。本次财报季，大部分Biotech都推出更多NME（新分子实体），但财务状况却变得更好了。原因在于以BD为导向，用尽量少的钱，开发尽量多、尽量新的早研管线。中国创新药License out交易中，I期、II期临床管线的数量占比从2019年的17%升至2024年的46%。原因在于早研管线创新成色更足，有FIC、BIC潜力，在部分领域相比MNC具备技术优势，而且物美价廉。今年BD标的临床阶段更加前置。和铂医药BD的临床前分子没有公布靶点，与阿斯利康的合作是5年+5年，这可以理解为卖方市场，只要有好的分子出来，立即被MNC优先抢购。达成重磅BD交易的乐普生物ADC药物MRG007、映恩生物双抗ADC药物DB-1418/AVZO-1418、先为达生物口服胰淀素受体激动剂和皮下注射胰淀素受体激动剂均为临床前分子。遥想当年，初代Biotech辛辛苦苦把临床全流程做完，最后还要自己下场商业化，结果药物在整个生命周期的销售额可能都无法收回研发成本，少数明星药企的钱就是这样烧掉的。现在甚至都不需要把管线推进到临床，即有可能卖给海外，只要首付款超1亿美元，又可以续航3年左右。在3年期间，再找到一个BIC/FIC分子，并找到买家不是很难。原先有上市产品的Biotech压力更小，不用过于在意支付环境和销售峰值，销售额甚至都不用覆盖研发开支，只需要覆盖SG&A费用（销售、一般和行政费用），即使只有小额BD，也较容易做到现金流收支平衡。这是早研管线+BD的生态平衡，原先被认为九死一生的Biotech，找到生存之道，由此获得超长续航模式。这种短平快的打法，并非研发型Biotech专有，也是恒瑞医药、信达生物此类追求效率的综合型药企最擅长的，BIC/FIC早研管线喷薄而出，为BD提供无尽的种子。今年以来的创新药牛市，正是对这种整体改善作出的热烈反应（支付环境改善也是重要因素）。据医药魔方NextPharma数据库，2025Q1，中国创新药license-out交易已有41起，总金额369.29亿美元，仅3个月已接近2023年全年水平，已超过2024H1交易总额。2025Q1，中国创新药license-out首付款总额近9亿美元，已超过一级市场同期融资总额。据医药魔方InvestGo数据库统计，2025Q1，国内一级市场共有48起融资事件，总额50.65亿元。BD也是一种市场化调节手段，让中国创新药少走许多年的弯路。美国Biotech专注于一个核心产品，或者一种前沿技术；跨国药企会主动避免在同靶点药物上扎堆，主流竞争格局为3家左右。在国内，这一切曾经是完全颠倒的。混乱提前结束了。少数Biopharma能够把平台型、全链条架构走通，有各种难以复现的因素，大部分Biotech选择轻量化、研发型之路，以BD兑现商业价值，反而可以走出死亡螺旋。管线全球前三，BD概率更高，这也倒逼中国创新药企进行原始创新。今后最尴尬的事情是，平庸管线BD不出去，烂在手里。02 前沿爆发方向落后者挤作一团，领先者海阔天空。在国内各大新兴产业中，生物科技真正具备世界领先水平，分子设计方面，特别是工程抗体（ADC、多抗）设计已经不输于海外MNC和Biotech。4月15日，复宏汉霖全球研发日展示更安全有效的TCE三特异性抗体平台，其通过精妙的分子设计，达到持久的特异的T细胞激活效应、低T细胞浸润下更优的药效，同时得到更大的安全窗口、更低的CRS（细胞因子风暴），解决目前TCE临床上很大的问题。确保安全性后，产品才有望上一线，从而成为爆款。每一天都是崭新的，国内创新药企在擅长的工程抗体领域，将有更多创造性的排练组合，在下一代新型药物上也将勇闯无人区，。双载荷ADC双载荷（双毒素）ADC通过在一种抗体上偶联两种不同载荷或同一载荷的两种不同Linker，灵活调整药抗比（DAR）值，提高ADC活性，并降低耐药性发生率，实现耐药性克服和多机制协同的目标。双载荷ADC仍面临诸多挑战，涉及如何灵活调整两个有效载荷的比例和DAR值、如何选择合适的偶联技术、如何解决分子均一性差以及工艺问题。康弘药业KH815是靶向TROP2的双载荷ADC新药，两种payload分别为TOP1i和RAN POL2i，同时抑制RAN合成并诱导DNA双链断裂，具有较高的人体抗肿瘤应答率，且对单喜树碱类ADC耐药患者具有治疗潜力。信达生物双载荷ADC IBI3020于4月17日获批IND，基于差异化的下一代连接子-载荷技术平台研发，可特异性结合CEACAM5靶点，已在Dxd耐药肿瘤模型中显示疗效，拟用于治疗肠癌和非鳞状非小细胞肺癌等实体瘤。康宁杰瑞走得更远，开发出双抗双毒素ADC，即EGFR/HER3双毒素ADC新药JSKN021，分别通过可切割接头与Fc上的聚糖，等比例偶联拓扑异构酶抑制剂毒素T01（Alphatecan）和微管抑制剂毒素MMAE，DAR值为6（4+2），其在多个CDX模型中，显示出比单有效载荷ADC更强的肿瘤抑制效果。宜联生物双毒素ADC特点包括自主开发的三肽TMALIN连接子、五种不同的毒素，以及两种偶联方式。DAR值方面，拓扑异构酶抑制剂TMALIN-YL0014（C24）的DAR值为8，而微管抑制剂的DAR值则在1-3之间。药明合联是双载荷ADC大户，已经储备超过20个双载荷ADC分子。RDC放射性核素偶联药物（RDC）商业逻辑得到验证，2024年两款RDC（Pluvicto、Lutathera）合计为诺华带来21.16亿美元收入。基于相似性，RDC将复制ADC的成功路径。据平安证券，ADC是一种体内精准化疗手段，而RDC是体内精准放疗手段；ADC由靶向配体、连接子、细胞毒性载荷三部分构成，而RDC结构为靶向配体、连接臂及螯合剂（作用与连接子类似）、放射性核素三部分构成；ADC、RDC适应症布局和迭代升级路径类似，都是从末线适应症做起，通过迭代和联用向前线推进；与ADC相比，RDC具有“所见即所治”的诊疗一体化优势，以及物理杀伤带来的不易耐药的优势。2024年新型核药合计市值约40-50亿美元，约相当于ADC 2021年水平，正处于大爆发的前夜。截至2025年3月国内核药在NDA阶段共3个品种，分别是诺华的PSMA诊断药和治疗药，以及百洋医药（瑞迪奥）的锝[99mTc]肼基烟酰胺聚乙二醇双环RGD肽。国内在新核素和新靶点上布局领先的企业，还包括东诚药业、远大医药、中国同辐、恒瑞医药、云南白药、科伦博泰。大环肽大环肽(macrocyclic peptides)是一种新兴分子类型，尺寸介于小分子与生物药之间，其巨大潜力在于，一是能够靶向传统小分子药物难以结合的PPI（蛋白质相互作用），二是能够为通常由生物药治疗的靶点提供口服剂型。现有上市药物仅能有效作用于少数与疾病相关的靶标。这主要是因为大多数靶蛋白缺乏明确的结合口袋，使得小分子药物难以与之结合，同时许多与疾病相关蛋白位于细胞内部，而细胞膜的屏障作用阻止大分子药物（如抗体）进入细胞内部。大环肽因其显著的生物活性，展现出卓越的靶向性和与靶蛋白的结合能力，尤其在抗肿瘤方面，大环肽有可能通过被动扩散穿过细胞膜，能够针对那些“不可成药”的蛋白提供新的治疗选择。环肽具有口服递送的潜质，生物稳定性较高，可以抵抗外切酶的降解作用。环肽在不同的极性环境中可以采取不同的空间结构，帮助环肽在穿越细胞膜的过程中，在细胞膜极性头部（polar headgroup）和非极性尾部（unpolar tail）中，采取不同的结构和排列方向，有利于环肽分子穿越消化道上皮细胞而进入系统循环，相对于直链肽，其口服生物利用度显著增加。所以，默沙东对大环肽宠爱有加，称其为金发姑娘，在研的口服大环肽MK-0616已推至临床III期，作用机制与可注射PCSK9抑制剂相同，但口服剂型在慢病治疗中具备突出的成本和依从性优势。BMS推出第二代大环肽PD-L1，采用脂肪酸修饰策略，使分子能够与血清白蛋白可逆结合，从而显著延长体内循环时间，这一技术路线与已获批的GLP-1减肥药物类似。药明康德拥有成熟的大环肽技术，2023年与Unnatural product共同通过高效的大环肽DEL筛选方式顺利找到新型MDM2抑制剂。2024年1月，默沙东与Unnatural Products达成2.2亿美元交易，利用其技术来开发大环肽候选药物。口服大环肽Biotech元思生肽今年3月与阿斯利康达成战略合作，共同开发针对慢病（自免、代谢）的全球首创大环肽类药物。阿斯利康将支付7500万美元首付款及近期里程碑付款、总计可达34亿美元的研发及商业化里程碑付款，获得元思生肽智能化高通量大环肽药物研发平台使用权。大环肽分子的发现、优化和合成具有较高技术壁垒，国内玩家稀缺，但这是暂时的。创新药10年历史反复验证，当每一个潜力巨大的技术方向，跨过成药或产业化临界点时，中国Biotech都会成为最重要的参与者。随着原始创新能力的积累，下一个十年，中国Biotech将逐步成为引领者。识别微信二维码，添加抗体圈小编，符合条件者即可加入抗体圈微信群！请注明：姓名+研究方向！本公众号所有转载文章系出于传递更多信息之目的，且明确注明来源和作者，不希望被转载的媒体或个人可与我们联系(cbplib@163.com)，我们将立即进行删除处理。所有文章仅代表作者观点，不代表本站立场。

抗体药物偶联物财报并购引进/卖出临床1期

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,

后查看更多信息

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,

后查看更多信息

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
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	2024-06-01
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
大肠类癌	临床3期	葡萄牙	Advanced Accelerator Applications SA	2012-09-06

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临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT03972488 (NETTER-2, CTgov)	临床3期	胃肠胰神经内分泌肿瘤	226	30 mg Octreotide long acting repeatable (LAR) (Sandostatin LAR Depot)+2.5% Lys-Arg sterile amino acid solution+Lutathera (Lutathera® Plus Octreotide LAR 30 mg (Investigational Arm))	餘積選築餘顧醖網繭醖(鏇願顧鏇構憲壓醖構鏇) = 襯選築製窪製鹹蓋廠範餘廠積範齋願鏇淵構壓 (積齋鑰夢鹽願鏇鹹繭鬱, 繭築齋鏇壓衊醖範積鏇 ~ 憲鹹顧齋艱範醖顧構窪) 更多	-	2024-10-10
NCT03972488 (NETTER-2, CTgov)	临床3期	胃肠胰神经内分泌肿瘤	226	High dose 60 mg octreotide long-acting repeatable (Octreotide LAR 60 mg (Control Arm))	餘積選築餘顧醖網繭醖(鏇願顧鏇構憲壓醖構鏇) = 鏇衊製窪壓鬱窪鑰鏇鬱餘廠積範齋願鏇淵構壓 (積齋鑰夢鹽願鏇鹹繭鬱, 範糧繭餘壓蓋顧鏇膚製 ~ 築廠繭夢觸壓艱鑰淵築) 更多	-	2024-10-10
ASTRO2024	N/A	胃肠胰神经内分泌肿瘤	-	<sup>177</sup>Lu-DOTATATE	網餘蓋壓願願範夢製築(鹽襯淵範願簾餘願簾選) = 鬱鏇鹽壓願餘艱襯簾衊鹹簾遞蓋齋淵衊鑰蓋簾 (糧醖襯餘夢淵顧選鑰繭 )	-	2024-10-01
NCT02743741 (OZM-067, ASTRO2024)	N/A	-	33	177Lu-DOTATATE	範壓醖糧築糧鬱顧壓簾(廠夢衊鏇願顧廠範積選) = 餘鏇膚鹽齋鹹築糧膚製憲蓋鹽艱鹽積壓餘鹹觸 (鏇構範鏇糧積壓顧繭廠, 0.87) 更多	积极	2024-10-01
NCT02743741 (OZM-067, ASTRO2024)	N/A	-	33	68Ga-DOTATATE	範壓醖糧築糧鬱顧壓簾(廠夢衊鏇願顧廠範積選) = 選蓋夢選憲簾觸鬱艱構憲蓋鹽艱鹽積壓餘鹹觸 (鏇構範鏇糧積壓顧繭廠, 0.87) 更多	积极	2024-10-01
ASTRO2024	临床2期	神经内分泌肿瘤	195	177 Lu-DOTATATE (177Lu-D >880 mCi)	壓衊衊窪遞窪糧襯繭夢(壓糧製蓋鏇簾醖簾鹽夢) = 範製繭積艱衊夢簾餘襯遞築窪獵範襯憲範糧窪 (構艱艱醖鏇鑰鬱淵範遞, 90 ~ 100) 更多	不佳	2024-10-01
ASTRO2024	临床2期	神经内分泌肿瘤	195	177 Lu-DOTATATE (177Lu-D 800 Â± 10%)	壓衊衊窪遞窪糧襯繭夢(壓糧製蓋鏇簾醖簾鹽夢) = 構糧積壓襯餘夢製襯顧遞築窪獵範襯憲範糧窪 (構艱艱醖鏇鑰鬱淵範遞, 73 ~ 100) 更多	不佳	2024-10-01
ASTRO2024	临床2期	脑膜瘤 somatostatin receptors	20	177Lu-Dotatate 7.4 GBq	襯夢鑰構餘網鹽蓋窪鑰(構願夢憲鏇餘糧鏇繭衊) = 襯廠築繭壓築積觸糧顧獵網膚願範願壓窪網餘 (鏇鏇憲鹹夢願選願築餘, 52 ~ 94) 更多	积极	2024-10-01
Biospace 人工标引	临床2期	脑膜瘤	20	Lutathera	醖憲鏇壓鏇壓鹹廠憲鬱(蓋獵遞餘鑰構顧襯壓範) = 築淵蓋觸願簾蓋襯窪構鑰築獵膚衊獵齋繭餘簾 (夢醖繭廠積築製願餘膚 ) 更多	积极	2024-09-30
NETTER-1 (EANM2024)	N/A	177Lu-DOTATATE \| 225Ac-DOTATATE	20	177Lu-DOTATATE	觸醖鑰蓋鬱淵製淵築繭(鏇繭餘艱襯網鹽齋壓餘) = 醖膚壓襯構鏇窪壓憲願鑰觸鑰鏇齋窪齋簾衊鬱 (艱鬱糧夢構範積觸構淵, 1.01) 更多	积极	2024-09-27
NETTER-1 (EANM2024)	N/A	177Lu-DOTATATE \| 225Ac-DOTATATE	20	225Ac-DOTATATE	觸醖鑰蓋鬱淵製淵築繭(鏇繭餘艱襯網鹽齋壓餘) = 遞衊淵選夢顧膚糧淵憲鑰觸鑰鏇齋窪齋簾衊鬱 (艱鬱糧夢構範積觸構淵, 0.31) 更多	积极	2024-09-27
EANM2024	N/A	骨转移癌	77	177Lu-DOTATATE PRRT	築艱襯壓糧餘範鹹襯顧(夢鹹選憲鹹糧網壓夢顧) = 觸鏇積齋艱觸構淵鏇繭鬱糧構築鹽襯網壓遞鑰 (糧製願廠顧製網築選獵 ) 更多	-	2024-09-27
NCT04949282 (SEPTRALU, EANM2024)	N/A	神经内分泌肿瘤 somatostatin receptor (SSTR) overexpressing	-	177Lu-DOTATATE	艱憲夢窪鹹築襯淵鏇糧(醖構膚製膚艱簾膚壓獵) = 壓選醖鬱餘選鹹衊鹽製蓋積夢壓簾餘鹽憲餘壓 (獵願獵蓋壓製觸廠廠糧 ) 更多	-	2024-09-27
EANM2024	N/A	神经母细胞瘤	23	Lu-177 DOTATATE	糧獵構觸鏇製製鬱襯鬱(網顧壓廠壓鏇壓壓艱醖) = 膚襯憲廠構夢衊夢膚鹽壓積選艱製廠構網壓網 (觸淵鏇獵顧鏇餘鹹膚膚 ) 更多	积极	2024-09-27