The goal of this study is to propose the first direct comparison of Ga-68-DOTATATE PET/CT or PET/MR and Ga-68-DOTATOC PET/CT in patients with meningioma.

开始日期2026-01-01

申办/合作机构

Weill Medical College of Cornell University

[+1]

NCT06479811

/ Recruiting临床1期IIT

Phase I Trial of [212Pb]VMT-Alpha-NET in Metastatic or Inoperable Somatostatin-Receptor Positive Gastrointestinal Neuroendocrine Tumors, Pheochromocytoma/Paragangliomas, Small Cell Lung, Renal Cell, and Head and Neck Cancers

Background:
Some cancers have high levels of proteins called somatostatin receptors (SSTRs) on the surface of the tumors. These tumors can be in the lung, head and neck, digestive tract, kidneys, and in or near the adrenal glands. Researchers want to know if drug treatments that target SSTRs can help shrink these types of tumors.
Objective:
To test a study drug ([212Pb]VMT-Alpha-NET) in people with tumors that have SSTRs.
Eligibility:
People aged 18 years and older with tumors of the lung, kidneys, head and neck, digestive tract, or adrenal glands that have SSTRs. Their tumors must have spread to other organs and cannot be removed with surgery.
Design:
Participants will be screened. They will have a physical exam with blood and urine tests. They will have imaging scans and a test of their heart function. A sample of tumor tissue may be collected if one is not already available.
[212Pb]VMT-Alpha-NET is given through a tube attached to a needle inserted into a vein. The drug will be given on the first day of four 8-week cycles. Participants will stay in the hospital for a few nights after each dose. They will have blood tests once a week during each cycle.
Some participants will also get a related study drug ([203Pb]VMT-Alpha-NET). They will receive this drug a few days before the first 2 cycles. At 4, 24, and 48 hours after each infusion, they will have whole body scans. These scans will show where the study drug went in their body.
Follow-up visits will continue up to 6 years after the last treatment.

开始日期2025-08-19

申办/合作机构

National Cancer Institute

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]

100 项与镓[68Ga]多特安肽相关的临床结果

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100 项与镓[68Ga]多特安肽相关的转化医学

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100 项与镓[68Ga]多特安肽相关的专利（医药）

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291

项与镓[68Ga]多特安肽相关的文献（医药）

2025-09-01·APPLIED RADIATION AND ISOTOPES

Sequential synthesis of [18F]FDG and [68Ga]Ga-DOTA-TATE on the AllinOne radiosynthesizer: A fully automated dual-radionuclides protocol with single cassette and reagents loading

Article

作者: Zhen, Zhifei ; Fu, Chang ; Yang, Lingyue ; XuanYuan, Yirui ; Li, Huiqiang ; Gao, Yongju ; Chen, Lijuan ; Liang, Jianfei ; Xu, Junling ; Li, Xiaochen

BACKGROUND:

The development of a unified and efficient protocol for the automated synthesis of PET imaging agents is crucial for enhancing operational efficiency and safety. This study aimed to streamline the sequential production process of ¹⁸F-fluorodeoxyglucose ([¹⁸F]FDG) and [⁶⁸Ga]Ga-DOTA-TATE with only single cassette and reagents loading using the AllinOne 36-valve synthesis module, with the goal of improving hot cell utilization and minimizing radiation exposure for operators. The protocol was designed to allow for sequential synthesis without the need for repeated hot cell access or waiting for radiation levels to decrease, thereby reducing the time and resources required for PET imaging agent production.

RESULTS:

Our study demonstrated the stability and reliability of the newly designed synthesis protocol. The activity yields for two batches of [¹⁸F]FDG were 73 ± 6.2 % and 64 ± 4.7 % (n = 3), respectively, all with synthesis times about 23 min, and with a radiochemical purity consistently over 96 %. For [⁶⁸Ga]Ga-DOTA-TATE, the yield was 71 ± 5.8 % with synthesis times about 18 min (n = 3), with a purity exceeding 97 %. The synthesized products met all quality control criteria, including appearance, pH value, radioactivity concentration, sterility, endotoxin levels, and solvent residue.

CONCLUSION:

The single-cassette protocol significantly improved efficiency and reduced radiation exposure. High yields and purities confirm its clinical feasibility, ensuring PET imaging agent availability. This scalable solution enhances patient care by simplifying the production process and meeting the demands of various patients for different PET imaging agents within a single day, demonstrating its potential in clinical settings.

2025-09-01·SEMINARS IN NUCLEAR MEDICINE

Targets for Molecular Imaging of Neuroendocrine Tumors (NETs): An Overview and Update

Review

作者: Assadi, Majid ; Nasiri, Meysam ; Ahmadzadehfar, Hojjat ; Jafari, Esmail

Neuroendocrine neoplasms (NENs) represent a diverse group of tumors originating from neuroendocrine cells, characterized by their unique biological behavior and clinical manifestations. The incidence of neuroendocrine tumors (NETs) has been rising, necessitating effective diagnostic and therapeutic strategies. Molecular imaging, particularly through techniques such as PET and SPECT, plays a pivotal role in the management of NETs. This review highlights the significance of somatostatin receptor imaging in the initial diagnostic work-up, staging, and treatment planning for NETs, emphasizing the utility of radiopharmaceuticals like [⁶⁸Ga]Ga-DOTATATE and [⁶⁸Ga]Ga-DOTA-LM3. These agents demonstrate high sensitivity and specificity, allowing for accurate delineation of disease extent and identification of occult primary tumors. Furthermore, the review discusses the emerging role of nonsomatostatin receptor targets, such as glucose metabolism and fibroblast activation protein, in enhancing the diagnostic capabilities of molecular imaging. The integration of advanced imaging modalities, including dual-tracer approaches, is explored for their potential to refine therapeutic strategies and improve patient outcomes. As the field of molecular imaging continues to evolve, ongoing research and clinical trials are essential to validate the efficacy and safety of novel imaging agents and techniques, ultimately enhancing the management of patients with neuroendocrine tumors.

2025-08-01·NUCLEAR MEDICINE COMMUNICATIONS

Diagnostic pitfalls in [68Ga]Ga-DOTATATE PET/CT imaging: a systematic review

Review

作者: Abdlkadir, Ahmed Saad ; Khalaf, Aysar ; Badarneh, Mohannad ; Al-Alawi, Hasan ; Al Yasjeen, Salem ; Al Busaidi, Khalid ; Al Rammahi, Mohammed ; Al-Alawi, Haider ; Al-Ibraheem, Akram ; Al-Adhami, Dhuha

[68Ga]Ga-DOTA-Tyr3-octreotate ([68Ga]Ga-DOTATATE) is an established somatostatin receptor imaging agent that has demonstrated superior efficacy in visualizing neuroendocrine tumors (NETs) and meningiomas compared with traditional [111In]In-octreotide imaging. Despite its enhanced affinity and sensitivity, [68Ga]Ga-DOTATATE imaging is not without challenges. To date, numerous diagnostic pitfalls and false-positive findings have been reported. This systematic review investigates the currently recognized diagnostic pitfalls in [68Ga]Ga-DOTATATE positron imaging. A systematic literature search was conducted using PubMed, Scopus, and Web of Science databases, with the most recent update on 8 March 2024. Two authors screened the titles and abstracts of retrieved articles and selected studies based on predefined inclusion and exclusion criteria. Qualitative analysis of 70 included research articles, encompassing 199 patients, identified 234 diagnostic pitfalls. Malignant neoplastic etiologies predominated, constituting 56% of pitfalls, followed by nononcologic pitfalls (32.1%), and benign oncologic tumors (11.9%). Anatomically, the head and neck region was the most frequent site for pitfalls (35.5%), followed by the musculoskeletal system (27.4%), abdomen (17.5%), and chest (16.6%). Pelvic-related pitfalls were least common, accounting for only 3% of cases. This study details potential diagnostic pitfalls, predominantly occurring in the head-neck regions – primary sites for meningiomas and paragangliomas. Understanding these diagnostic pitfalls is crucial for accurate diagnosis. Moreover, recognizing these diagnostic pitfalls may lead to novel applications of [68Ga]Ga-DOTATATE beyond its conventional use in NETs and meningiomas, potentially expanding its diagnostic utility.

项与镓[68Ga]多特安肽相关的新闻（医药）

2025-08-29

·EINPresswire

July - September 2021 | Potential Signals of Serious Risks/New Safety Information Identified by the FDA Adverse Event Reporting System (FAERS)

Ajovy (fremanezumab-vfrm) Emgality (galcanezumab-gnlm) Nurtec ODT (rimegepant) Ubrelvy (ubrogepant) Vyepti (eptinezumab-jjmr) Hypertension The "Warnings and Precautions", "Adverse Reactions", "Patient Counseling Information", and "Patient Information" sections of the labeling were updated in March 2025 to include information about the risk of hypertension. Example: Ajovy labeling Apriso (mesalamine) Asacol (mesalamine) Asacol HD (mesalamine) Azulfidine (sulfasalazine) Azulfidine EN-Tabs (sulfasalazine) Canasa (mesalamine) Colazal (balsalazide disodium) Delzicol (mesalamine) Dipentum (osalazine sodium) Giazo (balsalazide disodium) Lialda (mesalamine) Rowasa (mesalamine) Pentasa (mesalamine) Severe cutaneous adverse reactions The Warnings and Precautions section of the labeling was updated November 2021 to include severe cutaneous adverse reactions. Example: Delzicol labeling Avastin (bevacizumab) Mvasi (bevacizumab-awwb) Zirabev (bevacizumab-bvzr) Pancreatitis FDA determined that no action is necessary at the time based on available information. Avastin (bevacizumab) Mvasi (bevacizumab-awwb) Zirabev (bevacizumab-bvzr) Anaphylactic shock The "Warnings and Precautions" section of the labeling was updated between September 2022 and February 2023 to include anaphylactoid/anaphylactic reactions. Example: Avastin labeling Ayvakit (avapritinib) Photosensitivity reaction The "Warnings and Precautions", "Adverse Reactions", "Patient Counseling Information", and "Patient Information" sections of the labeling were updated in March 2023 to include information about photosensitivity. Ayvakit labeling Azacitidine Onureg (azacitidine) Vidaza (azacitidine) Generic products containing azacitidine Pericarditis The "Adverse Reactions" section of the labeling was updated between September 2022 and June 2023 to include pericarditis. Example: Vidaza labeling FDA determined that no action is necessary at the time based on available information for Onureg. Bavencio (avelumab) Imfinzi (durvalumab) Libtayo (cemiplimab-rwlc) Keytruda (pembrolizumab) Opdivo (nivolumab) Tecentriq (atezolizumab) Yervoy (ipilimumab) Tumour lysis syndrome FDA determined that no action is necessary at the time based on available information. Cymbalta (duloxetine hydrochloride) Drizalma Sprinkle (duloxetine hydrochloride) Generic products containing duloxetine hydrochloride Anosmia, Hyposmia This issue is posted as two individual newly identified safety signal (NISS) entries in the January-March 2022 quarter, to reflect the focus on the potential signals of anosmia and hyposmia, separately. Darzalex (daratumumab) Darzalex Faspro (daratumumab and hyaluronidase-fihj) Blood stem cell transplant failure FDA determined that no action is necessary at the time based on available information. Dipeptidyl peptidase-4 (DPP-4) inhibitors Glyxambi (empagliflozin and linagliptin) Janumet (metformin hydrochloride and sitagliptin phosphate) Janumet XR (metformin hydrochloride and sitagliptin phosphate) Jentadueto (linagliptin and metformin hydrochloride) Jentadueto XR (linagliptin and metformin hydrochloride) Kazano (alogliptin and metformin hydrochloride) Kombiglyze XR (metformin hydrochloride and saxagliptin) Nesina (alogliptin) Onglyza (saxagliptin) Oseni (alogliptin and pioglitazone) Steglujan (ertugliflozin and sitagliptin) Tradjenta (linagliptin) Trijardy XR (empagliflozin, linagliptin and metformin hydrochloride) Qtern (saxagliptin and dapagliflozin) Generic products containing dipeptidyl peptidase-4 inhibitors Tubulointerstitial nephritis The "Adverse Reactions" section of the labeling was updated between March 2022 and June 2022 for products containing alogliptin and sitagliptin to include tubulointerstitial nephritis. Example: Janumet labeling FDA determined that no action is necessary for products containing linagliptin and saxagliptin at the time based on available information. *An administrative error resulted in the omission of Januvia from the list of product names after the initial quarterly report was posted. Dupixent (dupilumab) Angioedema The "Warnings and Precautions" and "Adverse Reactions" sections of the labeling were updated in December 2021 to include angioedema. Dupixent labeling Glucagon-like peptide-1 (GLP-1) analogues Adlyxin (lixisenatide) Bydureon (exenatide) Bydureon BCise (exenatide) Byetta (exenatide) Ozempic (semaglutide) Rybelsus (semaglutide) Saxenda (liraglutide) Soliqua 100/33 (insulin glargine and lixisenatide injection) Trulicity (dulaglutide) Victoza (liraglutide) Wegovy (semaglutide) Xultophy 100/3.6 (insulin degludec and liraglutide injection) Generic products containing glucagon-like peptide-1 analogues Gallbladder related disorders The "Warnings and Precautions", "Adverse Reactions", and "Patient Counseling Information" sections of the GLP-1 analogues labeling were updated between March 2022 and June 2022 to include information about acute gallbladder disease. Example: Adlyxin labeling FDA has determined that the last approved labeling for Saxenda and Wegovy is adequately labeled for acute gallbladder disease, and that no further regulatory action is needed at this time. Gonadotropin releasing hormone (GnRH) analogues Fensolvi (leuprolide acetate) Lupron Depot-PED (leuprolide acetate) Supprelin LA (histrelin acetate) Synarel (nafarelin acetate) Triptodur (triptorelin) Idiopathic intracranial hypertension The "Warnings", "Precautions", and "Adverse Reactions" sections of the labeling were updated in April 2022 to include idiopathic intracranial hypertension. Example: Fensolvi labeling Jakafi (ruxolitinib phosphate) Herpes simplex virus (HSV) reactivation and/or disseminated HSV The "Dosage and Administration", "Warnings and Precautions", and "Adverse Reactions" sections of the labeling were updated in January 2023 to include information about herpes simplex and herpes zoster infections. Jakafi labeling Ibrance (palbociclib) Kisqali (ribociclib) Kisqali Femara Co-Pack (letrozole and ribociclib) Embolic and thrombotic events, venous The "Adverse Reactions" section of the Ibrance labeling was updated in December 2024 to include venous thromboembolism. Ibrance labeling FDA determined that no action is necessary at the time for Kisqali and Kisqali Femara Co-Pack based on available information. Ocrevus (ocrelizumab) Myocardial infarction FDA determined that no action is necessary at the time based on available information. Potassium Chloride Product preparation error The “Warnings” section of the labeling was updated in December 2022 to include information about fatal cardiac adverse reactions with intravenous administration of undiluted potassium chloride. Praxbind (idarucizumab) Wrong dose errors The carton labeling and "Dosage and Administration" sections of the labeling were revised in February 2022 to clarify the number of vials included in each carton and the recommended dosing. Praxbind labeling Qbrexza (glycopyrronium tosylate) Accidental exposure to product The container label, carton labeling, "Dosage and Administration", "Warnings and Precautions", "Patient Counseling Information", and "Patient Information" sections of the labeling were updated in October 2022 to include information about accidental exposure. Qbrexza labeling Qbrexza (glycopyrronium tosylate) Urinary retention The “Warnings and Precautions”, “Adverse Reactions”, and “Patient Counseling Information” sections of the labeling were updated in October 2022 to include information about new or worsening urinary retention. Qbrexza labeling Sodium-glucose cotransporter-2 (SGLT-2) inhibitors Farxiga (dapagliflozin) Glyxambi (empagliflozin and linagliptin) Invokamet (canagliflozin and metformin hydrochloride) Invokamet XR (canagliflozin and metformin hydrochloride) Invokana (canagliflozin) Jardiance (empagliflozin) Qtern (saxagliptin and dapagliflozin) Steglatro (ertugliflozin) Steglujan (ertugliflozin and sitagliptin) Segluromet (ertugliflozin and metformin hydrochloride) Synjardy (empagliflozin and metformin hydrochloride) Synjardy XR (empagliflozin and metformin hydrochloride) Trijardy XR (empagliflozin, linagliptin and metformin hydrochloride) Xigduo XR (dapagliflozin and metformin) Generic products containing sodium-glucose cotransporter-2 (SGLT-2) inhibitors Tubulointerstitial nephritis FDA determined that no action is necessary at the time based on available information. Somatostatin Receptor Imaging Agents Detectnet (copper Cu-64 dotatate injection) Gallium Dotatoc (GA 68) Octreoscan (Indium In 111 Pentetreotide) Netspot (Gallium GA 68 Dotatate) Hypersensitivity The "Warnings and Precautions" and "Adverse Reactions" sections of the labeling were updated in December 2021 to include hypersensitivity reactions. Example: Netspot labeling Stromectol (ivermectin) Generic products containing ivermectin Off label use FDA determined that no action is necessary at the time based on available information. Stromectol (ivermectin) Generic products containing ivermectin Neurotoxicity The "Warnings", "Adverse Reactions", and "Overdosage" sections of the labeling were updated in March 2022 to include neurotoxicity. Example: Stromectol labeling Sunosi (solriamfetol hydrochloride) Hypersensitivity FDA determined that no action is necessary at the time based on available information. Vivitrol (naltrexone) Incorrect route of product administration The container label (vial), carton labeling, "Dosage and Administration", "Warnings and Precautions", and "Description", sections of the labeling were revised in September 2022 to emphasize the appropriate route and site of administration. Vivitrol labeling Xcopri (cenobamate) Psychiatric disorders The "Adverse Reactions" section of the labeling was updated in June 2022 to include psychiatric disorders. Xcopri labeling Legal Disclaimer: EIN Presswire provides this news content "as is" without warranty of any kind. We do not accept any responsibility or liability for the accuracy, content, images, videos, licenses, completeness, legality, or reliability of the information contained in this article. If you have any complaints or copyright issues related to this article, kindly contact the author above.

上市批准

2025-01-23

·小核说核药

新核药[68Ga]Ga-DATA5m-LM4的首个临床研究！

今天因为你的分享，让小核元气满满！ FOCUS ON Xiaohe 点击蓝字.催更小核小核微信| xiaoheshuoheyao777 聚焦领域| 放射性药物与临床核医学分享一篇文献摘要与图文。文章于2025年1月20日online于Theranostics期刊，报道了一项关于新型SSTR拮抗剂68Ga-DATA5m-LM4在转移性神经内分泌肿瘤（NETs）患者中的首次临床研究！该研究的主要目的是评估68Ga-DATA5m-LM4用于PET/CT成像的可行性，并考察其安全性、生物分布和初步诊断效能。相关往期链接：JNM：靶向成纤维细胞激活蛋白(FAP):使用方酰胺偶联双功能DOTA和DATA 5m螯合剂的下一代PET放射示踪剂《Bioconjugate Chem》用于肿瘤显像和治疗的方酸类放射药物论文的通讯作者是新加坡国立大学张静静教授和德国Richard P. Baum教授。可下载原文仔细拜读doi:10.7150/thno.94521 01 摘要 Abstract 背景简介 FDA和EMA已批准68Ga标记的[68Ga]Ga-DOTA-TATE和[68Ga]Ga-DOTA-TOC用于SSTR阳性NETs的成像，SSTR2的激动剂能够轻易内化进入肿瘤细胞，从而在靶细胞中滞留。近期的研究表明SSTR拮抗剂在某些患者中，尤其是SSTR2表达较低的患者中，可能具有更好的成像效果。与SSTR2激动剂相比，SSTR2拮抗剂如68Ga标记的DOTA或NODAGA螯合物与JR11和LM3在临床前和临床研究中显示出更高的摄取。螯合剂和核素对SSTR示踪剂的亲和力和药代动力学有较大影响，例如DOTA螯合剂不太适合与相对较小的放射性金属镓螯合，且需要较高的反应温度，这对于许多抗体以及热敏感的生物分子都是不利的。此外，这类螯合通常需要较长的反应时间，还需要额外的时间进行冷却，然后才能进行静脉注射，由于68Ga的半衰期较短，也给临床应用带来了限制。DATA是一种新型螯合剂，与已有的螯合剂相比，它在68Ga标记方面具有优势：DATA可以在室温下快速定量放射性标记68Ga，此外相关的螯合剂AAZTA提供了用治疗性同位素（如177Lu）标记的可能性。从2020年9月到2022年1月，该研究共纳入27名经组织病理学确认的分化良好的转移性NETs患者。 02 正文图片 Figure DATA5m-LM4结构：研究在50°C 15分钟内实现了80-95%的放射化学产率，整个68Ga-DATA5m-LM4的标记过程大约需要20分钟，包括加热、纯化、过滤和配制。随后进行纯化、配制和无菌过滤。使用分析型高效液相色谱和薄层色谱进行质量控制，两者都显示放射化学纯度超过98%，比活度在12到17 MBq/nmol之间。 68Ga-DATA5m-LM4在患者中的生物分布如上图所示：68Ga-DATA5m-LM4在注射后1小时内从血液循环中有效清除，并主要通过肾脏和泌尿系统排泄。除肾脏和膀胱外，68Ga-DATA5m-LM4的最高正常器官摄取在肾上腺，其次是脾脏和垂体，注射后60分钟的SUVmax分别为13.16 ± 5.80、12.87 ± 9.37和10.84 ± 6.40。腮腺、甲状腺、肝和胰腺表现出中等摄取，SUVmax分别为5.29 ± 2.64、3.16 ± 1.26、3.90 ± 0.88和3.73 ± 1.13。上表显示了68Ga-DATA5m-LM4与68Ga标记的其他SSTR类似物（包括68Ga-DOTA-TATE、68Ga-DOTA-TOC、68Ga-NODAGA-JR11、68Ga-NODAGA-LM3）的分布比较。与68Ga-DOTA-TATE PET/CT相比，68Ga-DATA5m-LM4在正常肝实质中的摄取较低（3.90 ± 0.88 vs. 9.12 ± 3.64, P < 0.000001）。此外，甲状腺、胰腺和脾脏的摄取也较低（P < 0.05）。在27名患者中，14名还接受了68Ga-DOTA-TOC PET/CT，1名接受了68Ga-DOTA-TATE PET/CT，4名接受了68Ga-NODAGA-LM3 PET/CT（上表）。半定量分析显示，68Ga-DATA5m-LM4在肝脏和脾脏的摄取显著低于68Ga-DOTA-TOC（3.70 ± 0.79 vs. 5.33 ± 2.43, P = 0.0397；11.88 ± 6.88 vs. 26.55 ± 16.07, P = 0.0022）。相比之下，68Ga-DATA5m-LM4在肾脏的摄取高于68Ga-DOTA-TOC（19.40 ± 7.12 vs. 16.44 ± 6.04, P = 0.0059）。68Ga-DATA5m-LM4在垂体的摄取显著高于68Ga-NODAGA-LM3（8.87 vs. 4.79, P = 0.0183），代表性图像如下所示。下图展示了27名患者通过68Ga-DATA5m-LM4 PET/CT检测到的肿瘤的SUVmax、肿瘤与肝脏比值以及肿瘤与血池比值。数据表明68Ga-DATA5m-LM4 PET/CT能够检测到高摄取的肿瘤病变，其中最高的SUVmax达到167.93，平均值为44.47 ± 36.22，第二高的SUVmax为133.99，平均值为34.00 ± 27.43。这些结果表明68Ga-DATA5m-LM4在检测NETs患者肿瘤病变方面的高效性和敏感性，尤其是在检测微小病变和CT不可见的肿瘤方面。 Q 小核的笔记呢？声明：本公众号为科研文献分享公益公众号，小核主要分享核药、放射性药物、核医学、放射化学等公开发表的研究成果，对相关疾病的诊断及治疗方案不做推荐（也不涉及），此外本文不构成也不提供任何投资建议。非常感谢读者们的关注！因小核个人水平有限，错误不可避免，欢迎各位读者留言或私信指出，小核会及时修订，感谢！小核原创，版权所有若需转载，敬请联络文末附上了原文链接，方便请检索拜读。 ●新CLDN18.2靶向核药重磅来袭！ ●68Ga-FAP-2286精准诊断尿路上皮癌！ ●新TROP2靶向核药重磅来袭！ ●“罕见”的甲状腺髓样癌核药赛道戳“小核”一起来讨论吧!

放射疗法临床结果

2025-01-11

·小核说核药

放射性药物及应用综述（2025）

01. 综述介绍美国FDA批准的[177Lu]Lu-DOTA-TATE、[177Lu]Lu-PSMA-617等药物及其配套诊断剂，推动了靶向放射性药物治疗在肿瘤学临床实践中的广泛应用，开启了放射性药物的新时代。新一代放射性药物借助靶向载体，实现精准输送，避免靶外沉积，有望提升肿瘤诊断治疗效率和生物安全性。众多研究正开发针对更广谱疾病靶点的新型放射性药物，其在体内展现出高肿瘤摄取率、长滞留时间及良好药代动力学特性等卓越性能。 2025年1月3日，第十三、十四届全国政协常委，中国工程院院士（医药卫生学部），中国医学科学院学部委员，中国医学科学院药物研究所执行所长、北京协和医学院特聘教授，兰州大学一级教授、兰州大学原副校长，深圳大学院士工作站讲席教授，中国药学会副理事长，中华医学会常务理事，国家药典委员会执行委员，长江学者，国家杰青王锐教授与中国医学科学院药物研究所胡宽教授为共同通讯于《Signal Transduction and Targeted Therapy》( IF 40.8 )期刊发表题为“Radiopharmaceuticals and their applications in medicine”的综述，本综述全面总结了放射性药物的演变，涵盖FDA批准及临床在研的药物，并探讨细胞死亡机制，强调了治疗性放射性药物在精准医学推进中的重要性和未来前景。本文仅做概述，请检索原文拜读：https://doi-org.libproxy1.nus.edu.sg/10.1038/s41392-024-02041-6 02. 综述概览自20世纪40年代初使用镭-223和碘-131治疗癌症以来，放射性药物的研究已经开展了至少80年，至今已有超过60种放射性药物被批准用于诊断或治疗各种癌症、神经退行性疾病和心血管疾病。自Lutathera（[177Lu]Lu-DOTA-TATE）、Pluvicto（[177Lu]Lu-PSMA-617）及诊断核药Netspot（[68Ga]Ga-DOTA-TATE）和Locametz（[68Ga]Ga-PSMA-11）获批以来，靶向放射性药物因其在癌症治疗中的卓越表现，引发了越来越多的关注。推动核医学发展的三大关键因素是：放射性核素、设备以及药物。从天然放射性核素到人工放射性核素，新放射性核素的不断发现，为核医学的诞生与发展奠定了坚实基础。随着放射性核素在临床领域的广泛应用，其在疾病诊断与治疗中的重要作用日益凸显，这进一步激发了对各种先进诊断设备的强烈需求，促使相关设备研发与技术不断取得突破，从而推动核医学整体向前迈进。国际放射防护委员会（ICRP）发布的放射性核素目录涵盖了约1200种放射性核素，然而在临床和科学研究中，仅有几十种被广泛运用。目前全球有67种放射性药物被批准，其中54种用于疾病诊断，用于成像的放射性药物在市场上广泛应用于恶性肿瘤、神经退行性疾病、心血管疾病以及其他疾病（如肾病综合征和肝肺综合征）的诊断。临床上使用的有34种SPECT放射性药物和20种PET放射性药物。对于SPECT检测的放射性核素，99mTc占70.6%，123I、111In、67Ga、125I和201Tl分别占11.8%、8.8%、2.9%、2.9%和2.9%。对于PET检测的放射性核素，18F因其适中的半衰期（109.8分钟）、灵活的回旋加速器生产以及成熟的标记方法而占据主导地位（65.0%）。此外，68Ga、11C、13N、64Cu和82Rb分别占15.0%、5.0%、5.0%、5.0%和5.0%。值得注意的是，68Ga在未来有潜力与177Lu或90Y作为诊断治疗对，64Cu也因其较长的半衰期（12.8小时）、在PET/CT成像中的高分辨率和检测率以及良好的安全性而受到越来越多的关注。成像类放射性药物主要涵盖肿瘤成像（46.3%）、中枢神经系统成像（20.4%）、心血管成像（14.8%）、肾脏成像（7.4%）、肺部成像（3.7%）、肝脏成像（3.7%）以及骨骼成像（3.7%）等七个领域。诊断类核药的关键难题在于其在正常组织中的非特异性摄取，这会导致靶外或非靶向病变的摄取，进而干扰精准的临床诊断。例如，在区分神经炎症与神经退行性疾病相关区域、良性前列腺炎与前列腺癌时，可能会出现诊断混淆。此外，对于某些靶点（如PSMA）表达水平较低的患者，可能会遭遇检测陷阱，而结合能力较弱的诊断剂则可能无法有效检测低表达肿瘤。因此，亟需优化假阳性和假阴性诊断模式，以提升放射性药物诊断的准确性与效率。目前全球有13种治疗性放射性药物被批准，且都用于治疗癌症。早期市场上的放射性药物缺乏肿瘤特异性，安全性不足。为了提高肿瘤的吸收和滞留，新的靶向放射性核素共轭小分子、肽和抗体已经得到了很好的开发，能够更精准地将放射性核素递送至肿瘤部位，从而提高治疗效果并减少对正常组织的损伤。治疗性药物虽能延长晚期癌症患者的生存期，但在临床实践中观察到的全身毒性，如骨髓抑制、口干和肾脏损伤等，可能引发严重的副作用。其他不良影响，包括耐药性和复发的可能性，亦需加以解决。总体而言，基于已获批的放射性药物，放射性核素在各领域的应用潜力巨大，仍有广阔的发展空间。此外，已获批的放射性药物可为研究人员提供宝贵的参考和指导，助力加速新药的研发进程。确定合适的靶点对于核药的临床转化至关重要，这篇综述回顾了具有显著临床进展或显著癌症靶向能力的有前途的肿瘤靶点及其相关的放射性药物；讨论了这些靶点在其他领域的潜在应用，例如在心血管成像中使用肿瘤特异性靶点，预测未来将实现临床应用；总结了这些靶点的药理学特征，以及对代表性放射性药物的当前研究和临床进展，并对其未来发展提供了见解；介绍了涉及肿瘤定向放射性药物靶点的临床评估放射性药物的化学结构，以下仅做部分展示，建议读者朋友检索原文仔细拜读。 FAP, PSMA, SSTR 靶点的化学结构及相关信息： Integrin、CXCR4、GRPR、UPAR、NTSR-1和Nectin-4的化学结构及相关信息：涉及免疫相关靶点的化学结构及相关信息：涉及神经系统疾病靶点的化学结构及相关信息：放射性药物的治疗效果是通过放射性核素产生的电离辐射实现的，这种辐射会导致DNA损伤和靶向细胞死亡。尽管对放射性药物治疗（RPT）的确切机制和独特要素了解不足，但多项研究揭示了放疗引起的辐射诱导细胞死亡所涉及的多个关键细胞过程。这篇综述对放射性药物治疗机制的当前理解进展进行了总结，基于对放疗引起的生物学效应的知识评估放射性药物诱导细胞毒性的潜在机制，包括直接DNA细胞死亡、活性氧（ROS）介导的细胞死亡和免疫原性细胞死亡。 03. 小结未来放射性药物的研发还需重点关注的临床需求如下：一方面，要聚焦如何突破现有诊断局限，实现对那些隐匿性强、当前方法难以察觉疾病的精准、早期诊断，为患者的后续治疗争取宝贵先机；另一方面，对于那些接受化疗、放疗、免疫检查点阻断或靶向治疗后疗效欠佳的癌症患者，如何改善他们的预后，也是亟待攻克的难关。未来仍需要临床医生和不同领域研究人员的通力协作，为放射性药物的蓬勃发展注入源源不断的动力，推动其迈向更为广阔的未来。文末附上了原文链接，方便读者检索拜读。 ●肾癌诊断核药赛道迎来重磅进展！ ●Alpha-9的GRPR核药随感笔记 ●近期颗粒酶B新核药的临床研究 ●ESMO 2024：核药笔记声明：本文观点仅代表小核本人，视角局限，欢迎批评指正；如需转载，请务必注明文章作者和来源。如有其它问题，请在本平台留言或联系xiaoheshuoheyao777@163.com，小核将在第一时间处理。内容编辑 | 小核排版设计 | 小核媒体合作 | 科研宣传 | 转载开白 xiaoheshuoheyao777（小核微信）

放射疗法抗体药物偶联物上市批准

100 项与镓[68Ga]多特安肽相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	V09	-

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
神经内分泌肿瘤	美国	Advanced Accelerator Applications USA, Inc.	2016-06-01

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	临床3期	中国	原子高科股份有限公司	2024-01-05
鼻咽癌	临床2期	中国	福建医科大学附属第一医院（福建省皮肤病性病防治院、福建省皮肤病性病防治研究所）	2022-11-20
肿瘤	临床2期	美国	Stanford University	2014-05-27
甲状腺髓样癌	临床1期	中国	福建医科大学附属第一医院（福建省皮肤病性病防治院、福建省皮肤病性病防治研究所）	2023-06-21
神经嵴肿瘤	临床1期	中国	北京协和医院	2021-09-01
神经母细胞瘤	临床1期	中国	北京协和医院	2021-09-01
嗜铬细胞瘤	临床1期	中国	北京协和医院	2021-09-01
肿瘤源性骨软化症	临床1期	中国	北京协和医院	2020-03-15
间充质细胞肿瘤	临床1期	中国	北京协和医院	2011-12-01

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临床结果

适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT03448458 (CTgov)	临床2期	转移性去势抵抗性前列腺癌	17	CT (Computed Tomography)+Gallium Ga 68-DOTATATE	構廠鏇衊觸觸鹽鏇廠範 = 範衊繭鹹鏇網鑰獵積蓋衊糧鹹艱願鹹襯淵窪選 (製鹽遞積鑰遞膚構鬱糧, 構鹽齋顧遞膚齋觸願網 ~ 鹹簾築鹹鹽簾積網鬱選) 更多	-	2025-07-17
NCT03736564 (CTgov)	临床1/2期	间充质细胞肿瘤 \| 肿瘤源性骨软化症	18	68Ga-DOTATATE PET/CT	壓網顧鑰選窪選範淵廠 = 網憲鏇艱窪壓窪醖鹹鏇簾餘餘淵簾蓋醖壓鹽夢 (構繭淵醖艱蓋襯襯鏇憲, 網鹽蓋鹽鬱鏇製範獵艱 ~ 憲艱醖糧鹽簾築獵膚觸) 更多	-	2025-04-30
EANM2024	N/A	转移性甲状腺髓样癌 serum calcitonin levels	20	68Ga-DOTATATE PET/CT	齋顧糧鏇齋觸網窪夢積(廠築壓顧餘遞夢觸齋遞) = 構鏇顧鹽觸積繭憲廠鑰餘鑰鑰憲觸膚鹽憲衊膚 (憲壓構繭製齋繭齋壓顧, 5.52 ~ 29.48)	积极	2024-09-27
SNO2023	N/A	脑膜瘤 68 Ga-DOTATATE/PET	46	Positive 68Ga-DOTATATE/PET	製壓鏇鏇夢膚糧遞淵襯(築淵蓋餘膚鹽鑰齋網簾) = 鹽淵醖衊鹹顧願範襯襯憲築鬱膚鏇觸襯範壓觸 (製遞衊鹽鬱鹽廠選淵鑰 )	积极	2023-11-10
SNO2023	N/A	脑膜瘤 68 Ga-DOTATATE/PET	46	Negative 68Ga-DOTATATE/PET	範窪範夢鬱選築壓艱齋(網範積獵憲網積構簾襯) = 觸糧網憲糧獵製積糧餘願廠壓壓糧範願醖構顧 (艱鑰艱積齋鑰觸襯網膚 )	积极	2023-11-10
P15.11.B (EANO2023)	N/A	脑膜瘤 68 Ga-DOTATATE/PET	46	Positive 68Ga-DOTATATE/PET	壓壓簾遞齋衊膚衊選築(獵遞積網醖襯衊膚積鬱) = higher on PET compared to MRI 憲鹽鹹夢網齋醖齋顧製 (憲築醖夢糧選繭鑰壓鏇 )	积极	2023-09-08
ASCO_GI2023	N/A	APUD瘤	424	Ga68-DOTATE (Patients with well-differentiated NETs of GI and pancreatic origin)	淵積簾膚憲夢製選壓遞(獵選鬱觸夢獵顧遞廠鬱) = 蓋餘範製獵願窪壓鏇遞衊積範鹽齋憲願衊觸鏇 (襯願簾鏇遞齋遞選鏇鑰 ) 更多	-	2023-01-24
ASCO_GI2023	N/A	APUD瘤	424	Ga68-DOTATE (Patients with lung carcinoid)	衊觸糧願構蓋鏇襯壓膚(鬱範壓鏇襯獵簾願簾鏇) = 齋構鹹齋網構鏇齋壓鬱餘鑰鏇膚醖壓齋獵製壓 (齋淵網築衊顧窪遞憲衊 )	-	2023-01-24
ASTRO2022	N/A	脑膜瘤	-	[Ga68]-DOTATATE (fSRS (35 Gy in 5 fractions))	遞餘顧餘醖鬱窪醖觸壓(憲齋獵鑰顧構積鏇築鏇) = 觸觸積夢構鬱鏇築鑰鹹繭積簾蓋積醖獵築繭範 (襯餘壓廠艱獵遞蓋醖蓋 )	-	2022-11-01
SNMMI2022	N/A	神经内分泌肿瘤	-	68Ga-DOTATATE (Neuroendocrine tumor patients with cardiac metastases)	憲遞夢繭夢糧蓋鹽鏇憲(壓壓構繭憲衊鑰鑰膚觸) = mean ± SD: 26.2 ± 31.4 鑰鹽蓋鑰齋積廠鏇鹽糧 (壓選範製簾築膚窪衊蓋 ) 更多	-	2022-08-08
SNMMI2022	N/A	神经内分泌肿瘤	-	68Ga-DOTATATE (Patients with non-cardiac metastatic grade 1-2 gastroenteropancreatic NETs)		-	2022-08-08
SNMMI2022	N/A	神经内分泌肿瘤 tumor markers	98	68Ga-DOTATATE PET/CT	餘窪鹽積夢築膚夢衊構(願窪鬱鹽壓鏇鏇顧襯繭) = 顧築夢範夢網襯獵網網廠夢壓築遞壓築夢夢齋 (鏇鏇醖襯餘網廠襯選糧 ) 更多	积极	2022-08-08
NCT03549598 (CTgov)	临床4期	心脏结节病	15	13NH3 PET/CT scan+18FDG PET/CT scan+68Ga-DOTATATE PET/CT	鏇選憲製製選鹹構壓簾 = 觸積範淵網淵衊夢廠廠衊醖齋顧醖鏇憲積膚餘 (網願觸鏇範夢築鑰鹽簾, 淵蓋鬱製願獵鹽夢齋範 ~ 製壓構網構壓構遞餘顧) 更多	-	2020-10-20