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Nectin-4, Bladder Cancer, and Nuclear Medicine: A Theranostic Frontier Nectin-4,膀胱癌和核医学:治疗前沿。
IF 5.9 2区 医学 Q1 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING Pub Date : 2025-11-01 Epub Date: 2025-09-27 DOI: 10.1053/j.semnuclmed.2025.09.003
Joseph Kabunda , Honest Ndlovu , Karishma Singh , Sandile Sibiya , Sipho Mdanda , Kamo Ramonaheng , Akram Al-Ibraheem , Ken Herrmann , Kgomotso Mokoala , Mike Sathekge
Bladder cancer is among the top ten most common cancers globally, with advanced or metastatic disease associated with dismal survival outcomes. Current diagnostic imaging and therapies have significant limitations, highlighting the urgent need for novel theranostic targets. Nectin-4, a cell adhesion molecule frequently overexpressed in bladder cancer, especially urothelial carcinoma (∼60%-87% of tumors), has emerged as a promising biomarker and therapeutic target. This review critically evaluates the role of Nectin-4 in bladder cancer and explores its exciting potential in nuclear medicine for combined molecular imaging and targeted radionuclide therapy—embracing the "theranostic" paradigm. Nectin-4 is abundantly and selectively expressed in most urothelial carcinomas, correlating with advanced disease and poorer prognosis. Clinically validated by the FDA-approved antibody-drug conjugate enfortumab vedotin, Nectin-4 targeting achieves objective response rates around 40%-50% and significantly improves survival in refractory advanced urothelial carcinoma. Recent clinical advances in Nectin-4–targeted PET imaging (such as 68Ga-labeled agents) have demonstrated excellent tumor localization and specificity, enabling precise patient selection for targeted therapies. Additionally, emerging radionuclide therapeutics (eg, 225Ac- and 177Lu-based agents) show promising preclinical and early clinical efficacy, robust tumor targeting, and favorable safety profiles. Targeting Nectin-4 represents a new frontier in the management of bladder cancer, bridging the gap between precise molecular diagnostics and personalized targeted radionuclide therapy. Ongoing clinical trials and translational research are rapidly advancing this promising theranostic strategy towards routine clinical application, with significant potential to enhance patient selection, treatment monitoring, and ultimately, clinical outcomes.
膀胱癌是全球十大最常见的癌症之一,晚期或转移性疾病与惨淡的生存结果相关。目前的诊断成像和治疗有明显的局限性,突出了迫切需要新的治疗靶点。Nectin-4是一种在膀胱癌,特别是尿路上皮癌(约60%-87%的肿瘤)中经常过表达的细胞粘附分子,已成为一种有前途的生物标志物和治疗靶点。这篇综述批判性地评估了Nectin-4在膀胱癌中的作用,并探讨了其在核医学中结合分子成像和靶向放射性核素治疗的令人兴奋的潜力-拥抱“治疗”范式。Nectin-4在大多数尿路上皮癌中大量和选择性表达,与晚期疾病和较差预后相关。经fda批准的抗体-药物偶联物enfortumab vedotin临床验证,Nectin-4靶向治疗难治性晚期尿路上皮癌的客观缓解率约为40%-50%,显著提高生存率。最近在nectin -4靶向PET成像(如68ga标记剂)方面的临床进展已经证明了出色的肿瘤定位和特异性,可以精确地选择患者进行靶向治疗。此外,新兴的放射性核素疗法(例如,基于225Ac和177lu的药物)显示出有希望的临床前和早期临床疗效,强大的肿瘤靶向性和良好的安全性。靶向Nectin-4代表了膀胱癌治疗的新前沿,弥合了精确分子诊断和个性化靶向放射性核素治疗之间的差距。正在进行的临床试验和转化研究正迅速将这种有前景的治疗策略推向常规临床应用,在加强患者选择、治疗监测以及最终的临床结果方面具有巨大的潜力。
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引用次数: 0
The Role of [177Lu] Lu-Satoreotide Tetraxetan in Somatostatin Receptor-Positive Neuroendocrine Tumors [177Lu] Lu-Satoreotide Tetraxetan在生长抑素受体阳性神经内分泌肿瘤中的作用。
IF 5.9 2区 医学 Q1 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING Pub Date : 2025-11-01 Epub Date: 2025-08-11 DOI: 10.1053/j.semnuclmed.2025.07.002
Kalyan Mansukhbhai Shekhda , Shaunak Navalkissoor
Peptide receptor radionuclide therapy (PRRT) targeting the somatostatin receptor with receptor agonists has emerged as a key treatment in the management of well-differentiated neuroendocrine tumors (NETs). The therapeutic efficacy of these agents has traditionally been attributed to receptor-mediated internalization of the radiolabeled peptide into tumor cells. In contrast, somatostatin receptor (SSTR) antagonists bind to the receptor without undergoing significant internalization. Despite this theoretical limitation, accumulating preclinical and clinical evidence supports the therapeutic utility of SSTR antagonists. These agents have been shown to bind to a greater number of receptor sites and exhibit prolonged tumor retention, properties that may enhance both imaging sensitivity and therapeutic efficacy. Among the antagonists studied, [¹⁷⁷Lu]Lu-satoreotide tetraxetan is the most extensively investigated to date. In this article, we review both preclinical and clinical data evaluating the efficacy and safety of [¹⁷⁷Lu]Lu-satoreotide tetraxetan in the treatment of neuroendocrine tumors. We also provide a brief overview of other SSTR antagonists currently under investigation.
利用受体激动剂靶向生长抑素受体的肽受体放射性核素治疗(PRRT)已成为治疗分化良好的神经内分泌肿瘤(NETs)的关键治疗方法。这些药物的治疗效果传统上归因于受体介导的放射性标记肽内化到肿瘤细胞中。相反,生长抑素受体(SSTR)拮抗剂与受体结合而不经历显著的内化。尽管存在理论上的局限性,但越来越多的临床前和临床证据支持SSTR拮抗剂的治疗效用。这些药物已被证明可以结合更多的受体位点,并表现出长时间的肿瘤滞留,这些特性可能会提高成像敏感性和治疗效果。在研究的拮抗剂中,Lu-satoreotide tetraxetan是迄今为止研究最广泛的。在本文中,我们回顾了评估[¹⁷⁷Lu]Lu-satoreotide tetraxetan治疗神经内分泌肿瘤的有效性和安全性的临床前和临床数据。我们还简要概述了目前正在研究的其他SSTR拮抗剂。
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引用次数: 0
Implementation of Radiotheranostics: Challenges, Barriers, and IAEA-Driven Strategies for Sustainable Access 放射肿瘤学的实施:挑战、障碍和原子能机构驱动的可持续获取战略。
IF 5.9 2区 医学 Q1 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING Pub Date : 2025-11-01 Epub Date: 2025-08-31 DOI: 10.1053/j.semnuclmed.2025.07.005
Akram Al-Ibraheem , Anita Brink , Sze Ting Lee , Amelia De Los Reyes , Diana Paez , Pietro Selemo Craviolatti , Augusto Llamas-Olier , Francesco Giammarile , Ahmed S. Abdlkadir , Enrique Estrada-Lobato , May Abdel-Wahab , John Prior , Andrew M. Scott , Mike Machaba Sathekge
Radiotheranostics represent a cutting-edge advancement in the management of noncommunicable diseases, integrating diagnostic imaging with targeted radiotherapy in a single, personalized approach. Over the past decade, the field has gained substantial momentum, with several radiopharmaceuticals now incorporated into clinical practice, most notably for neuroendocrine tumors and prostate cancer. The pipeline of novel agents continues to grow, offering promising therapeutic options for patients with cancers resistant to conventional therapies. Despite these advances, the broad implementation of radiotheranostics is impeded by several challenges, including logistical constraints, financial limitations, resource scarcity, political instability, and regulatory and educational barriers. Overcoming these obstacles requires coordinated mitigation strategies focused on strengthening education and training, expanding radiopharmaceutical production and development, enhancing research capacity, and establishing robust quality management systems. This review provides a comprehensive overview of the current global landscape of radiotheranostics, identifies key implementation barriers, and offers expert-driven strategies and recommendations from the International Atomic Energy Agency to support sustainable and equitable access to radiotheranostics.
放射肿瘤学代表了非传染性疾病管理的前沿进展,将诊断成像与靶向放疗以单一的个性化方法相结合。在过去的十年中,该领域获得了巨大的发展势头,一些放射性药物现已纳入临床实践,最明显的是用于神经内分泌肿瘤和前列腺癌。新型药物的研发渠道持续增长,为那些对传统疗法有耐药性的癌症患者提供了有希望的治疗选择。尽管取得了这些进展,但放射治疗的广泛实施仍受到一些挑战的阻碍,包括后勤限制、财政限制、资源稀缺、政治不稳定以及监管和教育障碍。克服这些障碍需要协调一致的缓解战略,重点是加强教育和培训,扩大放射性药物的生产和开发,提高研究能力,建立健全的质量管理体系。本综述全面概述了当前全球放射治疗的概况,确定了关键的实施障碍,并提供了专家驱动的战略和国际原子能机构的建议,以支持可持续和公平地获得放射治疗。
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引用次数: 0
Advances With 225Ac-DOTATATE Targeted Alpha Therapy in Somatostatin Receptor Positive Neuroendocrine Tumors 225Ac-DOTATATE靶向α治疗生长抑素受体阳性神经内分泌肿瘤的研究进展
IF 5.9 2区 医学 Q1 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING Pub Date : 2025-11-01 Epub Date: 2025-07-04 DOI: 10.1053/j.semnuclmed.2025.06.008
Kunal Ramesh Chandekar, Chandrasekhar Bal
225Ac-DOTATATE-based targeted alpha therapy (TAT) is emerging as a transformative option in the management of advanced, well-differentiated, somatostatin receptor (SSTR)-positive neuroendocrine tumors (NETs), particularly in patients refractory to conventional β-emitter peptide receptor radionuclide therapy (PRRT). This review synthesizes current evidence from preclinical models and early-phase clinical studies, highlighting its therapeutic promise in terms of potent antitumor efficacy and favorable toxicity profile. We discuss the radiobiological and mechanistic advantages of α-particle therapy while also addressing key limitations such as radionuclide supply constraints, recoil-induced daughter redistribution, challenges in dosimetry, and regulatory hurdles. Emerging strategies including improved chelators, SSTR antagonists, and tandem or combination therapies are described. Key ongoing trials have also been summarized. As 225Ac-DOTATATE-based TAT progresses toward mainstream clinical integration, multidisciplinary collaboration across academia, industry, and regulatory bodies will be essential to refine protocols, optimize safety, and expand access.
225Ac-DOTATATE-based靶向α治疗(TAT)正在成为治疗晚期、分化良好的生长抑制素受体(SSTR)阳性神经内分泌肿瘤(NETs)的一种变革性选择,特别是在传统β-发射器肽受体放射性核素治疗(PRRT)难治的患者中。本综述综合了临床前模型和早期临床研究的现有证据,强调了其在抗肿瘤功效和良好毒性方面的治疗前景。我们讨论了α-粒子治疗的放射生物学和机制优势,同时也解决了诸如放射性核素供应限制、反冲诱导子再分布、剂量学挑战和监管障碍等关键限制。新兴的策略包括改进的螯合剂,SSTR拮抗剂,串联或联合治疗的描述。还总结了正在进行的关键试验。随着基于225ac - dotate的TAT向主流临床整合发展,学术界、工业界和监管机构之间的多学科合作对于完善方案、优化安全性和扩大可及性至关重要。
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引用次数: 0
Glypican-3: Novel Theranostic Agent for Hepatocellular Carcinoma Glypican-3:一种新的肝细胞癌治疗剂。
IF 5.9 2区 医学 Q1 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING Pub Date : 2025-11-01 Epub Date: 2025-09-27 DOI: 10.1053/j.semnuclmed.2025.09.004
Luca Filippi
Glypican-3 (GPC3) is a membrane-anchored heparan sulfate proteoglycan overexpressed in many hepatocellular carcinomas (HCCs) while minimally present in normal adult liver, making it an attractive target for integrated diagnostic and therapeutic ("theranostic") strategies. This review synthesizes preclinical and early clinical efforts to exploit GPC3 for targeted PET imaging and radionuclide therapy. Imaging approaches have evolved from 89Zr- and 124I-labeled full antibodies—demonstrating robust, delayed tumor localization—to smaller scaffolds (F(ab')₂, single-domain antibodies, peptides) paired with 18F or 68Ga for same-day, high-contrast imaging. First-in-human studies, including 124I-codrituzumab and 68Ga-RAYZ-8009, confirmed tumor-specific accumulation but remained limited in scale. Therapeutic investigations spanned beta-emitters (90Y, 177Lu) and high-LET alpha-emitters (225Ac, 227Th), showing potent antitumor effects in orthotopic and xenograft models yet raising dosimetric and toxicity concerns—especially for long-circulating antibody carriers and alpha therapies. Key translational challenges include hepatic background clearance, intra-patient heterogeneity of GPC3 expression, rigorous dosimetry, toxicology in larger species, and radionuclide supply logistics. The available evidence suggests a preferential pathway, involving the selection of a limited set of lead vectors, their pairing with suitable radionuclides, validation in orthotopic/PDX models using standardized endpoints, and the integration of comprehensive dosimetric and toxicologic studies before proceeding to broader human trials. GPC3-directed theranostics thus offers a compelling, disease-specific route to precision management of HCC, provided translational rigor addresses the outlined safety and quantitative imaging gaps.
Glypican-3 (GPC3)是一种膜锚定的硫酸肝素蛋白多糖,在许多肝细胞癌(hcc)中过表达,而在正常成人肝脏中含量极低,使其成为综合诊断和治疗(“治疗”)策略的一个有吸引力的靶点。本文综述了利用GPC3靶向PET成像和放射性核素治疗的临床前和早期临床工作。成像方法已经从89Zr-和124i标记的全抗体(显示稳健的,延迟的肿瘤定位)发展到较小的支架(F(ab') 2,单域抗体,肽)与18F或68Ga配对,进行当日高对比度成像。包括124I-codrituzumab和68Ga-RAYZ-8009在内的首次人体研究证实了肿瘤特异性积累,但规模仍然有限。治疗研究跨越β -发射体(90Y, 177Lu)和高α -发射体(225Ac, 227),显示出在原位和异种移植模型中有效的抗肿瘤作用,但引起了剂量学和毒性问题,特别是对于长循环抗体携带者和α -治疗。关键的翻译挑战包括肝脏背景清除、患者内部GPC3表达的异质性、严格的剂量学、大型物种的毒理学和放射性核素供应物流。现有证据表明有一条优先途径,包括选择一组有限的先导载体,将其与合适的放射性核素配对,使用标准化终点在原位/PDX模型中进行验证,以及在进行更广泛的人体试验之前整合综合剂量学和毒理学研究。因此,gpc3导向的治疗为HCC的精确治疗提供了一条引人注目的、针对特定疾病的途径,前提是翻译的严密性解决了概述的安全性和定量成像差距。
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引用次数: 0
Letter from the Editors 编辑的信
IF 5.9 2区 医学 Q1 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING Pub Date : 2025-11-01 Epub Date: 2025-10-24 DOI: 10.1053/j.semnuclmed.2025.09.007
M Michael Sathekge, Kirsten Bouchelouche
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引用次数: 0
New Targets for Imaging in Nuclear Medicine 核医学成像新靶点。
IF 5.9 2区 医学 Q1 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING Pub Date : 2025-09-01 Epub Date: 2025-05-06 DOI: 10.1053/j.semnuclmed.2025.04.004
Anita Brink , Diana Paez , Enrique Estrada Lobato , Roberto C. Delgado Bolton , Peter Knoll , Aruna Korde , Adriana K. Calapaquí Terán , Mohamad Haidar , Francesco Giammarile
Nuclear medicine is rapidly evolving with new molecular imaging targets and advanced computational tools that promise to enhance diagnostic precision and personalized therapy. Recent years have seen a surge in novel PET and SPECT tracers, such as those targeting prostate-specific membrane antigen (PSMA) in prostate cancer, fibroblast activation protein (FAP) in tumor stroma, and tau protein in neurodegenerative disease. These tracers enable more specific visualization of disease processes compared to traditional agents, fitting into a broader shift toward precision imaging in oncology and neurology. In parallel, artificial intelligence (AI) and machine learning techniques are being integrated into tracer development and image analysis. AI-driven methods can accelerate radiopharmaceutical discovery, optimize pharmacokinetic properties, and assist in interpreting complex imaging datasets. This editorial provides an expanded overview of emerging imaging targets and techniques, including theranostic applications that pair diagnosis with radionuclide therapy, and examines how AI is augmenting nuclear medicine. We discuss the implications of these advancements within the field’s historical trajectory and address the regulatory, manufacturing, and clinical challenges that must be navigated. Innovations in molecular targeting and AI are poised to transform nuclear medicine practice, enabling more personalized diagnostics and radiotheranostic strategies in the era of precision healthcare.
核医学正在迅速发展,新的分子成像目标和先进的计算工具有望提高诊断精度和个性化治疗。近年来,新的PET和SPECT示踪剂出现了激增,例如针对前列腺癌中的前列腺特异性膜抗原(PSMA)、肿瘤基质中的成纤维细胞激活蛋白(FAP)和神经退行性疾病中的tau蛋白的示踪剂。与传统药物相比,这些示踪剂能够更具体地可视化疾病过程,适应肿瘤和神经病学向精确成像的更广泛转变。与此同时,人工智能(AI)和机器学习技术正在被整合到示踪剂开发和图像分析中。人工智能驱动的方法可以加速放射性药物的发现,优化药代动力学特性,并协助解释复杂的成像数据集。这篇社论提供了新兴成像靶点和技术的扩展概述,包括将诊断与放射性核素治疗相结合的治疗应用,并研究了人工智能如何增强核医学。我们将讨论这些进展对该领域历史轨迹的影响,并解决必须解决的监管、制造和临床挑战。分子靶向和人工智能的创新将改变核医学实践,在精准医疗时代实现更个性化的诊断和放射治疗策略。
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引用次数: 0
Advances in Endocrine Tumor PET Imaging Targeting CXCR4 and GLP-1 靶向CXCR4和GLP-1的内分泌肿瘤PET成像研究进展
IF 5.9 2区 医学 Q1 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING Pub Date : 2025-09-01 Epub Date: 2025-05-29 DOI: 10.1053/j.semnuclmed.2025.05.001
Esther Mena , Liza Lindenberg , Peter Herscovitch , Samira M. Sadowski , Peter L. Choyke
Molecular imaging has experienced significant advances in the areas of imaging probes and technology, enabling the detection of tumors at earlier stages and more accurately identifying extent of disease. To better characterize lesions, nuclear medicine modalities utilize molecular imaging agents targeting specific pathways and cell surface molecules to improve both sensitivity and specificity. In the field of endocrinology, tumors encompass a wide spectrum of aggressiveness ranging from indolent, well differentiated tumors to highly aggressive cancers. Thus, in recent years, new molecular imaging biomarkers have been developed for noninvasively assessing different types of hormone-producing tumors. For instance, 68Ga-PentixaFor is a novel PET imaging agent targeting the C-X-C chemokine receptor type 4 (CXCR4) with proven utility in various malignancies, and has also shown multifunctionality in detecting endocrine pathologies, such as primary aldosteronism, adrenocorticotropic hormone (ACTH)-producing pituitary adenomas and ACTH-independent cortisol-producing adrenal adenomas. Another novel receptor-targeted radiotracer using the glucagon-like peptide-1 receptor (GLP-1R) analog, Exendin-4 has recently developed to preoperatively localize insulinomas, arising from pancreatic beta cells. This review presents an overview of new developments and potential clinical implementation of CXCR4- and Exendin- based radiotracers for imaging applications in endocrinology.
分子成像在成像探针和技术领域取得了重大进展,能够在早期阶段检测肿瘤并更准确地确定疾病的程度。为了更好地表征病变,核医学模式利用靶向特定途径和细胞表面分子的分子显像剂来提高灵敏度和特异性。在内分泌学领域,肿瘤涵盖了广泛的侵袭性,从惰性的、分化良好的肿瘤到高度侵袭性的肿瘤。因此,近年来,新的分子成像生物标志物已经被开发出来,用于无创评估不同类型的激素产生肿瘤。例如,68Ga-PentixaFor是一种针对C-X-C趋化因子受体4型(CXCR4)的新型PET显像剂,已被证明在各种恶性肿瘤中具有实用价值,并且在检测内分泌病变(如原发性醛固酮增多症、促肾上腺皮质激素(ACTH)产生的垂体腺瘤和不依赖促肾上腺皮质激素产生的肾上腺腺瘤)方面也显示出多种功能。另一种新型受体靶向放射性示踪剂使用胰高血糖素样肽-1受体(GLP-1R)类似物Exendin-4,最近被开发用于术前定位胰岛细胞产生的胰岛素瘤。本文综述了基于CXCR4和Exendin的放射示踪剂在内分泌成像中的新进展和潜在的临床应用。
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引用次数: 0
Fibroblast Activation Protein Inhibitor (FAPI) PET in Sarcoma: An Update and Future Perspective 成纤维细胞活化蛋白抑制剂(FAPI) PET在肉瘤中的应用:最新进展和未来展望。
IF 5.9 2区 医学 Q1 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING Pub Date : 2025-09-01 Epub Date: 2025-06-01 DOI: 10.1053/j.semnuclmed.2025.05.003
Roberto C. Delgado Bolton , Adriana K. Calapaquí Terán , Ludmila Santiago Almeida , Diana Paez , Enrique Estrada Lobato , Anita Brink , Peter Knoll , Giorgio Treglia , Francesco Giammarile
Nuclear medicine has seen significant advancements in recent years, especially in the area of Positron Emission Tomography (PET) imaging. One of these innovations is the use of Fibroblast Activation Protein Inhibitors (FAPI) as a novel radiotracer. FAPI PET imaging has shown promising results in various malignancies, including sarcomas, which are a diverse group of cancers originating from mesenchymal cells. This review aims to explore the potential of FAPI PET imaging in the diagnosis, staging, and treatment monitoring of sarcomas. Several studies have demonstrated the potential of FAPI PET in sarcomas. Furthermore, FAPI PET imaging has shown potential in assessing treatment response, with changes in FAPI uptake correlating with treatment outcomes. However, there are challenges to be addressed. The heterogeneity of sarcomas, both inter- and intra-tumoral, may affect the uniformity of Fibroblast Activation Protein (FAP) expression and thus the effectiveness of FAPI PET imaging. In conclusion, the introduction of FAPI PET imaging represents a significant advancement in the field of nuclear medicine and oncology. As we continue to deepen our understanding of this novel imaging technique, it is hoped that FAPI PET imaging will play an increasingly important role in the fight against cancer. However, as with any new technology, further research is needed to fully understand the potential and limitations of FAPI PET imaging in the clinical setting.
近年来,核医学取得了重大进展,特别是在正电子发射断层扫描(PET)成像领域。其中一个创新是使用成纤维细胞活化蛋白抑制剂(FAPI)作为一种新的放射性示踪剂。FAPI PET成像在各种恶性肿瘤中显示出令人鼓舞的结果,包括肉瘤,这是一种起源于间充质细胞的不同类型的癌症。本综述旨在探讨FAPI PET成像在肉瘤的诊断、分期和治疗监测中的潜力。一些研究已经证明了FAPI PET在肉瘤中的潜力。此外,FAPI PET成像显示出评估治疗反应的潜力,FAPI摄取的变化与治疗结果相关。然而,也有一些挑战需要解决。肉瘤的异质性(肿瘤间和肿瘤内)可能影响成纤维细胞活化蛋白(FAP)表达的均匀性,从而影响FAPI PET成像的有效性。总之,FAPI PET成像的引入代表了核医学和肿瘤学领域的重大进步。随着我们对这种新型成像技术的理解不断加深,希望FAPI PET成像在与癌症的斗争中发挥越来越重要的作用。然而,与任何新技术一样,需要进一步的研究来充分了解FAPI PET成像在临床环境中的潜力和局限性。
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引用次数: 0
New Radiopharmaceutical Tools in Imaging 新放射药物成像工具。
IF 5.9 2区 医学 Q1 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING Pub Date : 2025-09-01 Epub Date: 2025-05-26 DOI: 10.1053/j.semnuclmed.2025.05.002
Dirk Bender
The strength of Nuclear Medicine imaging are the compounds to be used as radioactive probes. Unfortunately there are many constraints both in relation to physiological parameters such as metabolism as well to compound related properties like lipophilicity or chemical stability. Due these constraints, many, otherwise promising, compounds could not be used in Nuclear Medicine imaging. Within this review a brief summary is given regarding possible limitations for imaging probes and approaches or techniques to overcome the constraints. Even so the review focuses on imaging with central active compounds, many of these problems appear likewise when targeting peripheral organs. Besides the established approaches to overcome limitations some new, so far not explored, directions are discussed. Finally, a potential new tool in imaging will be presented, a trojan horse approach for transportation of radioligands. Here, like in conventional drug development, lipid nanoparticles may have potential to be used as carrier systems in Nuclear Medicine as well. This, so far not explored, concept is briefly presented.
核医学成像的强度是用来作为放射性探针的化合物。不幸的是,在生理参数(如代谢)以及化合物相关特性(如亲脂性或化学稳定性)方面存在许多限制。由于这些限制,许多原本很有前途的化合物不能用于核医学成像。在这篇综述中,简要总结了成像探针和方法或技术可能存在的局限性,以克服这些局限性。尽管这篇综述关注的是中枢活性化合物的成像,但在针对外周器官时,许多问题也同样出现。除了已建立的克服局限性的方法外,还讨论了一些迄今尚未探索的新方向。最后,将介绍一种潜在的成像新工具,一种用于放射性配体运输的特洛伊木马方法。在这里,就像在传统药物开发中一样,脂质纳米颗粒也有可能被用作核医学的载体系统。这个迄今尚未探讨的概念被简要地提出。
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Seminars in nuclear medicine
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