American journal of nuclear medicine and molecular imaging最新文献

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Visualizing T-cell activation: PET imaging of CXCL9 as a window into the tumor immune response. 可视化t细胞活化:CXCL9的PET成像作为肿瘤免疫应答的窗口。
IF 1.8
American journal of nuclear medicine and molecular imaging Pub Date : 2025-10-25 eCollection Date: 2025-01-01 DOI: 10.62347/KSFZ9854
Jimmy S Patel, Runhong Li, Steven H Liang
{"title":"Visualizing T-cell activation: PET imaging of CXCL9 as a window into the tumor immune response.","authors":"Jimmy S Patel, Runhong Li, Steven H Liang","doi":"10.62347/KSFZ9854","DOIUrl":"10.62347/KSFZ9854","url":null,"abstract":"<p><p>T-cell activation within the tumor microenvironment is a key determinant of response to immunotherapy, yet current biomarkers fail to capture its spatial and temporal dynamics. Traditional assays such as PD-L1 immunohistochemistry, tumor mutational analysis, and circulating cytokine profiling offer static or systemic snapshots that inadequately reflect localized immune engagement. Positron emission tomography (PET) provides a unique opportunity to visualize these processes <i>in vivo</i>. Among emerging tracers, CXCL9-targeted imaging stands out as a promising approach to quantify IFNγ-driven T-cell activation and recruitment. Jacobson <i>et al</i>. report the development of [<sup>18</sup>F]F-h2A12, a high-affinity nanobody PET tracer specific for CXCL9. Preclinical studies demonstrate robust uptake in CXCL9-expressing tumors, close correlation with intratumoral immune activation, and clear distinction from blood-based biomarkers. Compared with existing immune PET tracers that target cytotoxic enzymes, soluble cytokines, or surface activation markers, CXCL9 imaging offers an advantageous balance of specificity, localization, and functional relevance. By visualizing the chemokine gradients that govern T-cell trafficking, CXCL9 PET could serve as an early, noninvasive biomarker of immunotherapy response and a powerful tool for guiding adaptive treatment strategies.</p>","PeriodicalId":7572,"journal":{"name":"American journal of nuclear medicine and molecular imaging","volume":"15 5","pages":"212-214"},"PeriodicalIF":1.8,"publicationDate":"2025-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12629901/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145585956","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Radiosynthesis and evaluation of an 18F-labeled radioligand for imaging metabotropic glutamate receptor 3 with positron emission tomography. 放射性合成和评价18f标记的放射性配体对代谢性谷氨酸受体3的正电子发射断层成像。
IF 1.8
American journal of nuclear medicine and molecular imaging Pub Date : 2025-10-25 eCollection Date: 2025-01-01 DOI: 10.62347/MHBJ1846
Jian Rong, Chunyu Zhao, Ahmad F Chaudhary, Jiahui Chen, Yinlong Li, Xin Zhou, Zhendong Song, Zhenkun Sun, Yabiao Gao, Siyan Feng, Taoqian Zhao, Qi-Long Hu, Chongjiao Li, Achi Haider, Jimmy Patel, Chongzhao Ran, Hongjie Yuan, Steven H Liang
{"title":"Radiosynthesis and evaluation of an <sup>18</sup>F-labeled radioligand for imaging metabotropic glutamate receptor 3 with positron emission tomography.","authors":"Jian Rong, Chunyu Zhao, Ahmad F Chaudhary, Jiahui Chen, Yinlong Li, Xin Zhou, Zhendong Song, Zhenkun Sun, Yabiao Gao, Siyan Feng, Taoqian Zhao, Qi-Long Hu, Chongjiao Li, Achi Haider, Jimmy Patel, Chongzhao Ran, Hongjie Yuan, Steven H Liang","doi":"10.62347/MHBJ1846","DOIUrl":"10.62347/MHBJ1846","url":null,"abstract":"<p><p>The metabotropic glutamate receptor 3 (mGluR3) is a G-protein-coupled receptor (GPCR) involved in modulating glutamatergic neurotransmission and maintaining neural homeostasis. By inhibiting adenylyl cyclase activity, mGluR3 negatively modulates the activity of adenylyl cyclase via Gi/o protein coupling, reducing cyclic AMP (cAMP) levels and modulating downstream signaling pathways. Dysfunction of mGluR3 is associated with a range of neurological and psychiatric disorders, including depression, autism, cognitive impairment, bipolar affective disorder, schizophrenia, and neurodegenerative diseases. Despite its therapeutic relevance, no selective mGluR3 positron emission tomography (PET) radioligand is currently available to image this target <i>in vivo</i>. In this study, we report the radiosynthesis and preclinical evaluation of [<sup>18</sup>F]VU6010572 - a novel PET tracer based on a therapeutical drug candidate. VU6010572 exhibits potent binding affinity (IC<sub>50</sub> = 39.9 nM) and exceptional selectivity (>100-fold over other mGluR subtypes). Radiolabeling with fluorine-18 yielded [<sup>18</sup>F]VU6010572 with high radiochemical yield (48%, decay-corrected) and molar activity (59 GBq/µmol). While <i>in vitro</i> autoradiography demonstrated heterogeneous brain distribution, dynamic PET imaging in rodents revealed reasonable brain uptake <i>in vivo</i> yet modest binding specificity and rapid brain washout. While these findings support the potential of [<sup>18</sup>F]VU6010572 as a lead structure, further medicinal chemistry optimization is warranted to enhance the metabolic and pharmacokinetic properties.</p>","PeriodicalId":7572,"journal":{"name":"American journal of nuclear medicine and molecular imaging","volume":"15 5","pages":"173-182"},"PeriodicalIF":1.8,"publicationDate":"2025-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12629903/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145585949","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
DLL3-targeted immunoPET and radioimmunotherapy ligands. dll3靶向免疫pet和放射免疫治疗配体。
IF 1.8
American journal of nuclear medicine and molecular imaging Pub Date : 2025-10-25 eCollection Date: 2025-01-01 DOI: 10.62347/MRZS8767
Steven H Liang
{"title":"DLL3-targeted immunoPET and radioimmunotherapy ligands.","authors":"Steven H Liang","doi":"10.62347/MRZS8767","DOIUrl":"10.62347/MRZS8767","url":null,"abstract":"<p><p>DLL3 is overexpressed on the cell surface of NENs, such as SCLC and NEPC, but notably restricted to cytoplasm with low expression levels in normal adult human tissues. Several radioligands have been developed by targeting DLL3 for immunoPET or radioimmunotherapy use. These ligands hold great promise for mapping the heterogeneous DLL3 expression in neuroendocrine tumors and guiding the DLL3-directed therapeutic strategies.</p>","PeriodicalId":7572,"journal":{"name":"American journal of nuclear medicine and molecular imaging","volume":"15 5","pages":"215-218"},"PeriodicalIF":1.8,"publicationDate":"2025-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12629904/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145585894","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Performance of PRIMARY Score based on PSMA-PET imaging in suspected prostate cancer patients with different PSA ranges: a retrospective study. 基于PSMA-PET成像的PRIMARY评分在不同PSA范围的疑似前列腺癌患者中的表现:一项回顾性研究。
IF 1.8
American journal of nuclear medicine and molecular imaging Pub Date : 2025-10-25 eCollection Date: 2025-01-01 DOI: 10.62347/MKPM5648
Fuhao Zhang, Xiang Li, Jingliang Zhang, Zhiyong Quan, Zefei Zhang, Tingting Han, Xiaoli Meng, Lingyu Ma, Xuebing Yu, Weijun Qin, Fei Kang
{"title":"Performance of PRIMARY Score based on PSMA-PET imaging in suspected prostate cancer patients with different PSA ranges: a retrospective study.","authors":"Fuhao Zhang, Xiang Li, Jingliang Zhang, Zhiyong Quan, Zefei Zhang, Tingting Han, Xiaoli Meng, Lingyu Ma, Xuebing Yu, Weijun Qin, Fei Kang","doi":"10.62347/MKPM5648","DOIUrl":"10.62347/MKPM5648","url":null,"abstract":"<p><strong>Purpose: </strong>To refine the optimal PRIMARY score thresholds across different PSA ranges, enhancing diagnostic accuracy for clinically significant prostate cancer (csPCa).</p><p><strong>Methods: </strong>The study retrospectively analyzed 373 patients who underwent PSMA PET/CT scans for suspected csPCa between June 2021 and December 2023. The diagnostic efficacy of PRIMARY score was independently assessed using 68Ga-PSMA PET/CT. Receiver-operating characteristic curve analysis was used to estimate the diagnostic performance. The diagnostic efficacy of the PRIMARY score with different thresholds in different PSA ranges was also calculated and compared.</p><p><strong>Results: </strong>The PRIMARY score maintains high diagnostic accuracy either in group of PSA ≤ 20 ng/mL or PSA > 20 ng/mL, with an AUC exceeding 0.8 at appropriate thresholds. Notably, in patients with PSA > 20 ng/mL, a PRIMARY score threshold of 4 demonstrated enhanced diagnostic accuracy compared to a threshold of 3, significantly improving specificity from 70.6% to 91.2% while maintaining high sensitivity (from 99.2% to 98.4%). Consequently, 91.2% (31/34) patients could avoid unnecessary biopsies, at the expense of missing 1.6% (2/125) of csPCa cases.</p><p><strong>Conclusion: </strong>Across different PSA ranges, the PRIMARY score based on <sup>68</sup>Ga-PSMA PET/CT imaging is useful in the diagnosis of csPCa. A threshold of 3 for PSA ≤ 20 ng/mL and a threshold of 4 for 20 ng/mL < PSA ≤ 50 ng/mL respectively demonstrated favorable diagnostic performance.</p>","PeriodicalId":7572,"journal":{"name":"American journal of nuclear medicine and molecular imaging","volume":"15 5","pages":"200-207"},"PeriodicalIF":1.8,"publicationDate":"2025-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12629899/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145585974","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Radiosynthesis and evaluation of a carbon-11 labeled PET ligand for imaging of O-GlcNAcase. 碳-11标记PET配体对O-GlcNAcase成像的放射性合成和评价。
IF 1.8
American journal of nuclear medicine and molecular imaging Pub Date : 2025-10-25 eCollection Date: 2025-01-01 DOI: 10.62347/IVXM3055
Yinlong Li, Xin Zhou, Zhendong Song, Taoqian Zhao, Jian Rong, Jiahui Chen, Chunyu Zhao, Qilong Hu, Xiaoyan Li, Chongjiao Li, Zhenkun Sun, Yabiao Gao, Jimmy S Patel, Ahmad Chaudhary, Hongjie Yuan, Steven H Liang
{"title":"Radiosynthesis and evaluation of a carbon-11 labeled PET ligand for imaging of O-GlcNAcase.","authors":"Yinlong Li, Xin Zhou, Zhendong Song, Taoqian Zhao, Jian Rong, Jiahui Chen, Chunyu Zhao, Qilong Hu, Xiaoyan Li, Chongjiao Li, Zhenkun Sun, Yabiao Gao, Jimmy S Patel, Ahmad Chaudhary, Hongjie Yuan, Steven H Liang","doi":"10.62347/IVXM3055","DOIUrl":"10.62347/IVXM3055","url":null,"abstract":"<p><p>O-GlcNAcase (OGA) is a key enzyme involved in regulating the dynamic cycling of O-GlcNAc modifications on intracellular proteins. OGA has emerged as a promising therapeutic target for neurodegenerative diseases, including Alzheimer's disease. In this report, we present the radiosynthesis and preclinical assessment of a novel carbon-11 labeled positron emission tomography (PET) radioligand [<sup>11</sup>C]1 (codenamed OGA-2504) targeting OGA. The aminopyrimidine-based compound 1 and its corresponding desmethyl precursor were synthesized efficiently with good chemical yields. Radiosynthesis of [<sup>11</sup>C]1 was accomplished <i>via</i> <sup>11</sup>C-methylation, yielding an 8% decay-corrected radiochemical yield with high purity (>98%) and high molar activity (92.5 GBq/µmol). [<sup>11</sup>C]1 exhibited moderate lipophilicity (LogD = 2.11) and excellent <i>in vivo</i> stability in serum. However, preliminary PET imaging revealed low brain uptake and slow clearance of [<sup>11</sup>C]1 in mice, suggesting a need for further structural optimization to enhance brain penetration.</p>","PeriodicalId":7572,"journal":{"name":"American journal of nuclear medicine and molecular imaging","volume":"15 5","pages":"183-192"},"PeriodicalIF":1.8,"publicationDate":"2025-10-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12629900/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145585880","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Effect of truncating blood sampling in measuring glomerular filtration rate. 截尾采血在测定肾小球滤过率中的作用。
IF 1.8
American journal of nuclear medicine and molecular imaging Pub Date : 2025-08-15 eCollection Date: 2025-01-01 DOI: 10.62347/XDLP4069
Kenneth J Nichols, Adam Kesner, Kuldeep K Bhargava, Paige Bennett, Christopher J Palestro
{"title":"Effect of truncating blood sampling in measuring glomerular filtration rate.","authors":"Kenneth J Nichols, Adam Kesner, Kuldeep K Bhargava, Paige Bennett, Christopher J Palestro","doi":"10.62347/XDLP4069","DOIUrl":"10.62347/XDLP4069","url":null,"abstract":"<p><p>Glomerular filtration rates (GFR's) are used to guide patient management. GFR's are based on radioactivity measurements of blood samples sampled at different times. We compared GFR computations from blood collected at 6 times to those collected at 2 timepoints. Thirty-seven GFR studies were performed on 25 patients. After intravenous administration of I-125 sodium iothalamate, 6 plasma samples were obtained at 5 min, 10 min, 15 min, 3 hr, 3.5 hr and 4 hr after injection, then counted in a well counter. Two different GFR calculation tools were applied to each set of 6 plasma counts (Methods 1 and 2), and a 2-sample algorithm (Method 3) computed GFR using only 3 hr and 4 hr data. Linear correlation between Method 1 and 2 GFR's was stronger than for Method 3 versus Methods 1 and 2 (r = 1.00 versus r = .91, P < .0001). Bland-Altman limits of agreement were larger (P < .0001) for Method 3 versus Methods 1 and 2 (-39.5 to +22.0 ml/min/1.73 m<sup>2</sup>) than for Method 1 versus 2 (-7.6 to +4.5 ml/min/1.73 m<sup>2</sup>). Method 3 overestimated lower GFR's and underestimated higher GFR's. Methods 1 and 2 agreed exactly in identifying 3 cases of GFR < 74 ml/min/1.73 m<sup>2</sup> (κ = 1.00), while Method 3 detected only 1 of the three (κ = .48). To avoid underdiagnosing low GFR's, larger GFR sample sizes are preferable to smaller sample sizes.</p>","PeriodicalId":7572,"journal":{"name":"American journal of nuclear medicine and molecular imaging","volume":"15 4","pages":"140-145"},"PeriodicalIF":1.8,"publicationDate":"2025-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12444398/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145111809","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Advancing patient education in PRRT through large language models: challenges and potential. 通过大型语言模型推进PRRT患者教育:挑战和潜力。
IF 1.8
American journal of nuclear medicine and molecular imaging Pub Date : 2025-08-15 eCollection Date: 2025-01-01 DOI: 10.62347/OAHP6281
Tilman Speicher, Moritz B Bastian, Arne Blickle, Armin Atzinger, Florian Rosar, Caroline Burgard, Samer Ezziddin
{"title":"Advancing patient education in PRRT through large language models: challenges and potential.","authors":"Tilman Speicher, Moritz B Bastian, Arne Blickle, Armin Atzinger, Florian Rosar, Caroline Burgard, Samer Ezziddin","doi":"10.62347/OAHP6281","DOIUrl":"10.62347/OAHP6281","url":null,"abstract":"<p><p>The increasing use of artificial intelligence (AI) chatbots for patient education raises questions about their accuracy, readability, and conciseness in delivering medical information. This study evaluates the performance of ChatGPT 4o and DeepSeek V3 in answering common patient inquiries about Peptide Receptor Radionuclide Therapy (PRRT). Twelve frequently asked patient questions regarding PRRT were submitted to both chatbots. The responses were assessed by nine professionals using a blinded survey, scoring accuracy, conciseness, and readability on a five-point scale. Statistical analyses included the Mann-Whitney U test for nonparametric data and the Chi-square test for medically incorrect responses. A total of 324 individual assessments were conducted. No significant differences were found in accuracy between ChatGPT 4o (mean 4.43) and DeepSeek V3 (mean 4.56; <i>P</i> = 0.0909) or in readability between ChatGPT 4o (mean 4.38) and DeepSeek V3 (mean 4.25; <i>P</i> = 0.1236). However, ChatGPT 4o provided significantly more concise responses (mean 4.55) compared to DeepSeek V3 (mean 4.24; <b><i>P</i> = 0.0013</b>). Medically incorrect information defined as accuracy ≤ 3 was present in 7-8% of chatbot responses, with no significant difference between the two models (<i>P</i> = 0.8005). Both AI chatbots demonstrated strong performance in providing medical information on PRRT, with ChatGPT 4o excelling in conciseness. However, the presence of medical inaccuracies highlights the need for physician oversight when using AI chatbots for patient education. Future research should explore methods to enhance AI reliability and personalization in clinical communication.</p>","PeriodicalId":7572,"journal":{"name":"American journal of nuclear medicine and molecular imaging","volume":"15 4","pages":"146-152"},"PeriodicalIF":1.8,"publicationDate":"2025-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12444397/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145111815","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
18F-NaF PET/CT for early detection of osteoporosis in the lumbar spine: two case reports. 18F-NaF PET/CT早期发现腰椎骨质疏松症2例报告
IF 1.8
American journal of nuclear medicine and molecular imaging Pub Date : 2025-08-15 eCollection Date: 2025-01-01 DOI: 10.62347/IXKG9158
Shiv Patil, Nirmal Patel, Eric Teichner, William Lee, Ehsan Ranjbar, Alexander Gerlach, Robert Subtirelu, Lancelot Herpin, Thomas Werner, Poul Flemming Høilund-Carlsen, Abass Alavi
{"title":"<sup>18</sup>F-NaF PET/CT for early detection of osteoporosis in the lumbar spine: two case reports.","authors":"Shiv Patil, Nirmal Patel, Eric Teichner, William Lee, Ehsan Ranjbar, Alexander Gerlach, Robert Subtirelu, Lancelot Herpin, Thomas Werner, Poul Flemming Høilund-Carlsen, Abass Alavi","doi":"10.62347/IXKG9158","DOIUrl":"10.62347/IXKG9158","url":null,"abstract":"<p><p>Osteoporosis is a highly prevalent skeletal disease involving a pathophysiology of altered bone turnover. Positron emission tomography (PET)/computed tomography (CT) imaging with <sup>18</sup>F-sodium fluoride (NaF) can visualize metabolic alterations in bone that precede clinical manifestations or structural alterations and thus may serve a role in the early detection and monitoring of osteoporosis. We present two non-oncological case reports demonstrating different metabolic changes in early and advanced disease stages as assessed by <sup>18</sup>F-NaF PET/CT that cannot be appreciated by conventional structural imaging alone, supporting a potential clinical application of <sup>18</sup>F-NaF PET/CT for early detection and monitoring of osteoporosis in the lumbar spine.</p>","PeriodicalId":7572,"journal":{"name":"American journal of nuclear medicine and molecular imaging","volume":"15 4","pages":"153-157"},"PeriodicalIF":1.8,"publicationDate":"2025-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12444402/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145111795","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Dual-receptor PET imaging of ovarian cancer using a 68Ga-labeled heterodimer targeting folate receptor and HER2. 使用靶向叶酸受体和HER2的68ga标记异二聚体对卵巢癌进行双受体PET成像。
IF 1.8
American journal of nuclear medicine and molecular imaging Pub Date : 2025-08-15 eCollection Date: 2025-01-01 DOI: 10.62347/IRKD4863
Xiaodan Shi, Zhangxin Wu, Yifeng Yuan, Ying Wang, Shuo Yang, Rong Li
{"title":"Dual-receptor PET imaging of ovarian cancer using a <sup>68</sup>Ga-labeled heterodimer targeting folate receptor and HER2.","authors":"Xiaodan Shi, Zhangxin Wu, Yifeng Yuan, Ying Wang, Shuo Yang, Rong Li","doi":"10.62347/IRKD4863","DOIUrl":"10.62347/IRKD4863","url":null,"abstract":"<p><p>Radiolabeled folate derivatives have been extensively investigated for positron emission tomography (PET) imaging of ovarian cancer due to the frequent overexpression of folate receptor α (FRα). However, clinical translation has been hindered, at least in part, by suboptimal tumor uptake of FRα-targeted radiotracers. In this study, we developed and characterized a <sup>68</sup>Ga-labeled heterodimeric radiotracer, <sup>68</sup>Ga-folate-KR, designed to concurrently target FRα and human epidermal growth factor receptor 2 (HER2), another receptor commonly overexpressed in ovarian cancer. Transcriptomics analysis confirmed the co-upregulation of <i>FOLR1</i> and <i>HER2</i> in ovarian cancer tissues relative to normal ovarian tissue, supporting the rationale for dual-receptor targeting. In vitro binding assays demonstrated specific binding of <sup>68</sup>Ga-folate-KR to both receptors. PET imaging and biodistribution studies in SKOV3 tumor-bearing mice revealed significantly enhanced tumor uptake and improved tumor-to-nontumor contrast compared to the monomeric radiotracers <sup>68</sup>Ga-folate and <sup>68</sup>Ga-KR. Competitive blocking experiments further confirmed the in vivo dual-receptor targeting capability of <sup>68</sup>Ga-folate-KR. Collectively, our results highlight that <sup>68</sup>Ga-folate-KR enables more sensitive PET detection of ovarian cancer xenografts. With further optimization, dual-receptor-targeted radiotracers hold promise for clinical translation in both lesion detection and therapy response monitoring in ovarian cancer.</p>","PeriodicalId":7572,"journal":{"name":"American journal of nuclear medicine and molecular imaging","volume":"15 4","pages":"130-139"},"PeriodicalIF":1.8,"publicationDate":"2025-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12444400/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145111773","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Streamlining first-in-human PET radiopharmaceutical development: FDA's evolving stance on preclinical dosimetry. 简化首次人体PET放射性药物开发:FDA在临床前剂量学方面的演变立场。
IF 1.8
American journal of nuclear medicine and molecular imaging Pub Date : 2025-08-15 eCollection Date: 2025-01-01 DOI: 10.62347/KJLM2547
Taoqian Zhao, Steven H Liang
{"title":"Streamlining first-in-human PET radiopharmaceutical development: FDA's evolving stance on preclinical dosimetry.","authors":"Taoqian Zhao, Steven H Liang","doi":"10.62347/KJLM2547","DOIUrl":"10.62347/KJLM2547","url":null,"abstract":"<p><p>The U.S. Food and Drug Administration (FDA) has proposed a regulatory shift in the early-phase development of positron emission tomography (PET) radiopharmaceuticals, specifically regarding the requirement for animal-based dosimetry in first-in-human (FIH) studies. This editorial discusses the implications of the FDA's recent Advisory Committee briefing, which supports the omission of preclinical dosimetry under defined conditions for radiopharmaceuticals labeled with <sup>18</sup>F, <sup>11</sup>C, <sup>68</sup>Ga, <sup>64</sup>Cu, <sup>82</sup>Rb, and <sup>13</sup>N. The proposed policy reflects a shift toward a more streamlined, evidence-based approach to FIH studies while maintaining stringent standards for patient safety.</p>","PeriodicalId":7572,"journal":{"name":"American journal of nuclear medicine and molecular imaging","volume":"15 4","pages":"171-172"},"PeriodicalIF":1.8,"publicationDate":"2025-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12444401/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145111741","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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