Zhong-Bin Hang, Hai Hu, Zi-Wei Liang, Yan Zhang, Chen-Yu Yan, Tian-Tian Zhang, Ke-Xin Wei, Ming-Zhe Song, Jing Wu, Zuo-Xiang He
{"title":"Dosimetric Development of Yttrium-90 Resin Microspheres for Selective Internal Radiation Therapy: Current Status and Perspectives","authors":"Zhong-Bin Hang, Hai Hu, Zi-Wei Liang, Yan Zhang, Chen-Yu Yan, Tian-Tian Zhang, Ke-Xin Wei, Ming-Zhe Song, Jing Wu, Zuo-Xiang He","doi":"10.1002/jlcr.70022","DOIUrl":"10.1002/jlcr.70022","url":null,"abstract":"<div>\u0000 \u0000 <p>Yttrium-90 resin microspheres selective internal radiation therapy (<span></span><math>\u0000 <semantics>\u0000 <mrow>\u0000 <msup>\u0000 <mrow></mrow>\u0000 <mrow>\u0000 <mn>90</mn>\u0000 </mrow>\u0000 </msup>\u0000 </mrow>\u0000 <annotation>$$ {}^{90} $$</annotation>\u0000 </semantics></math>Y-SIRT) has been increasingly adopted worldwide as a locoregional treatment option for appropriately selected patients with liver malignancies. The key to ensuring that the tumor receives an adequate radiation dose while minimizing the dose to normal tissues is to optimize the trade-off between tumor control and the probability of normal tissue complications. To accurately determine a patient's internal radiation dose, pre-treatment dose planning and post-treatment dose verification using dosimetric methods are recommended and increasingly considered best practice in <span></span><math>\u0000 <semantics>\u0000 <mrow>\u0000 <msup>\u0000 <mrow></mrow>\u0000 <mrow>\u0000 <mn>90</mn>\u0000 </mrow>\u0000 </msup>\u0000 </mrow>\u0000 <annotation>$$ {}^{90} $$</annotation>\u0000 </semantics></math>Y-SIRT, where feasible. Due to the increased demand for personalized treatment and dose accuracy in clinical practice, <span></span><math>\u0000 <semantics>\u0000 <mrow>\u0000 <msup>\u0000 <mrow></mrow>\u0000 <mrow>\u0000 <mn>90</mn>\u0000 </mrow>\u0000 </msup>\u0000 </mrow>\u0000 <annotation>$$ {}^{90} $$</annotation>\u0000 </semantics></math>Y-SIRT dosimetry has transitioned from organ-level to voxel-level dosimetry. This paper introduces the relevant principles and development history of <span></span><math>\u0000 <semantics>\u0000 <mrow>\u0000 <msup>\u0000 <mrow></mrow>\u0000 <mrow>\u0000 <mn>90</mn>\u0000 </mrow>\u0000 </msup>\u0000 </mrow>\u0000 <annotation>$$ {}^{90} $$</annotation>\u0000 </semantics></math>Y-SIRT dosimetry for resin microspheres. It also discusses the clinical performance, influencing factors and practical applications of relevant dosimetry methods. These include body surface area (BSA) method, MIRD multi-compartment model method, and partition model method; voxel-S-value (VSV); local deposition method (LDM); and Monte Carlo (MC) method. Finally, it covers the subsequent development of resin microsphere <span></span><math>\u0000 <semantics>\u0000 <mrow>\u0000 <msup>\u0000 <mrow></mrow>\u0000 <mrow>\u0000 <mn>90</mn>\u0000 </mrow>\u0000 ","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 3","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-03-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147344533","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Syed Qaiser Shah, Ralph Santos-Oliveira, Madeeha Shabnam, DeryaIlem-Ozdemir
{"title":"Preclinical Evaluation of [225Ac]Ac–Sibrotuzumab Employing a PEG4–Macropa Site-Specific Chelation Strategy for Targeted Ablation of Cancer-Associated Fibroblasts in Desmoplastic Tumors","authors":"Syed Qaiser Shah, Ralph Santos-Oliveira, Madeeha Shabnam, DeryaIlem-Ozdemir","doi":"10.1002/jlcr.70020","DOIUrl":"10.1002/jlcr.70020","url":null,"abstract":"<div>\u0000 \u0000 <p>Fibroblast activation protein is highly expressed in tumor-associated fibroblasts and represents a promising stromal target for cancer therapy. Actinium-225 (<sup>225</sup>Ac) offers potent α-emissions for targeted radiotherapy but requires exceptionally stable chelation. We report the synthesis and preclinical evaluation of the novel FAP-targeted α-immunoconjugate [<sup>225</sup>Ac]Ac–Macropa–PEG<sub>4</sub>–Sibrotuzumab. Sibrotuzumab was site-specifically modified with Macropa–PEG<sub>4</sub> and radiolabeled with <sup>225</sup>Ac under mild conditions. Radiochemical purity, serum stability, and immunoreactivity were assessed by radio-iTLC, SEC–HPLC, and FAP<sup>+</sup>/FAP<sup>−</sup> cell assays. In vivo biodistribution and therapeutic efficacy were evaluated in NIH/3T3-FAP<sup>+</sup> xenograft–bearing mice. The radioconjugate was obtained in 78.5% ± 2.2% yield with > 98% radiochemical purity and > 90% stability over 7 days. The immunoreactive fraction was 88.7%, and the construct demonstrated strong FAP-specific uptake with ~30% internalization at 24 h. In vivo, [<sup>225</sup>Ac]Ac–Macropa–PEG<sub>4</sub>–Sibrotuzumab showed high tumor accumulation (24.1 ± 1.6 %ID/g at 168 h), rapid clearance from normal tissues, and minimal bone uptake. Treatment achieved ~62% tumor growth inhibition, prolonged survival beyond 28 days, and induced partial (50%) or complete (17%) responses without systemic toxicity. These findings highlight Macropa as a robust chelation strategy and support Sibrotuzumab-based α-immunoconjugates for precise targeting of FAP-positive desmoplastic tumors.</p>\u0000 </div>","PeriodicalId":16288,"journal":{"name":"Journal of labelled compounds & radiopharmaceuticals","volume":"69 2","pages":""},"PeriodicalIF":0.9,"publicationDate":"2026-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146157242","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}