{"title":"具有骨靶向活性的131i -利塞膦酸盐的合成及生物学评价","authors":"Zehui Lin, Wangxi Hai, Pengfei Pan, Jin-Hong Lin, Biao Li, Ji-Chang Xiao","doi":"10.1021/acs.molpharmaceut.5c00300","DOIUrl":null,"url":null,"abstract":"<p><p>Current radiopharmaceuticals for treating bone metastatic tumors have various limitations. We focus on developing a universal, economical, efficient, and safe novel radiopharmaceutical for bone metastasis treatment. <sup>131</sup>I is a well-established medical radionuclide commonly used for both treatment and diagnosis. Risedronate exhibits strong bone-targeting properties with moderate bone retention. This study explored the combination of these two components and evaluated its biological properties in animal experiments. Based on the experimental results, <sup>131</sup>I-risedronate demonstrated high bone-targeting efficiency, low uptake in nontarget organs, and rapid clearance. Notably, at 3 days postadministration, significant bone retention was observed, indicating its potential for sustained therapeutic effects. Additionally, its biodistribution and therapeutic effect can be effectively monitored by SPECT/CT imaging.</p>","PeriodicalId":52,"journal":{"name":"Molecular Pharmaceutics","volume":" ","pages":""},"PeriodicalIF":4.5000,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis and Biological Evaluation of <sup>131</sup>I-Risedronate with Bone Targeting Activity.\",\"authors\":\"Zehui Lin, Wangxi Hai, Pengfei Pan, Jin-Hong Lin, Biao Li, Ji-Chang Xiao\",\"doi\":\"10.1021/acs.molpharmaceut.5c00300\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Current radiopharmaceuticals for treating bone metastatic tumors have various limitations. We focus on developing a universal, economical, efficient, and safe novel radiopharmaceutical for bone metastasis treatment. <sup>131</sup>I is a well-established medical radionuclide commonly used for both treatment and diagnosis. Risedronate exhibits strong bone-targeting properties with moderate bone retention. This study explored the combination of these two components and evaluated its biological properties in animal experiments. Based on the experimental results, <sup>131</sup>I-risedronate demonstrated high bone-targeting efficiency, low uptake in nontarget organs, and rapid clearance. Notably, at 3 days postadministration, significant bone retention was observed, indicating its potential for sustained therapeutic effects. Additionally, its biodistribution and therapeutic effect can be effectively monitored by SPECT/CT imaging.</p>\",\"PeriodicalId\":52,\"journal\":{\"name\":\"Molecular Pharmaceutics\",\"volume\":\" \",\"pages\":\"\"},\"PeriodicalIF\":4.5000,\"publicationDate\":\"2025-05-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Molecular Pharmaceutics\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1021/acs.molpharmaceut.5c00300\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"MEDICINE, RESEARCH & EXPERIMENTAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Molecular Pharmaceutics","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1021/acs.molpharmaceut.5c00300","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"MEDICINE, RESEARCH & EXPERIMENTAL","Score":null,"Total":0}
Synthesis and Biological Evaluation of 131I-Risedronate with Bone Targeting Activity.
Current radiopharmaceuticals for treating bone metastatic tumors have various limitations. We focus on developing a universal, economical, efficient, and safe novel radiopharmaceutical for bone metastasis treatment. 131I is a well-established medical radionuclide commonly used for both treatment and diagnosis. Risedronate exhibits strong bone-targeting properties with moderate bone retention. This study explored the combination of these two components and evaluated its biological properties in animal experiments. Based on the experimental results, 131I-risedronate demonstrated high bone-targeting efficiency, low uptake in nontarget organs, and rapid clearance. Notably, at 3 days postadministration, significant bone retention was observed, indicating its potential for sustained therapeutic effects. Additionally, its biodistribution and therapeutic effect can be effectively monitored by SPECT/CT imaging.
期刊介绍：
Molecular Pharmaceutics publishes the results of original research that contributes significantly to the molecular mechanistic understanding of drug delivery and drug delivery systems. The journal encourages contributions describing research at the interface of drug discovery and drug development.
Scientific areas within the scope of the journal include physical and pharmaceutical chemistry, biochemistry and biophysics, molecular and cellular biology, and polymer and materials science as they relate to drug and drug delivery system efficacy. Mechanistic Drug Delivery and Drug Targeting research on modulating activity and efficacy of a drug or drug product is within the scope of Molecular Pharmaceutics. Theoretical and experimental peer-reviewed research articles, communications, reviews, and perspectives are welcomed.
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