• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

用于人类骨痛缓解治疗试验的（177）镥-乙二胺四甲叉膦酸的生产、质量控制及药代动力学研究

Production, Quality Control and Pharmacokinetic Studies of (177)Lu-EDTMP for Human Bone Pain Palliation Therapy Trials.

作者信息

Bahrami-Samani Ali, Anvari Akbar, Jalilian Amir Reza, Shirvani-Arani Simindokht, Yousefnia Hassan, Aghamiri Mahmoud Reza, Ghannadi-Maragheh Mohammad

机构信息

Radiopharmaceutical Research and Development Lab (RRDL), Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran.

Department of Radiation Medicine, Engineering Shahid Beheshti University, Tehran, Iran.

出版信息

Iran J Pharm Res. 2012 Winter;11(1):137-44.

PMID:25317195
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3876567/
Abstract

Developing new bone pain palliation agents is a mandate in handling end-stage cancer patients around the world. Possibly, Lu-177 ethylenediaminetetramethylene phosphonic acid ((177)Lu-EDTMP) is a therapeutic agent which can be widely used in bone palliation therapy. In this study, (177)Lu-EDTMP complex was prepared successfully using synthesized EDTMP ligand and (177)LuCl3. Lu-177 chloride was obtained by thermal neutron irradiation (4 × 10(13) n.cm(-2)s(-1)) of natural Lu2O3 samples. Radiochemical purity of (177)Lu-EDTMP was determined by ITLC (more than 99%). Stability studies of the final preparations in the presence of human serum were performed. The biodistribution of (177)Lu-EDTMP and (177)LuCl3 in wild-type rats was studied by SPECT imaging. A comparative accumulation study for (177)Lu-EDTMP and (177)LuCl3 was performed for vital organs up to 7 days. The complex was obtained in high radiochemical purity (more than 99%). The complex was stable in vitro in presence of human serum as well as final formulation. Significant bone uptake (> 70%) was observed for the radiopharmaceutical. Due to better physical properties of Lu-177 compared to Sm-153 and acceptable biodistribution results of the compound, (177)Lu-EDTMP seemed to be an interesting new candidate for clinical trials for bone pain palliation therapy.

摘要

开发新的骨痛缓解剂是全球范围内治疗晚期癌症患者的一项任务。Lu-177乙二胺四亚甲基膦酸（(177)Lu-EDTMP）可能是一种可广泛用于骨缓解治疗的治疗剂。在本研究中，使用合成的EDTMP配体和(177)LuCl3成功制备了(177)Lu-EDTMP络合物。通过天然Lu2O3样品的热中子辐照（4×10(13) n·cm(-2)s(-1)）获得氯化镥-177。通过ITLC测定(177)Lu-EDTMP的放射化学纯度（超过99%）。对最终制剂在人血清存在下进行稳定性研究。通过SPECT成像研究了(177)Lu-EDTMP和(177)LuCl3在野生型大鼠体内的生物分布。对(177)Lu-EDTMP和(177)LuCl3在重要器官中的累积情况进行了长达7天的比较研究。该络合物以高放射化学纯度（超过99%）获得。该络合物在人血清存在下以及最终制剂中在体外是稳定的。观察到该放射性药物在骨中的摄取量显著（>70%）。由于与钐-153相比，镥-177具有更好的物理性质，且该化合物的生物分布结果可接受，(177)Lu-EDTMP似乎是骨痛缓解治疗临床试验中一个有吸引力的新候选药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3119/3876567/5462e025d124/IJPR-011-137-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3119/3876567/9632b959c052/IJPR-011-137-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3119/3876567/980a905d49b4/IJPR-011-137-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3119/3876567/6d31dd2204e7/IJPR-011-137-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3119/3876567/f9b555845bbf/IJPR-011-137-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3119/3876567/812b9a61f0f0/IJPR-011-137-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3119/3876567/5462e025d124/IJPR-011-137-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3119/3876567/9632b959c052/IJPR-011-137-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3119/3876567/980a905d49b4/IJPR-011-137-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3119/3876567/6d31dd2204e7/IJPR-011-137-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3119/3876567/f9b555845bbf/IJPR-011-137-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3119/3876567/812b9a61f0f0/IJPR-011-137-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3119/3876567/5462e025d124/IJPR-011-137-g006.jpg

相似文献

1
Production, Quality Control and Pharmacokinetic Studies of (177)Lu-EDTMP for Human Bone Pain Palliation Therapy Trials.用于人类骨痛缓解治疗试验的（177）镥-乙二胺四甲叉膦酸的生产、质量控制及药代动力学研究
Iran J Pharm Res. 2012 Winter;11(1):137-44.
2
Formulation, preclinical evaluation, and preliminary clinical investigation of an in-house freeze-dried EDTMP kit suitable for the preparation of 177Lu-EDTMP.适用于制备177Lu-EDTMP的自制冻干EDTMP试剂盒的配方、临床前评估及初步临床研究
Cancer Biother Radiopharm. 2014 Dec;29(10):412-21. doi: 10.1089/cbr.2014.1664.
3
Production, quality control and pharmacokinetic studies of Ho-EDTMP for therapeutic applications.用于治疗应用的钬-乙二胺四甲叉膦酸（Ho-EDTMP）的生产、质量控制和药代动力学研究。
Sci Pharm. 2010 Jul-Sep;78(3):423-33. doi: 10.3797/scipharm.1004-21. Epub 2010 Jun 9.
4
Absorbed dose assessment of (177)Lu-zoledronate and (177)Lu-EDTMP for human based on biodistribution data in rats.基于大鼠生物分布数据对人用（177）镥-唑来膦酸盐和（177）镥-乙二胺四甲基膦酸的吸收剂量评估。
J Med Phys. 2015 Apr-Jun;40(2):102-8. doi: 10.4103/0971-6203.158694.
5
Multispecies animal investigation on biodistribution, pharmacokinetics and toxicity of 177Lu-EDTMP, a potential bone pain palliation agent.多物种动物研究 177Lu-EDTMP 的生物分布、药代动力学和毒性，这是一种有潜力的骨痛缓解药物。
Nucl Med Biol. 2010 Feb;37(2):215-26. doi: 10.1016/j.nucmedbio.2009.09.004. Epub 2009 Nov 12.
6
(170)Tm-EDTMP: a potential cost-effective alternative to (89)SrCl(2) for bone pain palliation.（170）铥-乙二胺四甲撑膦酸：一种在缓解骨痛方面可能比（89）氯化锶更具成本效益的替代物。
Nucl Med Biol. 2009 Jul;36(5):561-8. doi: 10.1016/j.nucmedbio.2009.02.002. Epub 2009 May 7.
7
Synthesis and Ready to Use Kit Formulation of EDTMP for the Preparation of 177Lu-EDTMP as a Bone Palliation Radiopharmaceutical.EDTMP 的合成及即用试剂盒配方，用于制备 177Lu-EDTMP 作为骨缓解放射性药物。
Curr Radiopharm. 2023;16(1):38-43. doi: 10.2174/1874471015666220721095938.
8
Production, quality control, biodistribution assessment and preliminary dose evaluation of (177)Lu-PDTMP as a possible bone palliative agent.（177）Lu-PDTMP作为一种可能的骨姑息治疗药物的生产、质量控制、生物分布评估及初步剂量评估
Nucl Med Commun. 2014 Jan;35(1):99-107. doi: 10.1097/MNM.0000000000000018.
9
177Lu-EDTMP: a viable bone pain palliative in skeletal metastasis.177镥-乙二胺四甲基膦酸：一种治疗骨转移引起骨痛的可行姑息治疗药物。
Cancer Biother Radiopharm. 2008 Apr;23(2):202-13. doi: 10.1089/cbr.2007.374.
10
Production, biodistribution assessment and dosimetric evaluation of (177)Lu-TTHMP as an agent for bone pain palliation.作为缓解骨痛药物的（177）镥-三亚乙基四胺六甲基膦酸的制备、生物分布评估及剂量学评价
Asia Ocean J Nucl Med Biol. 2015 Winter;3(1):35-42.

引用本文的文献

1
IGF2BP3 Modulates mRNA Splicing and Stability to Promote Trophoblast Progression via Interaction with PDE3A and Suppression by miR-196a-5p in Preeclampsia.IGF2BP3通过与PDE3A相互作用调节mRNA剪接和稳定性以促进滋养层细胞进展，并在子痫前期中受到miR-196a-5p的抑制。
Biomedicines. 2025 May 22;13(6):1268. doi: 10.3390/biomedicines13061268.
2
Photopharmacological Applications for Cherenkov Radiation Generated by Clinically Used Radionuclides.临床应用放射性核素产生的切伦科夫辐射的光药理学应用
Int J Mol Sci. 2021 Aug 20;22(16):9010. doi: 10.3390/ijms22169010.
3
Progress in Targeted Alpha-Particle-Emitting Radiopharmaceuticals as Treatments for Prostate Cancer Patients with Bone Metastases.

本文引用的文献

1
Ethylene diamine tetramethylene phosphonic acid labeled with various β(-)-emitting radiometals: labeling optimization and animal biodistribution.乙二胺四亚甲基膦酸标记各种β(-)发射放射性金属：标记优化及动物生物分布。
Cancer Biother Radiopharm. 2011 Apr;26(2):159-64. doi: 10.1089/cbr.2010.0846. Epub 2011 Apr 21.
2
Multispecies animal investigation on biodistribution, pharmacokinetics and toxicity of 177Lu-EDTMP, a potential bone pain palliation agent.多物种动物研究 177Lu-EDTMP 的生物分布、药代动力学和毒性，这是一种有潜力的骨痛缓解药物。
Nucl Med Biol. 2010 Feb;37(2):215-26. doi: 10.1016/j.nucmedbio.2009.09.004. Epub 2009 Nov 12.
3
针对前列腺癌骨转移患者的靶向 α 粒子放射性药物治疗的进展。
Molecules. 2021 Apr 9;26(8):2162. doi: 10.3390/molecules26082162.
4
Bone-Seeking Matrix Metalloproteinase-2 Inhibitors Prevent Bone Metastatic Breast Cancer Growth.趋骨性基质金属蛋白酶-2抑制剂可预防骨转移性乳腺癌的生长。
Mol Cancer Ther. 2017 Mar;16(3):494-505. doi: 10.1158/1535-7163.MCT-16-0315-T. Epub 2017 Jan 9.
5
Production, biodistribution assessment and dosimetric evaluation of (177)Lu-TTHMP as an agent for bone pain palliation.作为缓解骨痛药物的（177）镥-三亚乙基四胺六甲基膦酸的制备、生物分布评估及剂量学评价
Asia Ocean J Nucl Med Biol. 2015 Winter;3(1):35-42.
6
Absorbed dose assessment of (177)Lu-zoledronate and (177)Lu-EDTMP for human based on biodistribution data in rats.基于大鼠生物分布数据对人用（177）镥-唑来膦酸盐和（177）镥-乙二胺四甲基膦酸的吸收剂量评估。
J Med Phys. 2015 Apr-Jun;40(2):102-8. doi: 10.4103/0971-6203.158694.
7
Metastatic Bone Pain Palliation using (177)Lu-Ethylenediaminetetramethylene Phosphonic Acid.使用（177）镥-乙二胺四亚甲基膦酸缓解转移性骨痛
World J Nucl Med. 2015 May-Aug;14(2):109-15. doi: 10.4103/1450-1147.157124.
8
(175)Yb-TTHMP as a good candidate for bone pain palliation and substitute of other radiopharmaceuticals.（175）镱-四甲基戊二酸钇作为缓解骨痛的良好候选药物及其他放射性药物的替代品。
Indian J Nucl Med. 2014 Jul;29(3):135-9. doi: 10.4103/0972-3919.136555.
9
Radiosynthesis and Quality Control of [(67)Ga]-3,4-dimethoxylated Porphyrin Complex as a Possible Imaging agent.[(67)Ga]-3,4-二甲氧基卟啉配合物作为一种潜在显像剂的放射性合成及质量控制
Iran J Pharm Res. 2013 Fall;12(4):735-44.
Peptide receptor therapies in neuroendocrine tumors.
神经内分泌肿瘤的肽受体疗法
J Endocrinol Invest. 2009 Apr;32(4):360-9. doi: 10.1007/BF03345728.
4
Preparation and preliminary studies on 177Lu-labeled hydroxyapatite particles for possible use in the therapy of liver cancer.用于肝癌治疗的¹⁷⁷镥标记羟基磷灰石颗粒的制备及初步研究
Nucl Med Biol. 2008 Jul;35(5):589-97. doi: 10.1016/j.nucmedbio.2008.03.003.
5
177Lu-EDTMP: a viable bone pain palliative in skeletal metastasis.177镥-乙二胺四甲基膦酸：一种治疗骨转移引起骨痛的可行姑息治疗药物。
Cancer Biother Radiopharm. 2008 Apr;23(2):202-13. doi: 10.1089/cbr.2007.374.
6
Preparation and preliminary biological evaluation of 177Lu-labelled hydroxyapatite as a promising agent for radiation synovectomy of small joints.177Lu标记的羟基磷灰石作为小关节放射性滑膜切除的有前景药物的制备及初步生物学评价
Nucl Med Commun. 2006 Aug;27(8):661-8. doi: 10.1097/00006231-200608000-00008.
7
177Lu-antibody conjugates for single-cell kill of B-lymphoma cells in vitro and for therapy of micrometastases in vivo.用于体外单细胞杀伤B淋巴瘤细胞及体内微转移灶治疗的177Lu抗体偶联物
Nucl Med Biol. 2005 Apr;32(3):269-78. doi: 10.1016/j.nucmedbio.2005.01.003.
8
Complexation of ytterbium to human transferrin and its uptake by K562 cells.
Eur J Biochem. 2002 Dec;269(24):6082-90. doi: 10.1046/j.1432-1033.2002.03326.x.
9
Therapy of metastatic bone pain.转移性骨痛的治疗。
J Nucl Med. 2001 Jun;42(6):895-906.
10
Samarium-153-EDTMP biodistribution and dosimetry estimation.钐-153-乙二胺四甲基膦酸的生物分布及剂量学估算。
J Nucl Med. 1993 Jul;34(7):1031-6.