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镥[177Lu]奥曲肽：首个获美国食品药品监督管理局和欧洲药品管理局批准用于肽受体放射性核素治疗的放射性药物。

Lutathera: The First FDA- and EMA-Approved Radiopharmaceutical for Peptide Receptor Radionuclide Therapy.

作者信息

Hennrich Ute, Kopka Klaus

机构信息

German Cancer Research Center (DKFZ), Division of Radiopharmaceutical Chemistry, Im Neuenheimer Feld 280, 69120 Heidelberg, Germany.

German Cancer Consortium (DKTK), Im Neuenheimer Feld 280, 69120 Heidelberg, Germany.

出版信息

Pharmaceuticals (Basel). 2019 Jul 29;12(3):114. doi: 10.3390/ph12030114.

DOI:10.3390/ph12030114
PMID:31362406
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6789871/
Abstract

As the first radiopharmaceutical for Peptide Receptor Radionuclide Therapy (PRRT), Lutathera was approved by the EMA in 2017 and the FDA in 2018 for the treatment of somatostatin receptor (SSTR) positive gastroenteropancreatic neuroendocrine tumors. Using the concept of PRRT, Lutathera combines the radionuclide Lu with the somatostatin analogue DOTA-TATE, thus delivering ionizing radiation specifically to tumor cells expressing somatostatin receptors. As a result, DNA single- and double-strand breaks are provoked, in case of double-strand breaks leading to cell death of the tumor and its SSTR-positive lesions.

摘要

作为首个用于肽受体放射性核素治疗（PRRT）的放射性药物，Lutathera于2017年获欧洲药品管理局（EMA）批准，并于2018年获美国食品药品监督管理局（FDA）批准，用于治疗生长抑素受体（SSTR）阳性的胃肠胰神经内分泌肿瘤。Lutathera运用PRRT的概念，将放射性核素镥与生长抑素类似物DOTA-TATE相结合，从而将电离辐射特异性地传递至表达生长抑素受体的肿瘤细胞。结果，引发了DNA单链和双链断裂，若出现双链断裂，则会导致肿瘤及其SSTR阳性病灶的细胞死亡。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7631/6789871/79a662ac3439/pharmaceuticals-12-00114-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7631/6789871/a9c4450dea03/pharmaceuticals-12-00114-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7631/6789871/79a662ac3439/pharmaceuticals-12-00114-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7631/6789871/a9c4450dea03/pharmaceuticals-12-00114-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7631/6789871/79a662ac3439/pharmaceuticals-12-00114-g002.jpg

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[1]
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[5]
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[6]
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[10]
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本文引用的文献

[1]
An introduction to the clinical practice of theranostics in oncology.

Br J Radiol. 2018-11

[2]
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[3]
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Radiat Environ Biophys. 2018-3

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Nucl Med Biol. 2017-12

[5]
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J Nucl Med. 2017-9

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J Nucl Med. 2017-7

[7]
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N Engl J Med. 2017-1-12

[8]
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Asia Ocean J Nucl Med Biol. 2015

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Biomed Res Int. 2015

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Cancer Biother Radiopharm. 2015-3

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