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Open AccessReview

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

1
German Cancer Research Center (DKFZ), Division of Radiopharmaceutical Chemistry, Im Neuenheimer Feld 280, 69120 Heidelberg, Germany
2
German Cancer Consortium (DKTK), Im Neuenheimer Feld 280, 69120 Heidelberg, Germany
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2019, 12(3), 114; https://doi.org/10.3390/ph12030114
Received: 1 July 2019 / Revised: 23 July 2019 / Accepted: 26 July 2019 / Published: 29 July 2019
(This article belongs to the Special Issue The Story of Successful Drugs and Recent FDA-Approved Molecules)
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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 177Lu 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. View Full-Text
Keywords: Lutathera®, [177Lu]Lu-DOTA-TATE; thera(g)nostics; peptide receptor radionuclide therapy (PRRT); somatostatin receptor (SSTR); neuroendocrine tumors (NET) Lutathera®, [177Lu]Lu-DOTA-TATE; thera(g)nostics; peptide receptor radionuclide therapy (PRRT); somatostatin receptor (SSTR); neuroendocrine tumors (NET)
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Hennrich, U.; Kopka, K. Lutathera®: The First FDA- and EMA-Approved Radiopharmaceutical for Peptide Receptor Radionuclide Therapy. Pharmaceuticals 2019, 12, 114.

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