In vitro dose-response comparison of [177Lu]Lu-labelled somatostatin receptor agonist and antagonist

Giulia Tamborino; Marijke De Saint-Hubert; Lara Struelens; Simone Dalm; Eline A.M. Ruigrok; Marion de Jong; Julie Nonnekens; Mark W. Konijnenberg

doi:10.1007/s00259-019-04486-2

In vitro dose-response comparison of [177Lu]Lu-labelled somatostatin receptor agonist and antagonist

Giulia Tamborino, Marijke De Saint-Hubert, Lara Struelens, Simone Dalm, Eline A.M. Ruigrok, Marion de Jong, Julie Nonnekens, Mark W. Konijnenberg

Research output › peer-review

Abstract

Peptide receptor radionuclide therapy (PRRT) using radiolabeled somatostatin receptor (SST) is very effective for treatment of neuroendocrine metastatic tumors. Recent studies indicate that radiolabeled SST antagonists show better tumor targeting during clinical imaging and preclinical therapy, despite little to no internalization in the cancer cells. However, preclinical studies are often limited to activity uptake, with no correlation between the delivered absorbed dose and the biological end-point. This study aims to calculate the absorbed dose to the nucleus for [177Lu]Lu-DOTA-Tyr3,octreotate (177Lu-DOTA-TATE, SST agonist) and [177Lu]Lu-DOTA-JR11 (177Lu- DOTA-JR11, SST antagonist), for comparison with DNA damage induction.

Original language	English
Title of host publication	Annual Congress of the European Association of Nuclear Medicine October 12 – 16, 2019 Barcelona, Spain
Subtitle of host publication	European Journal of Nuclear Medicine and Molecular Imaging volume
Pages	S83-S84
Number of pages	2
Volume	46
Edition	2019
DOIs	https://doi.org/10.1007/s00259-019-04486-2
State	Published - 16 Oct 2019

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Cite this

Tamborino, G., De Saint-Hubert, M., Struelens, L., Dalm, S., Ruigrok, E. A. M., de Jong, M., Nonnekens, J., & Konijnenberg, M. W. (2019). In vitro dose-response comparison of [177Lu]Lu-labelled somatostatin receptor agonist and antagonist. In Annual Congress of the European Association of Nuclear Medicine October 12 – 16, 2019 Barcelona, Spain: European Journal of Nuclear Medicine and Molecular Imaging volume (2019 ed., Vol. 46, pp. S83-S84) https://doi.org/10.1007/s00259-019-04486-2

Tamborino, Giulia ; De Saint-Hubert, Marijke ; Struelens, Lara et al. / In vitro dose-response comparison of [177Lu]Lu-labelled somatostatin receptor agonist and antagonist. Annual Congress of the European Association of Nuclear Medicine October 12 – 16, 2019 Barcelona, Spain: European Journal of Nuclear Medicine and Molecular Imaging volume . Vol. 46 2019. ed. 2019. pp. S83-S84

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title = "In vitro dose-response comparison of [177Lu]Lu-labelled somatostatin receptor agonist and antagonist",

abstract = "Peptide receptor radionuclide therapy (PRRT) using radiolabeled somatostatin receptor (SST) is very effective for treatment of neuroendocrine metastatic tumors. Recent studies indicate that radiolabeled SST antagonists show better tumor targeting during clinical imaging and preclinical therapy, despite little to no internalization in the cancer cells. However, preclinical studies are often limited to activity uptake, with no correlation between the delivered absorbed dose and the biological end-point. This study aims to calculate the absorbed dose to the nucleus for [177Lu]Lu-DOTA-Tyr3,octreotate (177Lu-DOTA-TATE, SST agonist) and [177Lu]Lu-DOTA-JR11 (177Lu- DOTA-JR11, SST antagonist), for comparison with DNA damage induction.",

keywords = "Double strand breaks, Targeted Radionuclide Therapy, Dose-response",

author = "Giulia Tamborino and {De Saint-Hubert}, Marijke and Lara Struelens and Simone Dalm and Ruigrok, {Eline A.M.} and {de Jong}, Marion and Julie Nonnekens and Konijnenberg, {Mark W.}",

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Tamborino, G , De Saint-Hubert, M , Struelens, L, Dalm, S, Ruigrok, EAM, de Jong, M, Nonnekens, J & Konijnenberg, MW 2019, In vitro dose-response comparison of [177Lu]Lu-labelled somatostatin receptor agonist and antagonist. in Annual Congress of the European Association of Nuclear Medicine October 12 – 16, 2019 Barcelona, Spain: European Journal of Nuclear Medicine and Molecular Imaging volume . 2019 edn, vol. 46, pp. S83-S84. https://doi.org/10.1007/s00259-019-04486-2

In vitro dose-response comparison of [177Lu]Lu-labelled somatostatin receptor agonist and antagonist. / Tamborino, Giulia ; De Saint-Hubert, Marijke ; Struelens, Lara et al.
Annual Congress of the European Association of Nuclear Medicine October 12 – 16, 2019 Barcelona, Spain: European Journal of Nuclear Medicine and Molecular Imaging volume . Vol. 46 2019. ed. 2019. p. S83-S84.

Research output › peer-review

TY - GEN

T1 - In vitro dose-response comparison of [177Lu]Lu-labelled somatostatin receptor agonist and antagonist

AU - Tamborino, Giulia

AU - De Saint-Hubert, Marijke

AU - Struelens, Lara

AU - Dalm, Simone

AU - Ruigrok, Eline A.M.

AU - de Jong, Marion

AU - Nonnekens, Julie

AU - Konijnenberg, Mark W.

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N2 - Peptide receptor radionuclide therapy (PRRT) using radiolabeled somatostatin receptor (SST) is very effective for treatment of neuroendocrine metastatic tumors. Recent studies indicate that radiolabeled SST antagonists show better tumor targeting during clinical imaging and preclinical therapy, despite little to no internalization in the cancer cells. However, preclinical studies are often limited to activity uptake, with no correlation between the delivered absorbed dose and the biological end-point. This study aims to calculate the absorbed dose to the nucleus for [177Lu]Lu-DOTA-Tyr3,octreotate (177Lu-DOTA-TATE, SST agonist) and [177Lu]Lu-DOTA-JR11 (177Lu- DOTA-JR11, SST antagonist), for comparison with DNA damage induction.

AB - Peptide receptor radionuclide therapy (PRRT) using radiolabeled somatostatin receptor (SST) is very effective for treatment of neuroendocrine metastatic tumors. Recent studies indicate that radiolabeled SST antagonists show better tumor targeting during clinical imaging and preclinical therapy, despite little to no internalization in the cancer cells. However, preclinical studies are often limited to activity uptake, with no correlation between the delivered absorbed dose and the biological end-point. This study aims to calculate the absorbed dose to the nucleus for [177Lu]Lu-DOTA-Tyr3,octreotate (177Lu-DOTA-TATE, SST agonist) and [177Lu]Lu-DOTA-JR11 (177Lu- DOTA-JR11, SST antagonist), for comparison with DNA damage induction.

KW - Double strand breaks

KW - Targeted Radionuclide Therapy

KW - Dose-response

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BT - Annual Congress of the European Association of Nuclear Medicine October 12 – 16, 2019 Barcelona, Spain

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Tamborino G , De Saint-Hubert M , Struelens L, Dalm S, Ruigrok EAM, de Jong M et al. In vitro dose-response comparison of [177Lu]Lu-labelled somatostatin receptor agonist and antagonist. In Annual Congress of the European Association of Nuclear Medicine October 12 – 16, 2019 Barcelona, Spain: European Journal of Nuclear Medicine and Molecular Imaging volume . 2019 ed. Vol. 46. 2019. p. S83-S84 doi: 10.1007/s00259-019-04486-2