Literature DB >> 31482426

First-in-human dosimetry of gastrin-releasing peptide receptor antagonist [177Lu]Lu-RM2: a radiopharmaceutical for the treatment of metastatic castration-resistant prostate cancer.

Jens Kurth1, Bernd Joachim Krause2, Sarah M Schwarzenböck2, Carina Bergner2, Oliver W Hakenberg3, Martin Heuschkel2.   

Abstract

PURPOSE: Besides PSMA, prostate cancer cells also express gastrin-releasing peptide receptor (GRPr) which is therefore a promising target for theranostic approaches. The high affinity GRPr antagonist RM2 can be labeled with beta-emitting radiometals for therapeutic purposes. The aim of this study was to calculate absorbed doses for critical organs and tumor lesions for [177Lu]Lu-RM2 therapy administered in a group of metastatic castration-resistant prostate cancer (mCRPC) patients who had insufficient PSMA expression or showed lower PSMA accumulation after previous cycles of [177Lu]Lu-PSMA-617 therapy.
METHODS: Thirty-five patients suffering from mCRPC without further treatment options for approved therapies were examined with [68Ga]Ga-RM2-PET/CT. Out of these, 4 patients (mean age 68 years) were treated with [177Lu]Lu-RM2; two of these also received a 2nd therapy cycle. Mean activity was 4.5 ± 0.9 GBq. For dosimetry, patients underwent planar WB-scintigraphy and SPECT/CT imaging of the upper and lower abdomen at approximately 1, 24, 48, and 72 h p.i. along with blood sampling. Absorbed doses for kidneys, pancreas, liver, spleen, gallbladder wall, and tumor lesions were derived based on quantitative SPECT/CT according to RADAR dosimetry scheme; individual organ masses were extracted from CT. Absorbed dose to bone marrow was calculated based on serial whole-body images and blood sampling according to the EANM guideline.
RESULTS: Therapy was well tolerated by all patients and no side effects were observed. An increased uptake in tumor lesions and the pancreas was seen within the first 1 h. Mean absorbed organ doses were 1.08 ± 0.44 Gy/GBq in the pancreas, 0.35 ± 0.14 Gy/GBq in the kidneys, 0.05 ± 0.02 Gy/GBq in the liver, 0.07 ± 0.02 Gy/GBq in the gallbladder wall, 0.10 ± 0.06 Gy/GBq in the spleen, and 0.02 ± 0.01 Gy/GBq for the red bone marrow. The mean dose for tumor lesions was 6.20 ± 3.00 Gy/GBq.
CONCLUSIONS: Application of GRPr antagonist [177Lu]Lu-RM2 is suitable for targeted radiotherapy of mCRPC as it shows high tumor uptake and rapid clearance from normal organs. Absorbed doses in tumor lesions are therapeutically relevant. The critical organ receiving the highest absorbed dose was the pancreas. Results suggest that the activity administered for each cycle could be increased to maximize the absorbed dose of tumors and metastases.

Entities:  

Keywords:  177Lu-RM2; Dosimetry; Gastrin-releasing peptide receptor; Prostate cancer; Radionuclide therapy; Theranostics

Mesh:

Substances:

Year:  2019        PMID: 31482426     DOI: 10.1007/s00259-019-04504-3

Source DB:  PubMed          Journal:  Eur J Nucl Med Mol Imaging        ISSN: 1619-7070            Impact factor:   9.236


  53 in total

1.  MIRD pamphlet no. 16: Techniques for quantitative radiopharmaceutical biodistribution data acquisition and analysis for use in human radiation dose estimates.

Authors:  J A Siegel; S R Thomas; J B Stubbs; M G Stabin; M T Hays; K F Koral; J S Robertson; R W Howell; B W Wessels; D R Fisher; D A Weber; A B Brill
Journal:  J Nucl Med       Date:  1999-02       Impact factor: 10.057

2.  Quantitative Analyses of Normal Tissue Effects in the Clinic (QUANTEC): an introduction to the scientific issues.

Authors:  Søren M Bentzen; Louis S Constine; Joseph O Deasy; Avi Eisbruch; Andrew Jackson; Lawrence B Marks; Randall K Ten Haken; Ellen D Yorke
Journal:  Int J Radiat Oncol Biol Phys       Date:  2010-03-01       Impact factor: 7.038

3.  Lacrimal Glands May Represent Organs at Risk for Radionuclide Therapy of Prostate Cancer with [(177)Lu]DKFZ-PSMA-617.

Authors:  Melanie Hohberg; Wolfgang Eschner; Matthias Schmidt; Markus Dietlein; Carsten Kobe; Thomas Fischer; Alexander Drzezga; Markus Wild
Journal:  Mol Imaging Biol       Date:  2016-06       Impact factor: 3.488

4.  68Ga/177Lu-NeoBOMB1, a Novel Radiolabeled GRPR Antagonist for Theranostic Use in Oncology.

Authors:  Simone U Dalm; Ingrid L Bakker; Erik de Blois; Gabriela N Doeswijk; Mark W Konijnenberg; Francesca Orlandi; Donato Barbato; Mattia Tedesco; Theodosia Maina; Berthold A Nock; Marion de Jong
Journal:  J Nucl Med       Date:  2016-09-08       Impact factor: 10.057

5.  Patient-specific dosimetry in predicting renal toxicity with (90)Y-DOTATOC: relevance of kidney volume and dose rate in finding a dose-effect relationship.

Authors:  Raffaella Barone; Françoise Borson-Chazot; Roelf Valkema; Stéphan Walrand; Franck Chauvin; Lida Gogou; Larry K Kvols; Eric P Krenning; François Jamar; Stanislas Pauwels
Journal:  J Nucl Med       Date:  2005-01       Impact factor: 10.057

6.  EAU-ESTRO-SIOG Guidelines on Prostate Cancer. Part II: Treatment of Relapsing, Metastatic, and Castration-Resistant Prostate Cancer.

Authors:  Philip Cornford; Joaquim Bellmunt; Michel Bolla; Erik Briers; Maria De Santis; Tobias Gross; Ann M Henry; Steven Joniau; Thomas B Lam; Malcolm D Mason; Henk G van der Poel; Theo H van der Kwast; Olivier Rouvière; Thomas Wiegel; Nicolas Mottet
Journal:  Eur Urol       Date:  2016-08-31       Impact factor: 20.096

7.  Treatment with the radiolabeled somatostatin analog [177 Lu-DOTA 0,Tyr3]octreotate: toxicity, efficacy, and survival.

Authors:  Dik J Kwekkeboom; Wouter W de Herder; Boen L Kam; Casper H van Eijck; Martijn van Essen; Peter P Kooij; Richard A Feelders; Maarten O van Aken; Eric P Krenning
Journal:  J Clin Oncol       Date:  2008-05-01       Impact factor: 44.544

8.  Individualised 177Lu-DOTATATE treatment of neuroendocrine tumours based on kidney dosimetry.

Authors:  Anna Sundlöv; Katarina Sjögreen-Gleisner; Johanna Svensson; Michael Ljungberg; Tomas Olsson; Peter Bernhardt; Jan Tennvall
Journal:  Eur J Nucl Med Mol Imaging       Date:  2017-03-22       Impact factor: 9.236

9.  External radiation exposure, excretion, and effective half-life in 177Lu-PSMA-targeted therapies.

Authors:  J Kurth; B J Krause; S M Schwarzenböck; L Stegger; M Schäfers; K Rahbar
Journal:  EJNMMI Res       Date:  2018-04-12       Impact factor: 3.138

10.  Dose to organs at risk in the upper abdomen in patients treated with extended fields by helical tomotherapy: a dosimetric and clinical preliminary study.

Authors:  Sara Bresciani; Elisabetta Garibaldi; Gabriella Cattari; Angelo Maggio; Amalia Di Dia; Elena Delmastro; Domenico Gabriele; Michele Stasi; Pietro Gabriele
Journal:  Radiat Oncol       Date:  2013-10-25       Impact factor: 3.481

View more
  14 in total

1.  68Ga-Labeled [Leu13ψThz14]Bombesin(7-14) Derivatives: Promising GRPR-Targeting PET Tracers with Low Pancreas Uptake.

Authors:  Lei Wang; Zhengxing Zhang; Helen Merkens; Jutta Zeisler; Chengcheng Zhang; Aron Roxin; Ruiyan Tan; François Bénard; Kuo-Shyan Lin
Journal:  Molecules       Date:  2022-06-11       Impact factor: 4.927

2.  Copper-67-Labeled Bombesin Peptide for Targeted Radionuclide Therapy of Prostate Cancer.

Authors:  Truc T Huynh; Ellen M van Dam; Sreeja Sreekumar; Cedric Mpoy; Benjamin J Blyth; Fenella Muntz; Matthew J Harris; Buck E Rogers
Journal:  Pharmaceuticals (Basel)       Date:  2022-06-08

Review 3.  Recent updates and developments in PET imaging of prostate cancer.

Authors:  Steven P Rowe; Geoffrey B Johnson; Martin G Pomper; Michael A Gorin; Spencer C Behr
Journal:  Abdom Radiol (NY)       Date:  2020-12

Review 4.  Radiopharmaceutical therapy in cancer: clinical advances and challenges.

Authors:  George Sgouros; Lisa Bodei; Michael R McDevitt; Jessie R Nedrow
Journal:  Nat Rev Drug Discov       Date:  2020-07-29       Impact factor: 84.694

5.  Effect of the versatile bifunctional chelator AAZTA5 on the radiometal labelling properties and the in vitro performance of a gastrin releasing peptide receptor antagonist.

Authors:  Michael Hofstetter; Euy Sung Moon; Fabio D'Angelo; Lucien Geissbühler; Ian Alberts; Ali Afshar-Oromieh; Frank Rösch; Axel Rominger; Eleni Gourni
Journal:  EJNMMI Radiopharm Chem       Date:  2020-11-30

6.  Gastrin-Releasing Peptide Receptor Antagonist [68Ga]RM2 PET/CT for Staging of Pre-Treated, Metastasized Breast Cancer.

Authors:  Kerstin Michalski; Lars Kemna; Jasmin Asberger; Anca L Grosu; Philipp T Meyer; Juri Ruf; Tanja Sprave
Journal:  Cancers (Basel)       Date:  2021-12-03       Impact factor: 6.639

Review 7.  Bombesin Receptor Family Activation and CNS/Neural Tumors: Review of Evidence Supporting Possible Role for Novel Targeted Therapy.

Authors:  Terry W Moody; Lingaku Lee; Irene Ramos-Alvarez; Tatiana Iordanskaia; Samuel A Mantey; Robert T Jensen
Journal:  Front Endocrinol (Lausanne)       Date:  2021-09-01       Impact factor: 5.555

Review 8.  More Than Meets the Eye: Scientific Rationale behind Molecular Imaging and Therapeutic Targeting of Prostate-Specific Membrane Antigen (PSMA) in Metastatic Prostate Cancer and Beyond.

Authors:  Anniina Hyväkkä; Verneri Virtanen; Jukka Kemppainen; Tove J Grönroos; Heikki Minn; Maria Sundvall
Journal:  Cancers (Basel)       Date:  2021-05-07       Impact factor: 6.639

Review 9.  Combination Therapy, a Promising Approach to Enhance the Efficacy of Radionuclide and Targeted Radionuclide Therapy of Prostate and Breast Cancer.

Authors:  Tyrillshall S T Damiana; Simone U Dalm
Journal:  Pharmaceutics       Date:  2021-05-07       Impact factor: 6.321

Review 10.  Prognostic and Theranostic Applications of Positron Emission Tomography for a Personalized Approach to Metastatic Castration-Resistant Prostate Cancer.

Authors:  Luca Filippi; Viviana Frantellizzi; Agostino Chiaravalloti; Mariano Pontico; Maria Silvia De Feo; Ferdinando Corica; Melissa Montebello; Orazio Schillaci; Giuseppe De Vincentis; Oreste Bagni
Journal:  Int J Mol Sci       Date:  2021-03-16       Impact factor: 5.923

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.