First in-human radiation dosimetry of the gastrin-releasing peptide (GRP) receptor antagonist

Gastrin-releasing peptide receptor antagonists have promise in theranostics of several highly incident tumours, including prostate and breast. This study presents the first human dosimetry of 68Ga-NODAGA-MJ9 in the first five consecutive patients with recurrent prostate cancer included in a dual-tracer positron emission tomography (PET) protocol. Five male patients with biochemical relapse of prostate adenocarcinoma underwent four whole-body time-of-flight PET/CT scans within 2 h after tracer injection. To be used as input in OLINDA/EXM 2.0, time-integrated activity coefficients were derived from manually drawn regions of interest over the following body regions: brain, thyroid, lungs, heart, liver, gallbladder, spleen, stomach, kidneys, adrenals, red marrow, pancreas, intestines, urinary bladder and whole body. Organ absorbed doses and effective dose (ED) were calculated with OLINDA/EXM 2.0 using the NURBS voxelized phantoms adjusted to the ICRP-89 organ masses and ICRP103 tissue-weighting factors. Additional absorbed dose estimations were performed with OLINDA/EXM 1.1 to be comparable with similar previous [...] GNESIN, Silvano, et al. First in-human radiation dosimetry of the gastrin-releasing peptide (GRP) receptor antagonist 68Ga-NODAGA-MJ9. EJNMMI Research, 2018, vol. 8, no. 1, p. 108 DOI : 10.1186/s13550-018-0462-9

[1]  C. Buchpiguel,et al.  Comparative Dosimetry for 68Ga-DOTATATE: Impact of Using Updated ICRP Phantoms, S Values, and Tissue-Weighting Factors , 2018, The Journal of Nuclear Medicine.

[2]  Michael G Stabin,et al.  RADAR Dose Estimate Report: A Compendium of Radiopharmaceutical Dose Estimates Based on OLINDA/EXM Version 2.0 , 2018, The Journal of Nuclear Medicine.

[3]  Xiaoyuan Chen,et al.  PET Using a GRPR Antagonist 68Ga-RM26 in Healthy Volunteers and Prostate Cancer Patients , 2017, The Journal of Nuclear Medicine.

[4]  A. Iagaru.  Will GRPR Compete with PSMA as a Target in Prostate Cancer? , 2017, The Journal of Nuclear Medicine.

[5]  E. Hindié,et al.  Expression of Gastrin-Releasing Peptide Receptor in Breast Cancer and Its Association with Pathologic, Biologic, and Clinical Parameters: A Study of 1,432 Primary Tumors , 2017, The Journal of Nuclear Medicine.

[6]  M. de Jong,et al.  68Ga/177Lu-NeoBOMB1, a Novel Radiolabeled GRPR Antagonist for Theranostic Use in Oncology , 2017, The Journal of Nuclear Medicine.

[7]  A. Iagaru,et al.  Bombesin-Targeted PET of Prostate Cancer , 2016, The Journal of Nuclear Medicine.

[8]  U. Haberkorn,et al.  Radiation dosimetry of 68Ga-PSMA-11 (HBED-CC) and preliminary evaluation of optimal imaging timing , 2016, European Journal of Nuclear Medicine and Molecular Imaging.

[9]  M. Schwaiger,et al.  Biodistribution and radiation dosimetry of 68Ga-PSMA HBED CC—a PSMA specific probe for PET imaging of prostate cancer , 2016, European Journal of Nuclear Medicine and Molecular Imaging.

[10]  R. Jensen,et al.  Bombesin related peptides/receptors and their promising therapeutic roles in cancer imaging, targeting and treatment , 2016, Expert opinion on therapeutic targets.

[11]  Xiaoyuan Chen,et al.  68Ga-NOTA-Aca-BBN(7–14) PET/CT in Healthy Volunteers and Glioma Patients , 2016, The Journal of Nuclear Medicine.

[12]  Tim Holland-Letz,et al.  The Theranostic PSMA Ligand PSMA-617 in the Diagnosis of Prostate Cancer by PET/CT: Biodistribution in Humans, Radiation Dosimetry, and First Evaluation of Tumor Lesions , 2015, The Journal of Nuclear Medicine.

[13]  R. Jensen,et al.  Insights into bombesin receptors and ligands: Highlighting recent advances , 2015, Peptides.

[14]  A. Buck,et al.  Biodistribution and Radiation Dosimetry for a Probe Targeting Prostate-Specific Membrane Antigen for Imaging and Therapy , 2015, The Journal of Nuclear Medicine.

[15]  I. Burger,et al.  Dosimetry and First Clinical Evaluation of the New 18F-Radiolabeled Bombesin Analogue BAY 864367 in Patients with Prostate Cancer , 2015, The Journal of Nuclear Medicine.

[16]  J. Reubi,et al.  N-Terminal Modifications Improve the Receptor Affinity and Pharmacokinetics of Radiolabeled Peptidic Gastrin-Releasing Peptide Receptor Antagonists: Examples of 68Ga- and 64Cu-Labeled Peptides for PET Imaging , 2014, The Journal of Nuclear Medicine.

[17]  R. Sadeghi,et al.  Diagnostic value of 99mTc-bombesin scintigraphy for differentiation of malignant from benign breast lesions , 2014, Nuclear medicine communications.

[18]  W. Schultze‐Seemann,et al.  Positron Emission Tomography (PET) Imaging of Prostate Cancer with a Gastrin Releasing Peptide Receptor Antagonist - from Mice to Men , 2014, Theranostics.

[19]  I. Jambor,et al.  In Vivo Imaging of Prostate Cancer Using [68Ga]-Labeled Bombesin Analog BAY86-7548 , 2013, Clinical Cancer Research.

[20]  I. Jambor,et al.  Plasma Pharmacokinetics, Whole-Body Distribution, Metabolism, and Radiation Dosimetry of 68Ga Bombesin Antagonist BAY 86-7548 in Healthy Men , 2013, The Journal of Nuclear Medicine.

[21]  R. Walker,et al.  Measured Human Dosimetry of 68Ga-DOTATATE , 2013, The Journal of Nuclear Medicine.

[22]  K. Jingu,et al.  Intraoperative radiotherapy for pancreatic cancer: 30-year experience in a single institution in Japan. , 2012, International journal of radiation oncology, biology, physics.

[23]  V. Bettinardi,et al.  Physical performance of the new hybrid PET∕CT Discovery-690. , 2011, Medical physics.

[24]  C. Santos-Cuevas,et al.  Targeted imaging of gastrin-releasing peptide receptors with 99mTc-EDDA/HYNIC-[Lys3]-bombesin: biokinetics and dosimetry in women , 2008, Nuclear medicine communications.

[25]  Anastasia Nikolopoulou,et al.  Bombesin Receptor Antagonists May Be Preferable to Agonists for Tumor Targeting , 2008, Journal of Nuclear Medicine.

[26]  Icrp.  Main Text , 2008, Annals of the ICRP.

[27]  Paul Schellhammer,et al.  Defining biochemical failure following radiotherapy with or without hormonal therapy in men with clinically localized prostate cancer: recommendations of the RTOG-ASTRO Phoenix Consensus Conference. , 2006, International journal of radiation oncology, biology, physics.

[28]  Michael G Stabin,et al.  OLINDA/EXM: the second-generation personal computer software for internal dose assessment in nuclear medicine. , 2005, Journal of nuclear medicine : official publication, Society of Nuclear Medicine.

[29]  G. D. Vincentis,et al.  99mTc-bombesin detects prostate cancer and invasion of pelvic lymph nodes , 2003, European Journal of Nuclear Medicine and Molecular Imaging.

[30]  J. Valentin.  Basic anatomical and physiological data for use in radiological protection: reference values , 2002, Annals of the ICRP.

[31]  G. de Vincentis,et al.  Technetium labeled bombesin-like peptide: preliminary report on breast cancer uptake in patients. , 2002, Cancer biotherapy & radiopharmaceuticals.

[32]  G. Slegers,et al.  Technetium-99m RP527, a GRP analogue for visualisation of GRP receptor-expressing malignancies: a feasibility study , 2000, European Journal of Nuclear Medicine.

[33]  F Dumont,et al.  Biodistribution and dosimetry of (99m)Tc-RP527, a gastrin-releasing peptide (GRP) agonist for the visualization of GRP receptor-expressing malignancies. , 2000, Journal of nuclear medicine : official publication, Society of Nuclear Medicine.

[34]  J C Reubi,et al.  Gastrin-releasing peptide receptors in the human prostate: relation to neoplastic transformation. , 1999, Cancer research.

[35]  M. Ciomei,et al.  Bombesin stimulates growth of human prostatic cancer cells in vitro , 1990, Cancer.

[36]  T. Renda,et al.  The brain-gut-skin triangle: New peptides , 1981, Peptides.

[37]  G Nilsson,et al.  Characterization of a gastrin releasing peptide from porcine non-antral gastric tissue. , 1979, Biochemical and biophysical research communications.

[38]  J. Valentin,et al.  The 2007 Recommendations of the International Commission on Radiological Protection. ICRP publication 103. , 2007, Annals of the ICRP.

[39]  M. Zasloff,et al.  Peptides from frog skin. , 1990, Annual review of biochemistry.

[40]  John D. Minna,et al.  Bombesin-like peptides can function as autocrine growth factors in human small-cell lung cancer , 1985, Nature.

[41]  V. Erspamer,et al.  Isolation and structure of bombesin and alytesin, 2 analogous active peptides from the skin of the European amphibians Bombina and Alytes. , 1971, Experientia.