Theranostic perspectives in prostate cancer with the gastrin-releasing peptide receptor antagonist NeoBOMB1: preclinical and first clinical results

BA Nock, A Kaloudi, E Lymperis, A Giarika… - Journal of Nuclear …, 2017 - Soc Nuclear Med
We recently introduced the potent gastrin-releasing peptide receptor (GRPR) antagonist 68
Ga-SB3 ( 68 Ga-DOTA-p-aminomethylaniline-diglycolic acid-DPhe-Gln-Trp-Ala-Val-Gly-His-…

[HTML][HTML] NeoBOMB1, a GRPR-Antagonist for Breast Cancer Theragnostics: First Results of a Preclinical Study with [67Ga]NeoBOMB1 in T-47D Cells and Tumor …

A Kaloudi, E Lymperis, A Giarika, S Dalm, F Orlandi… - Molecules, 2017 - mdpi.com
Background: The GRPR-antagonist-based radioligands [ 67/68 Ga/ 111 In/ 177 Lu]NeoBOMB1
have shown excellent theragnostic profiles in preclinical prostate cancer models, while [ …

Radiometal-dependent biological profile of the radiolabeled gastrin-releasing peptide receptor antagonist SB3 in cancer theranostics: Metabolic and biodistribution …

E Lymperis, A Kaloudi, W Sallegger… - Bioconjugate …, 2018 - ACS Publications
Recent advances in oncology involve the use of diagnostic/therapeutic radionuclide-carrier
pairs that target cancer cells, offering exciting opportunities for personalized patient treatment…

Improving the In Vivo Profile of Minigastrin Radiotracers: A Comparative Study Involving the Neutral Endopeptidase Inhibitor Phosphoramidon

A Kaloudi, BA Nock, E Lymperis… - Cancer Biotherapy …, 2016 - liebertpub.com
Minigastrin radiotracers, such as [ 111 In-DOTA]MG0 ([ 111 In-DOTA-DGlu 1 ]minigastrin),
have been considered for diagnostic imaging and radionuclide therapy of CCK2R-positive …

[HTML][HTML] Impact of clinically tested NEP/ACE inhibitors on tumor uptake of [111In-DOTA]MG11—first estimates for clinical translation

A Kaloudi, BA Nock, E Lymperis, R Valkema… - EJNMMI research, 2016 - Springer
Background We have recently shown that treatment of mice with the neutral endopeptidase (NEP)
inhibitor phosphoramidon (PA) improves the bioavailability and tumor uptake of …

Comparative evaluation of the new GRPR‐antagonist 111In‐SB9 and 111In‐AMBA in prostate cancer models: Implications of in vivo stability

E Lymperis, A Kaloudi, P Kanellopoulos… - Journal of Labelled …, 2019 - Wiley Online Library
Gastrin‐releasing peptide receptors (GRPRs) are overexpressed in prostate cancer,
representing attractive targets for diagnosis and therapy with bombesin (BBN)‐like radioligands. …

99mTc-labeled gastrins of varying peptide chain length: Distinct impact of NEP/ACE-inhibition on stability and tumor uptake in mice

A Kaloudi, BA Nock, E Lymperis, EP Krenning… - Nuclear Medicine and …, 2016 - Elsevier
Introduction In situ inhibition of neutral endopeptidase (NEP) has been recently shown to
impressively increase the bioavailability and tumor uptake of biodegradable gastrin …

In vivo inhibition of neutral endopeptidase enhances the diagnostic potential of truncated gastrin 111In-radioligands

A Kaloudi, BA Nock, E Lymperis, W Sallegger… - Nuclear Medicine and …, 2015 - Elsevier
Introduction Radiolabeled gastrin analogs represent attractive candidates for diagnosis and
therapy of cholecystokinin subtype-2 receptor (CCK2R)-expressing tumors. Radiolabeled …

[HTML][HTML] Comparing Gly11/dAla11-Replacement vs. the in-Situ Neprilysin-Inhibition Approach on the Tumor-targeting Efficacy of the 111In-SB3/111In-SB4 …

E Lymperis, A Kaloudi, P Kanellopoulos, M de Jong… - Molecules, 2019 - mdpi.com
Background: The GRPR-antagonist 68 Ga-SB3 visualized prostate cancer lesions in animal
models and in patients. Switching radiometal from 68 Ga to 111 In impaired tumor targeting …

[HTML][HTML] Localization of 99mTc-GRP Analogs in GRPR-Expressing Tumors: Effects of Peptide Length and Neprilysin Inhibition on Biological Responses

A Kaloudi, E Lymperis, P Kanellopoulos, B Waser… - Pharmaceuticals, 2019 - mdpi.com
The overexpression of gastrin-releasing peptide receptors (GRPRs) in frequently occurring
human tumors has provided the opportunity to use bombesin (BBN) analogs as radionuclide …