Title | Phase I Trial of [99mTc]Tc-maSSS-PEG2-RM26, a Bombesin Analogue Antagonistic to Gastrin-Releasing Peptide Receptors (GRPRs), for SPECT Imaging of GRPR Expression in Malignant Tumors. |
Publication Type | Journal Article |
Year of Publication | 2023 |
Authors | Chernov V, Rybina A, Zelchan R, Medvedeva A, Bragina O, Lushnikova N, Doroshenko A, Usynin E, Tashireva L, Vtorushin S, Abouzayed A, Rinne SS, Sörensen J, Tolmachev V, Orlova A |
Journal | Cancers (Basel) |
Volume | 15 |
Issue | 6 |
Date Published | 2023 Mar 07 |
ISSN | 2072-6694 |
Abstract | The gastrin-releasing peptide receptor (GRPR) is overexpressed in prostate cancer (PCa) and in hormone-driven breast cancer (BCa). The aim of this phase I clinical trial was to evaluate safety, biodistribution, and dosimetry after the administration of the recently developed GRPR-targeting antagonistic bombesin analogue [99mTc]Tc-maSSS-PEG2-RM26 in PCa and BCa patients. Planar and whole-body SPECT/CT imaging was performed in six PCa patients and seven BCa patients 2, 4, 6, and 24 h post the intravenous administration of 40 µg of [99mTc]Tc-maSSS-PEG2-RM26 (600-700 MBq). No adverse events or pathological changes were observed. The rapid blood clearance of [99mTc]Tc-maSSS-PEG2-RM26 was observed with predominantly hepatobiliary excretion. The effective doses were 0.0053 ± 0.0007 for male patients and 0.008 ± 0.003 mSv/MBq for female patients. The accumulation of [99mTc]Tc-maSSS-PEG2-RM26 in tumors was observed in four out of six PCa and in seven out of seven BCa patients. In four BCa patients, a high uptake of the agent into the axillary lymph nodes was detected. Immunohistochemistry revealed positive GRPR expression in 60% of primary PCa, 71.4% of BCa tumors, and 50% of examined BCa lymph nodes. In conclusion, a single administration of [99mTc]Tc-maSSS-PEG2-RM26 was safe and well tolerated. [99mTc]Tc-maSSS-PEG2-RM26 SPECT may be useful for tumor detection in PCa and BCa patients, pending further studies. |
DOI | 10.3390/cancers15061631 |
Alternate Journal | Cancers (Basel) |
PubMed ID | 36980517 |
PubMed Central ID | PMC10046460 |
Grant List | 20-0815 PjF / / Swedish Cancer Society / 20 0814 UsF / / Swedish Cancer Society / 2019-00986 / / Swedish Research Council / 2022-00556 / / Swedish Research Council / 075-15-2022-1103 / / Ministry of Health and Higher Education of the Russian Federation / |
Related Institute:
Brain Health Imaging Institute (BHII)