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; Cancers; Vol. 15 - iss. 6

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

Bibliographic Details
Parent link:	Cancers.— .— Basel: MDPI AG Vol. 15 - iss. 6.— 2023.— Article number 1631, P. 1-15
Corporate Author:	National Research Tomsk Polytechnic University
Other Authors:	Chernov V. I. Vladimir Ivanovich, Rybina A. N. Anastasiya Nikolaevna, Zelchan (Zeltchan) R. V. Roman Vladimirovich, Medvedeva А. А. Anna Aleksandrovna, Bragina O. D. Olga Dmitrievna, Lushnikova N. Nadejda, Doroshenko A. Artem, Usynin E. Evgeniy, Tashireva L. Liubov, Vtorushin S. Sergey, Abouzayed A. Ayman, Rinne S. S. Sara, Sorensen J. Jens, Tolmachev V. M. Vladimir Maksimilianovich, Orlova A. M. Anna Markovna
Summary:	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-maSSSPEG2-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. Текстовый файл
Language:	English
Published:	2023
Subjects:	GRPR antagonist 99mTc phase I trial труды учёных ТПУ электронный ресурс
Online Access:	https://doi.org/10.3390/cancers15061631
Format:	Electronic Book Chapter
KOHA link:	https://koha.lib.tpu.ru/cgi-bin/koha/opac-detail.pl?biblionumber=671233

Internet

https://doi.org/10.3390/cancers15061631