Åpne denne publikasjonen i ny fane eller vindu >>Russian Acad Sci, Tomsk Natl Res Med Ctr, Canc Res Inst, Dept Nucl Med, Tomsk 634009, Russia.;Tomsk Polytech Univ, Res Sch Chem & Appl Biomed Sci, Res Ctr Oncotheranost, Tomsk 634050, Russia..
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Russian Acad Sci, Tomsk Natl Res Med Ctr, Canc Res Inst, Dept Gen Oncol, Tomsk 634009, Russia..
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Uppsala universitet, Medicinska och farmaceutiska vetenskapsområdet, Farmaceutiska fakulteten, Institutionen för läkemedelskemi, Theranostics.
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Uppsala universitet, Science for Life Laboratory, SciLifeLab. Tomsk Polytech Univ, Res Sch Chem & Appl Biomed Sci, Res Ctr Oncotheranost, Tomsk 634050, Russia.;Siberian State Med Univ, Pathol Dept, Tomsk 634050, Russia..
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2023 (engelsk)Inngår i: Cancers, ISSN 2072-6694, Vol. 15, nr 6, artikkel-id 1631Artikkel i tidsskrift (Fagfellevurdert) Published
Abstract [en]
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 [Tc-99m]Tc-maSSS-PEG(2)-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 mu g of [Tc-99m]Tc-maSSS-PEG(2)-RM26 (600-700 MBq). No adverse events or pathological changes were observed. The rapid blood clearance of [Tc-99m]Tc-maSSS-PEG(2)-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 [Tc-99m]Tc-maSSS-PEG(2)-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 [Tc-99m]Tc-maSSS-PEG(2)-RM26 was safe and well tolerated. [Tc-99m]Tc-maSSS-PEG(2)-RM26 SPECT may be useful for tumor detection in PCa and BCa patients, pending further studies.
sted, utgiver, år, opplag, sider
MDPI, 2023
Emneord
GRPR, antagonist, 99mTc, phase I trial
HSV kategori
Identifikatorer
urn:nbn:se:uu:diva-500596 (URN)10.3390/cancers15061631 (DOI)000957432700001 ()36980517 (PubMedID)
Forskningsfinansiär
Swedish Cancer Society, 20-0815 PjFSwedish Cancer Society, 20 0814 UsFSwedish Research Council, 2019-00986Swedish Research Council, 2022-00556
2023-04-212023-04-212023-05-06bibliografisk kontrollert