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Phase I Trial of [T...
Phase I Trial of [Tc-99m]Tc-maSSS-PEG(2)-RM26, a Bombesin Analogue Antagonistic to Gastrin-Releasing Peptide Receptors (GRPRs), for SPECT Imaging of GRPR Expression in Malignant Tumors
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- Chernov, Vladimir (author)
- 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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- Rybina, Anastasiya (author)
- Russian Acad Sci, Tomsk Natl Res Med Ctr, Canc Res Inst, Dept Nucl Med, Tomsk 634009, Russia.
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- Zelchan, Roman (author)
- 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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- Medvedeva, Anna (author)
- Russian Acad Sci, Tomsk Natl Res Med Ctr, Canc Res Inst, Dept Nucl Med, Tomsk 634009, Russia.
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- Bragina, Olga (author)
- 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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- Lushnikova, Nadejda (author)
- Russian Acad Sci, Tomsk Natl Res Med Ctr, Canc Res Inst, Dept Gen Oncol, Tomsk 634009, Russia.
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- Doroshenko, Artem (author)
- Russian Acad Sci, Tomsk Natl Res Med Ctr, Canc Res Inst, Dept Gen Oncol, Tomsk 634009, Russia.
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- Usynin, Evgeniy (author)
- Russian Acad Sci, Tomsk Natl Res Med Ctr, Canc Res Inst, Dept Gen Oncol, Tomsk 634009, Russia.
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- Tashireva, Liubov (author)
- Russian Acad Sci, Tomsk Natl Res Med Ctr, Canc Res Inst, Dept Gen & Mol Pathol, Tomsk 634009, Russia.;Russian Acad Sci, Tomsk Natl Res Med Ctr, Canc Res Inst, Lab Mol Therapy Canc, Tomsk 634028, Russia.
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- Vtorushin, Sergey (author)
- Russian Acad Sci, Tomsk Natl Res Med Ctr, Canc Res Inst, Dept Gen & Mol Pathol, Tomsk 634009, Russia.;Siberian State Med Univ, Pathol Dept, Tomsk 634050, Russia.
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- Abouzayed, Ayman (author)
- Uppsala universitet,Theranostics
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- Rinne, Sara S. (author)
- Uppsala universitet,Theranostics
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- Sörensen, Jens (author)
- Uppsala universitet,Radiologi
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- Tolmachev, Vladimir (author)
- Uppsala universitet,Cancerprecisionsmedicin,Tomsk Polytech Univ, Res Sch Chem & Appl Biomed Sci, Res Ctr Oncotheranost, Tomsk 634050, Russia.
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- Orlova, Anna, 1960- (author)
- 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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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. Russian Acad Sci, Tomsk Natl Res Med Ctr, Canc Res Inst, Dept Nucl Med, Tomsk 634009, Russia. (creator_code:org_t)
- 2023-03-07
- 2023
- English.
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In: Cancers. - : MDPI. - 2072-6694. ; 15:6
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Abstract
Subject headings
Close
- 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.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Cancer och onkologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Cancer and Oncology (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Radiologi och bildbehandling (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Radiology, Nuclear Medicine and Medical Imaging (hsv//eng)
Keyword
- GRPR
- antagonist
- 99mTc
- phase I trial
Publication and Content Type
- ref (subject category)
- art (subject category)
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Cancers
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Chernov, Vladimi ...
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Rybina, Anastasi ...
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Zelchan, Roman
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Medvedeva, Anna
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Bragina, Olga
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Lushnikova, Nade ...
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Doroshenko, Arte ...
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Usynin, Evgeniy
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Tashireva, Liubo ...
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Vtorushin, Serge ...
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Abouzayed, Ayman
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Rinne, Sara S.
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Sörensen, Jens
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Tolmachev, Vladi ...
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Orlova, Anna, 19 ...
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Cancers
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Uppsala University