Single-Photon Emission Computer Tomography Imaging of Prostate-Specific Membrane Antigen (PSMA) Expression in Prostate Cancer Patients Using a Novel Peptide-Based Probe [99mTc]Tc-BQ0413 with Picomolar Affinity to PSMA: A Phase I/II Clinical Study
| Parent link: | ACS Pharmacology & Translational Science.— .— Washington: ACS Publications Vol. 8, iss. 3.— 2025.— P. 736-747 |
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| מחברים אחרים: | , , , , , , , , , , |
| סיכום: | Title screen Radionuclide imaging of prostate-specific membrane antigen (PSMA) expression can be used for staging prostate cancer. The pseudo-peptide [99mTc]Tc-BQ0413 demonstrated high affinity and specificity to PSMA in preclinical evaluation. The purpose of this study was to clinically evaluate the safety and tolerability of a single administration of [99mTc]Tc-BQ0413 as well as study its biodistribution using SPECT to estimate dosimetry. [99mTc]Tc-BQ0413 was studied in a single-center diagnostic Phase I open-label exploratory study. Whole-body planar scintigraphy and SPECT/CT imaging were performed 2, 4, and 6 h after administration of 50, 100, or 150 μg (680 ± 140 MBq) of [99mTc]Tc-BQ0413 in five PCa patients per injected mass (NCT05839990). All injections of [99mTc]Tc-BQ0413 were well tolerated. The elimination of [99mTc]Tc-BQ0413 was predominantly renal. The stable physiological uptake of [99mTc]Tc-BQ0413 was observed in the lacrimal and salivary glands, liver, spleen, and kidneys for all tested peptide-injected masses. The average effective doses were 0.007 ± 0.001, 0.0049 ± 0.0003, and 0.0062 ± 0.0008 mSv/MBq for 50, 100, and 150 μg/injection, respectively. The radionuclide-associated dose burden per patient was 4–7 mSv/study for the given activity. Uptake of [99mTc]Tc-BQ0413 in primary tumors was identified in all patients and increased with the peptide-injected mass. Uptake in lymph nodes and bone metastases was the highest at 100 μg/injected mass. The highest tumor lesion/background ratios were observed 6 h after the administration of 100 μg of [99mTc]Tc-BQ0413. The results of the Phase I study showed that injections of [99mTc]Tc-BQ0413 were well tolerated, safe, and associated with low absorbed doses. Imaging using [99mTc]Tc-BQ0413 enabled the visualization of primary prostate cancer lesions as well as metastases in lymph nodes and bones Текстовый файл |
| שפה: | אנגלית |
| יצא לאור: |
2025
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| נושאים: | |
| גישה מקוונת: | https://doi.org/10.1021/acsptsci.4c00637 |
| פורמט: | אלקטרוני Book Chapter |
| KOHA link: | https://koha.lib.tpu.ru/cgi-bin/koha/opac-detail.pl?biblionumber=679784 |
| סיכום: | Title screen Radionuclide imaging of prostate-specific membrane antigen (PSMA) expression can be used for staging prostate cancer. The pseudo-peptide [99mTc]Tc-BQ0413 demonstrated high affinity and specificity to PSMA in preclinical evaluation. The purpose of this study was to clinically evaluate the safety and tolerability of a single administration of [99mTc]Tc-BQ0413 as well as study its biodistribution using SPECT to estimate dosimetry. [99mTc]Tc-BQ0413 was studied in a single-center diagnostic Phase I open-label exploratory study. Whole-body planar scintigraphy and SPECT/CT imaging were performed 2, 4, and 6 h after administration of 50, 100, or 150 μg (680 ± 140 MBq) of [99mTc]Tc-BQ0413 in five PCa patients per injected mass (NCT05839990). All injections of [99mTc]Tc-BQ0413 were well tolerated. The elimination of [99mTc]Tc-BQ0413 was predominantly renal. The stable physiological uptake of [99mTc]Tc-BQ0413 was observed in the lacrimal and salivary glands, liver, spleen, and kidneys for all tested peptide-injected masses. The average effective doses were 0.007 ± 0.001, 0.0049 ± 0.0003, and 0.0062 ± 0.0008 mSv/MBq for 50, 100, and 150 μg/injection, respectively. The radionuclide-associated dose burden per patient was 4–7 mSv/study for the given activity. Uptake of [99mTc]Tc-BQ0413 in primary tumors was identified in all patients and increased with the peptide-injected mass. Uptake in lymph nodes and bone metastases was the highest at 100 μg/injected mass. The highest tumor lesion/background ratios were observed 6 h after the administration of 100 μg of [99mTc]Tc-BQ0413. The results of the Phase I study showed that injections of [99mTc]Tc-BQ0413 were well tolerated, safe, and associated with low absorbed doses. Imaging using [99mTc]Tc-BQ0413 enabled the visualization of primary prostate cancer lesions as well as metastases in lymph nodes and bones Текстовый файл |
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| DOI: | 10.1021/acsptsci.4c00637 |