{"entity": "publication", "iuid": "90c78f702b6d4479b87f3657d73d498e", "timestamp": "2026-09-30T01:27:58.289Z", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/90c78f702b6d4479b87f3657d73d498e.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/90c78f702b6d4479b87f3657d73d498e"}}, "title": "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.", "authors": [{"family": "Medvedeva", "given": "Anna", "initials": "A"}, {"family": "Chernov", "given": "Vladimir", "initials": "V"}, {"family": "Larkina", "given": "Maria", "initials": "M"}, {"family": "Rybina", "given": "Anastasiya", "initials": "A"}, {"family": "Zelchan", "given": "Roman", "initials": "R"}, {"family": "Bragina", "given": "Olga", "initials": "O"}, {"family": "Varvashenya", "given": "Ruslan", "initials": "R"}, {"family": "Zebzeeva", "given": "Olga", "initials": "O"}, {"family": "Bezverkhniaia", "given": "Ekaterina", "initials": "E", "orcid": "0000-0001-7699-5719", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/211d24252bc84d43aed1d7ed4c3d3238.json"}}, {"family": "Tolmachev", "given": "Vladimir", "initials": "V", "orcid": "0000-0002-6122-1734", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/896ae9fae8b74251afe11b4354c62794.json"}}, {"family": "Orlova", "given": "Anna", "initials": "A", "orcid": "0000-0001-6120-2683", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/1c374f429702489494c05f84f298b4b7.json"}}], "type": "journal article", "published": "2025-03-14", "journal": {"title": "ACS pharmacology & translational science", "issn": "2575-9108", "volume": "8", "issue": "3", "pages": "736-747", "issn-l": "2575-9108"}, "abstract": "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 \u03bcg (680 \u00b1 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 \u00b1 0.001, 0.0049 \u00b1 0.0003, and 0.0062 \u00b1 0.0008 mSv/MBq for 50, 100, and 150 \u03bcg/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 \u03bcg/injected mass. The highest tumor lesion/background ratios were observed 6 h after the administration of 100 \u03bcg 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.", "doi": "10.1021/acsptsci.4c00637", "pmid": "40109737", "labels": [], "xrefs": [{"db": "pmc", "key": "PMC11915028"}], "notes": [], "created": "2026-09-23T11:30:23.820Z", "modified": "2026-09-23T11:30:23.875Z"}