{"entity": "publication", "iuid": "1bb6a2b629274e35a5ecea07c4372fca", "timestamp": "2026-08-20T20:25:20.432Z", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/1bb6a2b629274e35a5ecea07c4372fca.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/1bb6a2b629274e35a5ecea07c4372fca"}}, "title": "Ga-68-Labeled Affibody Molecule-Based Radiopharmaceutical Targeting Platelet Derived Growth Factor Receptor Beta for Detection of Active Fibrosis in Patients with Myocardial Infarction.", "authors": [{"family": "Velikyan", "given": "Irina", "initials": "I", "orcid": "0000-0002-3732-8857", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/947ae561cd794e5b94c6736880620287.json"}}, {"family": "Grinnemo", "given": "Karl-Henrik", "initials": "KH"}, {"family": "Flodin", "given": "Viktor", "initials": "V"}, {"family": "James", "given": "Stefan", "initials": "S"}, {"family": "Thelander", "given": "Ulrika", "initials": "U", "orcid": "0000-0002-6647-0967", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/32aaf2779ea844fb90b434b62c3be4fc.json"}}, {"family": "Wagner", "given": "Michael", "initials": "M"}, {"family": "Rodin", "given": "Sergey", "initials": "S"}, {"family": "Kero", "given": "Tanja", "initials": "T"}, {"family": "Korsgren", "given": "Olle", "initials": "O", "orcid": "0000-0002-8524-9547", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/f4f384eeb31a4b2dba5c9301bb34c156.json"}}, {"family": "Eriksson", "given": "Olof", "initials": "O", "orcid": "0000-0002-2515-8790", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/85991bf00e4b4a26ab15599d25c58601.json"}}], "type": "journal article", "published": "2025-12-01", "journal": {"title": "Pharmaceuticals (Basel, Switzerland)", "issn": "1424-8247", "volume": "18", "issue": "12", "issn-l": "1424-8247"}, "abstract": "Introduction: Platelet-derived growth factor receptor beta (PDGFR\u03b2) is a key regulator of fibrogenesis. Non-invasive imaging of PDGFR\u03b2 expression may offer a novel approach to assess fibrotic remodeling, particularly in cardiac patients' post-intervention, where fibrosis poses clinical risk. This study presents the GMP-compliant production of a novel PDGFR\u03b2-targeted PET radiopharmaceutical, [68Ga]Ga-DOTA-Z09591 ([68Ga]Ga-ATH001), and its preclinical evaluation in mouse and human myocardial tissue, along with initial clinical imaging in patients with ST-elevation myocardial infarction (STEMI). Methods: The precursor was chemically synthesized and radiolabeled with gallium-68 using a fully automated, GMP-compatible system and a pharmaceutical-grade 68Ge/68Ga generator. Autoradiography, H&E, Sirius Red, Masson's trichrome, and IHC staining were performed on infarcted mouse hearts and human myocardial biopsies. In vivo PET/MRI with [68Ga]Ga-ATH001, 15O-H2O, and gadolinium contrast was conducted in STEMI patients one week post-percutaneous coronary intervention. Results: [68Ga]Ga-ATH001 was produced with high radiochemical yield and purity. Autoradiography demonstrated specific, receptor-mediated binding of [68Ga]Ga-ATH001, co-localizing with PDGFR\u03b2 immunoreactivity, collagen deposition, and tissue damage. In STEMI patients, focal tracer uptake was observed in infarcted myocardium correlating with MRI-detected structural abnormalities and perfusion defects on 15O-H2O PET. Uptake in unaffected myocardium was low and homogeneous, consistent with minimal physiological PDGFR\u03b2 expression. Conclusions: [68Ga]Ga-ATH001 was successfully developed and validated for phase 0 clinical study. The tracer demonstrated PDGFR\u03b2-specific binding in human fibrotic myocardium and enabled non-invasive detection of myocardial fibrogenic activity in STEMI patients. These findings support further clinical evaluation of [68Ga]Ga-ATH001 as a targeted molecular imaging agent for early assessment of post-infarction fibrosis.", "doi": "10.3390/ph18121833", "pmid": "41471324", "labels": [], "xrefs": [{"db": "pmc", "key": "PMC12735932"}, {"db": "pii", "key": "ph18121833"}], "notes": [], "created": "2026-08-20T13:42:54.944Z", "modified": "2026-08-20T13:42:55.058Z"}