FAP-targeted radioligand therapy — pancreatic, sarcoma, breast, head-and-neck investigational evidence. Curated daily from Europe PMC (PubMed + PMC + preprints) and OpenAlex — free-full-text link on each open-access paper.
Irina Vierasu, Francesco Sclafani, Jean‐Luc Van Laethem, Wendy Delbart et al.
Colorectal cancer liver metastases (CRLM) are characterized by distinct histopathological growth patterns (HGPs), desmoplastic (dHGP) also called encapsulated, replacement (rHGP) and pushing (pHGP) types, which have major prognostic and therapeutic implications. HGPs can only be determined histologically after surgical resection. This review explores molecular imaging as a pote…
Purpose: Radionuclide therapy targeting fibroblast activation protein (FAP) offers an effective treatment for tumors with high FAP expression, such as those imaged with 68 Ga-fibroblast activation protein inhibitor (FAPI) and treated with 177 Lu-FAPI. Personalized therapy planning, based on imaging-derived standardized uptake values, pharmacokinetic parameters, and dosimetric m…
Fibroblast activation protein-α (FAP) is an attractive cell surface target for radiopharmaceutical development due to its tumor-restricted expression. This study aimed to develop a novel dimeric FAP inhibitor (FAPI), DOTA-PEG4-CO-N-bis(PEG4-7N) (D7ND), and evaluate its potential as a therapeutic radiopharmaceutical in preclinical models and clinical studies. The precursor D7ND …
Fibroblast activation protein (FAP) and integrin αvβ3 are attractive theranostic targets. We developed a dual-targeting radiotheranostic agent, 177Lu-DOTA-FAPI-RGD (177Lu-LNC1009), and conducted a first-in-human study to evaluate its safety, biodistribution, dosimetry, and preliminary efficacy in patients with advanced adenocarcinomas. Methods: LNC1009 was synthesized by conjug…
Luca Russo, Ossian Longoria, Silvia Bottazzi, Nuria Porta et al.
Background Unequivocal clinical progression without radiological progression according to Prostate Cancer Clinical Trials Working Group 3 (PCWG3) criteria is recognised in metastatic castration-resistant prostate cancer (mCRPC), reflecting limitations of bone scintigraphy in distinguishing an osteoblastic progression from an osteoblastic flare. Objective To compare the METastas…
Abstract Purpose: This study aimed to evaluate the efficacy, safety, and prognostic value of fibroblast activation protein (FAP)-targeted radioligand therapy (RLT) using 177 Lu-FAP-2286 in patients with end-stage metastatic cancer. Patients and Methods: In this single-center retrospective study, 31 patients with end-stage metastatic cancer who had exhausted standard therapies w…
Fibroblast activation protein (FAP)-targeted radiotheranostics show strong promise for cancer imaging and therapy, yet their clinical translation is limited by the trade-off between rapid tumor targeting and insufficient systemic residence time. To address this challenge, we report the design and evaluation of 177Lu-Albb-2FAPI, a long-acting dimeric FAPI derivative that integra…
This study evaluated the imaging performance, tumor retention, and therapeutic potential of two new FAPI homodimers, DOTAGA.Glu2.(FAPI)2 and DOTAGA.PEG2.Glu.(FAPI)2, specifically designed to improve FAP-targeted tumor retention. DOTAGA.Glu2.(FAPI)2 and DOTAGA.PEG2.Glu.(FAPI)2 were radiolabeled with gallium-68 and lutetium-177. In vitro studies included lipophilicity, protein bi…
Al-Ibraheem A, Moghrabi S, Al-Houwari RM, Al-Qasem S et al.
Radiotheranostics is reshaping precision oncology by integrating molecular imaging with targeted radionuclide therapy through matched diagnostic-therapeutic radiopharmaceutical pairs. Landmark clinical successes, including Lutetium-177-DOTATATE (177Lu-DOTATATE) and 177Lu-prostate-specific membrane antigen-617 (177Lu-PSMA-617), have validated this approach and accelerated the sh…
In the last decade, fibroblast activation protein-α inhibitors (FAPIs), which target the cancer-associated fibroblasts of the tumour microenvironment, have become a topic of great interest. In oncology, FAPI PET/CT imaging has repeatedly demonstrated a higher lesion detection rate than other conventional imaging modalities such as CT or 18F-FDG PET/CT for several tumours. In so…
AimTo evaluate and compare the diagnostic performance of [68Ga]Ga-DOTA-FAPI-04 with [18F]F-FDG and [68Ga]Ga-DOTATATE PET/CT for detecting recurrent disease in patients with medullary thyroid carcinoma (MTC) and additionally evaluate their role for prognostication and theranostics in management of MTC.MethodsIn this prospective single-centre study, 56 patients with suspected rec…
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