Development of Cysteic Acid-Modified FAP Radioligands for Enhanced Renal Clearance: From Preclinical Optimization to First-in-Human Study.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.5c01163
Abstract: Fibroblast activation protein (FAP)-targeting radioligands hold promise for cancer theranostics. Cyclic peptide-based DOTA-FAP-2286 radioligands have demonstrated high kidney uptake and retention, raising concerns regarding potential nephrotoxicity. Hence, we aimed to design three cysteic acid-modified FAP-targeting… read more here.
Keywords: acid modified; modified fap; fap 2286; cysteic acid ... See more keywords
Feasibility of Early 68Ga-FAP-2286 PET Imaging: A Case Study.
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DOI: 10.1097/rlu.0000000000005519
Abstract: ABSTRACT Fibroblast activation protein (FAP) has emerged as a promising molecular target for diagnostic and therapeutic strategies. Previous research, including our own study and other published reports, has highlighted the potential of FAP inhibitors labeled… read more here.
Keywords: feasibility early; early 68ga; fap 2286; pet ... See more keywords
Visualization of the Gallbladder on 177Lu-FAP-2286 SPECT/CT Imaging: A Potential Pitfall.
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DOI: 10.1097/rlu.0000000000006209
Abstract: Fibroblast activation protein (FAP) is a membrane-bound protease predominantly expressed on the surface of cancer-associated fibroblasts activated within the solid tumor microenvironment, while its expression remains minimal in normal tissues. Following radiolabeling, FAP-2286 has demonstrated… read more here.
Keywords: gallbladder 177lu; visualization gallbladder; 177lu fap; fap 2286 ... See more keywords
Abstract 4599: Preclinical evaluation, and clinical translation of 68Ga/177Lu-JH04, a novel FAP-targeting radiolabeled agent
Sign Up to like & getrecommendations! Published in 2025 at "Cancer Research"
DOI: 10.1158/1538-7445.am2025-4599
Abstract: Fibroblast activation protein (FAP) is an ideal target for tumor imaging and therapy. To enhance tumor uptake and prolong the retention of FAP-targeting agents, we developed JH04, a novel cyclic peptide composed of a FAP-targeting… read more here.
Keywords: fap targeting; 177lu jh04; fap 2286; tumor ... See more keywords
Autophagy inhibition improves the targeted radionuclide therapy efficacy of 131I-FAP-2286 in pancreatic cancer xenografts
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DOI: 10.1186/s12967-024-04958-6
Abstract: Radiotherapy can induce tumor cell autophagy, which might impair the antitumoral effect. This study aims to investigate the effect of autophagy inhibition on the targeted radionuclide therapy (TRT) efficacy of 131I-FAP-2286 in pancreatic cancer. Human… read more here.
Keywords: pancreatic cancer; fap 2286; tumor; 131i fap ... See more keywords
Comparison of 68Ga-FAP-2286 and 18F-FDG PET/CT in the diagnosis of advanced lung cancer
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DOI: 10.3389/fonc.2024.1413771
Abstract: Purpose The 68Ga/177Lu-FAP-2286 is a newly developed tumor imaging agent that shows potential for visualizing and treating tumor stroma. The objective of this research was to evaluate the effectiveness of 68Ga-FAP-2286 PET/CT and 18F-FDG PET/CT… read more here.
Keywords: fdg pet; lung cancer; fap 2286; 18f fdg ... See more keywords
[68Ga]Ga-FAP-2286—Synthesis, Quality Control and Comparison with [18F]FDG PET/CT in a Patient with Suspected Cholangiocellular Carcinoma
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DOI: 10.3390/ph17091141
Abstract: [68Ga]Ga-FAP-2286 is a new peptide-based radiopharmaceutical for positron-emission tomography (PET) that targets fibroblast activation protein (FAP). This article describes in detail the automated synthesis of [68Ga]Ga-FAP-2286 using a commercially available synthesis tool that includes quality… read more here.
Keywords: fap 2286; synthesis; quality control; 68ga fap ... See more keywords