ArticleAnnals of nuclear medicine2026
Preclinical evaluation of novel
Article in Annals of nuclear medicine, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
1 citing paper in PubMed.
- Head-to-Head Comparison of Monomeric, Homodimeric, and Heterodimeric Fibroblast Activation Protein-Targeting Radioligands Based on Small Molecule Inhibitor and Cyclic Peptide.ACS pharmacology & translational science · 2026Article
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12 authors.
Funding
Abstract
objectiveFibroblast activation protein (FAP) is a promising biomarker for the development of tumor-targeting agents. To date, various FAP-targeting radioligands have been developed. In particular, [68Ga]Ga/[177Lu]Lu-FAPI-46 are recognized as prospective FAP-targeting radioligands. However, the therapeutic efficacy of [177Lu]Lu-FAPI-46 for radioligand therapy (RLT) is limited due to its insufficient tumor accumulation. To address this issue, we previously reported an albumin binder (ALB)-conjugated FAP-targeting radioligand, [111In]In-FAPI-46-I. [111In]In-FAPI-46-I demonstrated higher tumor accumulation than [111In]In-FAPI-46, suggesting its potential utility for FAP-targeted RLT. In this study, we radiolabeled FAPI-46-I with 177Lu, a widely used therapeutic radionuclide, and evaluated its utility as a FAP-targeted RLT agent.
methods[177Lu]Lu-FAPI-46-I was synthesized by incubating the precursor with [177Lu]LuCl3 in acetate buffer. In vitro stability of [177Lu]Lu-FAPI-46-I was evaluated in murine plasma for 24 h. An in vitro cell competition binding assay was performed using U87MG cells with high FAP expression. The pharmacokinetics of [177Lu]Lu-FAPI-46-I was evaluated using U87MG tumor-bearing mice. A SPECT/CT study was conducted using U87MG (high FAP expression) and HT-1080 (low FAP expression) tumor-bearing mice. An RLT study was also carried out using U87MG tumor-bearing mice, comparing the therapeutic effects of [177Lu]Lu-FAPI-46-I, [177Lu]Lu-FAPI-46, and vehicle control.
results[177Lu]Lu-FAPI-46-I was synthesized with high radiochemical purity and exhibited marked stability in murine plasma for 24 h. The FAP-binding affinity of [natLu]Lu-FAPI-46-I (IC50 = 1.5 ± 0.3 nM) was comparable with that of [natIn]In-FAPI-46-I and [natIn]In-FAPI-46. [177Lu]Lu-FAPI-46-I exhibited prolonged blood retention and enhanced tumor accumulation due to the interaction between its ALB moiety and albumin in blood, resulting in selective accumulation in FAP-expressing tumors. Furthermore, administration of [177Lu]Lu-FAPI-46-I led to tumor growth suppression and shrinkage, demonstrating superior therapeutic efficacy compared with [177Lu]Lu-FAPI-46.
conclusion[177Lu]Lu-FAPI-46-I achieved prolonged tumor accumulation and marked tumor growth inhibition. Therefore, [177Lu]Lu-FAPI-46-I is a promising candidate for FAP-targeted RLT.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.