Evidence map›Paper›PMID 41979762›Full record

ArticleEJNMMI research2026

Preliminary study of FAP-targeted radiopharmaceuticals based on covalent targeting strategy and pharmacokinetic characteristics.

Yiheng Ai, Zhongcai Jin, Tongtong Wu, Yi Li, Yanggang Liu, Jing Yang, Shijie Tang, Yue Chen, Lin Qiu

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in EJNMMI research, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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1 · What the graph read from it

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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.

2 · The registry

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3 · Its place in the literature

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4 · The record

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5 · Who and what money

Authors and funding

9 authors.

Yiheng Ai *Department of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25, Taiping St., Luzhou, 646000, Sichuan, PR China.
Zhongcai Jin *Department of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25, Taiping St., Luzhou, 646000, Sichuan, PR China.
Tongtong Wu *Department of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25, Taiping St., Luzhou, 646000, Sichuan, PR China.
Yi Li *Department of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25, Taiping St., Luzhou, 646000, Sichuan, PR China.
Yanggang LiuDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25, Taiping St., Luzhou, 646000, Sichuan, PR China.
Jing YangDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25, Taiping St., Luzhou, 646000, Sichuan, PR China.
Shijie TangDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25, Taiping St., Luzhou, 646000, Sichuan, PR China.
Yue ChenDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25, Taiping St., Luzhou, 646000, Sichuan, PR China.
Lin QiuDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25, Taiping St., Luzhou, 646000, Sichuan, PR China. qiulin17111210041@163.com.ORCID http://orcid.org/0000-0002-1010-5020

Funding

Health Commission of Sichuan Province Medical Science and Technology Program Project No. 24QNMP093Natural Science Foundation of Sichuan Province Project No. 2023YFS0091Project of Luzhou Science and Technology Bureau Project No. 2025JYJ014Special Funding for Cultivation of Defense Talents Project No. CW202410Youth Innovation Project of Sichuan Medical Association Project No. Q20250004
6 · The paper itself

Abstract

backgroundIn tumor imaging and therapy, fibroblast activation protein (FAP)-targeted radiotracers remains a research hotspot. The recently reported [68Ga]Ga/[177Lu]Lu-DOTA-mFS-FAPI-04 has been demonstrated to address limitations in conventional FAP-targeted agents, such as low tumor uptake, short retention time, and suboptimal therapeutic efficacy. However, [68Ga]Ga-DOTA-mFS-FAPI-04 positron emission tomography (PET) clinical imaging revealed high uptake in salivary glands, thyroid, and pancreas, necessitating further structural optimization. To address this limitation, we developed two novel radiopharmaceuticals.

results[68Ga]Ga-DOTA-mFS-FAP-2286 and [68Ga]Ga-DOTA-mFS-KERERG-FAP-2286 demonstrated favorable targeting specificity and diagnostic efficacy. [68Ga]Ga-DOTA-mFS-FAP-2286 exhibited dual excretion pathways (hepatobiliary and urinary systems), whereas [68Ga]Ga-DOTA-mFS-KERERG-FAP-2286 showed exclusive urinary excretion, demonstrating superior pharmacokinetic properties. [68Ga]Ga-DOTA-mFS-KERERG-FAP-2286 exhibited significantly enhanced tracer uptake compared to [68Ga]Ga-DOTA-FAP-2286 in primary tumors (SUVmax: 11.03 ± 1.45 vs. 5.47 ± 1.66), lymph node metastases (SUVmax: 12.13 ± 2.22 vs. 5.70 ± 1.08), and distant metastases (SUVmax: 12.03 ± 6.56 vs. 6.83 ± 0.36) (all p < 0.05).

conclusionBoth [68Ga]Ga-DOTA-mFS-FAP-2286 and [68Ga]Ga-DOTA-mFS-KERERG-FAP-2286 effectively overcame the drawback of high uptake in salivary glands, thyroid, and pancreas observed with [68Ga]Ga-DOTA-mFS-FAPI-04. [68Ga]Ga-DOTA-mFS-KERERG-FAP-2286 demonstrated superior pharmacokinetic characteristics with urinary excretion and showed the potential for superior diagnostic efficacy compared with [68Ga]Ga-DOTA-FAP-2286.

Indexed as

Covalent targeted drugsFAPLung cancerPET/CTPharmacokinetics

Identifiers

PMID41979762
PMCPMC13187106

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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.