Novel Covalent FAP-Targeted [ <sup>68</sup> Ga]Ga-DOTA-mFS-KERERG-FAP-2286 for Improved Pharmacokinetics and Enhanced Tumor Uptake
Zhongcai JinInstitute of Nuclear MedicineTongtong WuNuclear Medicine and Theranostics Key Laboratory of Sichuan ProvinceShijie TangDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaYanggang LiuNuclear Medicine and Theranostics Key Laboratory of Sichuan ProvinceYuqi AiDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaQiang WanNuclear Medicine and Theranostics Key Laboratory of Sichuan ProvinceYan ZhaoDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaShuang YanSouthwest Medical UniversityJie ZengMolecular Theranostics (United States)Naiguo XingDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaYang LiuMolecular Theranostics (United States)Lin ChenNuclear Medicine and Theranostics Key Laboratory of Sichuan ProvinceZhijun ZhouMolecular Theranostics (United States)Chen YSouthwest Medical UniversityLin QiuInstitute of Nuclear Medicine
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Ga]Ga-DOTA-mFS-KERERG-FAP-2286 lies in its design as a derivative of the DOTA-FAP-2286 scaffold, incorporating a sulfur(VI) fluoride exchange (SuFEx)-based covalent warhead and a hydrophilic polypeptide. This modification is anticipated to alter the pharmacokinetic profile, leading to enhanced tumor uptake and retention, thereby improving clinical diagnostic accuracy.
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