Novel Covalent FAP-Targeted [ <sup>68</sup> Ga]Ga-DOTA-mFS-KERERG-FAP-2286 for Improved Pharmacokinetics and Enhanced Tumor Uptake
Zhongcai JinDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaTongtong WuDepartment of Pharmacy, The Second People’s Hospital of Neijiang, 470 Xinjiang Road, Dongxing District, Neijiang, Sichuan 641000, People’s Republic of ChinaShijie TangDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaYanggang LiuDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaYuqi AiDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaQiang WanDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaYan ZhaoDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaShuang YanDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaJie ZengDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaNaiguo XingDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaYang LiuDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaLin ChenDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaZhijun ZhouDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaChen YDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of ChinaLin QiuDepartment of Nuclear Medicine, Affiliated Hospital of Southwest Medical University, No. 25 Taiping St, Jiangyang District, Luzhou, Sichuan 646000, People’s Republic of China
ABI
Abstract
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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