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Fibroblasts activated protein (FAP) appears to be a promising target for tumor theranostics. However, the development of radioiodinated probes for FAP has been slow. In this study, a progressive abumin-driven strategy was adopted to improve the FAP-targeted delivery of radioiodinated probes for tumor theranostics. A series of FAP-targeted probes (namely 131 IIPB-FAPI, 131 IIPB-FAPI-A1, 131 IIPB-FAPI-A3, 131 IFSDD 3 I) were synthesized by incorporating an albumin-binding moiety (4-( p -iodophenyl)butyric acid, 4-IPBA) labeled with radioiodine . The specificity and binding characteristics of the radiotracers to FAP and human serum albumin (HSA) were confirmed. SPECT imaging results showed that the 131 IFSDD 3 I had more prominent tumor retention property and superior target-to-nontarget ratio, which were consistent with the biodistribution results. As expected, the FAP-targeted therapy with 11.1 MBq 131 IFSDD 3 I significantly inhibited tumor growth. In conclusion, this proof-of-concept study employed a progressive design strategy to enhance pharmacokinetics of radioiodinated FAP-targeted probes. Among these radioiodinated FAPI probes, 131 I-labeled FSDD 3 I ( 131 IFSDD 3 I) emerged as a standout candidate with superior competitive advantages for application in radioiodine-guided internal irradiation therapy.
Li et al. (Fri,) studied this question.