dataset
posted on 2025-08-01, 07:21 authored by Tongtong Wu, Zhicong Yang, Sufan Tang, Hongmei Yuan, Yang Liu, Haiyang Li, Nan Liu, Zhanwen Huang, Yue Chen, Zhijun Zhou <p>Table S1. Stability data of 68Ga and 177Lu complexes of DOTA-LP, DOTA-ALB-01, DOTA-ALB-02, and DOTA-ALB-03 in human serum (HS)and PBS buffer, expressed as the percentage of stable complexes (percentage of labeled compound to free activity found at a given time point), with the corresponding analytical conditions detailed in the main text.</p>
Funding
Luzhou-Southwest Medical University Cooperative Application Foundation
Doctoral Research Initiation Fund of Affiliated Hospital of Southhwest Medical University
National Natural Science Foundation of China (NSFC)
History
ARTICLE ABSTRACT
Fibroblast activation protein (FAP) is overexpressed on cancer-associated fibroblasts, making it an important target for cancer diagnosis and treatment, but limited tumor retention hinders late-stage diagnosis and radionuclide therapy. In this study, three albumin-bound FAP inhibitor (FAPI) radioligands, 68Ga/177Lu-DOTA-ALB-01, 68Ga/177Lu-DOTA-ALB-02, and 68Ga/177Lu-DOTA-ALB-03, were synthesized and evaluated for their in vitro stability, binding affinity, in vivo biodistribution, and tumor uptake using 68Ga and 177Lu labeling. All radioligands are stable in saline and plasma and exhibit high FAP-binding affinity. 177Lu-DOTA-ALB-02 has longer retention in circulation than 177Lu-FAPI-46 and other radioligands. Continuous tumor accumulation was observed during imaging with both 177Lu-DOTA-ALB-01 and 177Lu-DOTA-ALB-02. Notably, 177Lu-DOTA-ALB-02 had a significant tumor/nontarget ratio as indicated by biodistribution data. The outstanding tumor retention properties of 177Lu-DOTA-ALB-02 have been demonstrated in small-animal single-photon emission computed tomography imaging and biodistribution studies; therefore, it is considered the albumin-binding FAPI with the most favorable pharmacokinetic and imaging properties, worthy of further clinical investigation.
