公开(公告)号：US11952368B2

公开(公告)日：2024-04-09

申请号：US17956727

申请日：2022-09-29

Applicant: XIAMEN UNIVERSITY

Inventor： Haojun Chen ,  Liang Zhao ,  Qin Lin ,  Kaili Fu ,  Yizhen Pang ,  Zhide Guo ,  Jianyang Fang ,  Long Sun ,  Hua Wu

IPC: C07D401/14 ,  A61K51/04

CPC classification number: C07D401/14 ,  A61K51/0482

Abstract: Provided are a fibroblast activation protein inhibitor (FAPI) dimer compound, an FAPI dimer-based positron emission tomography (PET) imaging agent for tumor diagnosis, and a preparation method and use thereof. An amphiphilic polyethylene glycol (PEG) chain and a dimerized structure of FAPI in the FAPI dimer compound with a structure shown in formula I can improve the in vivo kinetic properties of the compound and prolong a residence time of the compound in a tumor, thereby improving the uptake and imaging effects in the tumor. The accurate tumor diagnosis can be achieved by labeling the FAPI dimer compound with a diagnostic nuclide (68Ga), which has promising application prospects in PET imaging for diagnosis and in the preparation of a therapeutic nuclide (such as 177Lu or 90Y)-labeled drug for treating a FAP-α-expressing tumor.