FAPI dimer compound, FAPI dimer-based positron emission tomography (PET) imaging agent for tumor diagnosis, and preparation method and use thereof
US11952368B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Sep 29, 2022 |
| Grant date | Apr 9, 2024 |
| Priority date | — |
| Expiry date | Sep 29, 2042 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY02P20/55
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.