Cage-like chelate, targeted cage-like chelating ligand, and complex and use thereof
By employing a cage-like chelate structure, the problems of instability and targeting issues in radionuclide chelation in radiopharmaceuticals are solved, thereby improving drug stability and targeting, reducing toxic side effects, and improving drug distribution and metabolic performance in vivo.
Patent Information
- Application Number
- PCT/CN2025/082680
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2024-12-31
- Filing Date
- 2025-03-14
- Publication Date
- 2026-07-09
AI Technical Summary
The chelation stability of radionuclides in existing radiopharmaceuticals is insufficient, leading to instability of the labeled radiopharmaceuticals and the deposition of free nuclides in bone, hematopoietic tissue, or other organs, causing radiation damage. The lack of systematic regulation of metabolic properties during drug molecule development increases development costs. The chelation reaction of nuclides affects the activity of heat-sensitive targeted functional structures. The secondary decay of nuclides leads to the decomposition of chelated structures or the delabeling of decay daughter nuclei, causing toxic side effects.
The cage-like chelate structure, similar to a clam-like molecular structure, improves the thermodynamic and kinetic stability of the metal complex in vivo, provides more connection sites, connects the target molecule and functional fragment, forms a targeted cage-like chelate ligand, and enhances the PKPD performance of the drug in vivo.
It improves the stability and targeting of radiopharmaceuticals, reduces the recoil nuclear effect of alpha nuclide decay, reduces toxic side effects, regulates in vivo distribution and metabolism, and improves drug-like properties.