Pharmacokinetic characterization of fibroblast activation protein-targeting radiotherapeutic drugs
10.3760/cma.j.cn321828-20241016-00351
- VernacularTitle:靶向成纤维细胞激活蛋白放射性治疗药物药代动力学特征分析
- Author:
Zhirong ZHANG
1
;
Tianhong ZHANG
1
;
Ming HAO
1
;
Jie YAN
1
Author Information
1. 青岛峰玺协同创新医药技术开发有限公司，青岛 266100
- Publication Type:Journal Article
- Keywords:
Membrane proteins;
Radiopharmaceuticals;
Drug therapy;
Pharmacokinetics;
FAP;
Trends
- From:
Chinese Journal of Nuclear Medicine and Molecular Imaging
2025;45(9):566-570
- CountryChina
- Language:Chinese
-
Abstract:
Fibroblast activation protein (FAP) has attracted much attention as a pan-cancer target with tumor-specific expression. Successful translation of FAP-targeting radiotherapeutic drugs requires a multidisciplinary approach, in which ideal pharmacokinetic (PK) characteristics are essential. This paper summarizes the PK mechanisms governing systemic clearance, tissue distribution, cellular uptake, and intracellular retention of various ligands (such as organic small molecules, peptide mid-molecules, non-peptide mid-molecules, and antibody macromolecules), analyzes the advantages and disadvantages of FAP-targeting ligands based on non-clinical PK data, and reviews PK alterations following various modification strategies (such as antibody fragmentation, albumin binding, homo- or hetero-polymerization, and click chemistry modifications), as well as the comparison of clinical PK data of different FAP-targeting radiotherapeutic drugs. This review aims to provide references for the development of FAP-targeting radiotherapeutic drugs in the industry.
