In vitro and in vivo metabolism of Lu-AMBA, a GRP-receptor binding compound, and the synthesis and characterization of its metabolites.

@article{Linder2009InVA,
  title={In vitro and in vivo metabolism of Lu-AMBA, a GRP-receptor binding compound, and the synthesis and characterization of its metabolites.},
  author={Karen E Linder and Edmund C Metcalfe and Thangavel Arunachalam and Jianqing Chen and Stephen M Eaton and Weiwei Feng and Hong Wei Fan and Natarajan Raju and Aldo Cagnolini and Laura E. Lantry and Adrian D. Nunn and Rolf E. Swenson},
  journal={Bioconjugate chemistry},
  year={2009},
  volume={20 6},
  pages={1171-8}
}
The metabolism of (177)Lu-AMBA (AMBA = DO3A-CH(2)CO-G-(4-aminobenzoyl)-QWAVGHLM-NH(2)), a radiotherapeutic compound in clinical development that binds to GRP and NMB receptors, was studied in vitro (mouse, rat and human plasma, mouse kidney homogenate) and in vivo (by analysis of mouse and rat plasma and urine following IV injection of (177)Lu-AMBA). The primary metabolites were Lu-DO3A-CH(2)CO-G-Abz4-R, where R = -Q-OH (A), -QW-OH (B), and -QWAVGH-OH (C). Minor amounts of (D) where R… CONTINUE READING