Molecular imaging, pharmacokinetics, and dosimetry of 111In-AMBA in human prostate tumor-bearing mice

Abstract

Molecular imaging with promise of personalized medicine can provide patient-specific information noninvasively, thus enabling treatment to be tailored to the specific biological attributes of both the disease and the patient. This study was to investigate the characterization of DO3A-CH 2CO-G-4-aminobenzoyl-Q-W-A-V-G-H-L-M-NH2 (AMBA) in vitro, MicroSPECT/CT imaging, and biological activities of 111In-AMBA in PC-3 prostate tumor-bearing SCID mice. The uptake of 111In-AMBA reached highest with 3.87±0.65 %ID/g at 8h. MicroSPECT/CT imaging studies suggested that the uptake of 111In-AMBA was clearly visualized between 8 and 48h postinjection. The distribution half-life (t 1/2β) and the elimination half-life (t1/2) of 111In-AMBA in mice were 1.53h and 30.7h, respectively. The C max and AUC of 111In-AMBA were 7.57%ID/g and 66.39h()%ID/g, respectively. The effective dose appeared to be 0.11mSv/MBq -1. We demonstrated a good uptake of 111In-AMBA in the GRPR-overexpressed PC-3 tumor-bearing SCID mice. 111In-AMBA is a safe, potential molecular image-guided diagnostic agent for human GRPR-positive tumors, ranging from simple and straightforward biodistribution studies to improve the efficacy of combined modality anticancer therapy. Copyright © 2011 Chung-Li Ho et al.