Molecular Imaging, Pharmacokinetics, and Dosimetry of 111In-AMBA in Human Prostate Tumor-Bearing Mice

• Published in: BioMed research international 2011-01, Vol.2011 (2011), p.1-8
• Main Authors: Lee, Te-Wei, Lin, Wuu-Jyh, Shen, Lie-Hang, Chang, Chih-Hsien, Ho, Chung-Li, Chuang, Cheng-Hui, Lee, Wan-Chi, Chen, Chun-Lin, Liu, I-Hsiang, Wu, Yu-Hsien, Chen, Liang-Cheng
• Format: Article
• Language: English
• Subjects: Amino acids; Cancer therapies; Chemotherapy; Clinical trials; Dosimetry; Medicine; Molecular weight; Nuclear energy; Peptides; Prostate cancer; Radiation therapy; Studies
• ISSN: 1110-7243; 2314-6133; 1110-7251; 2314-6141
• DOI: 10.1155/2011/101497

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-CH2CO-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 8 h. MicroSPECT/CT imaging studies suggested that the uptake of 111In-AMBA was clearly visualized between 8 and 48 h postinjection. The distribution half-life (t1/2α) and the elimination half-life (t1/2β) of 111In-AMBA in mice were 1.53 h and 30.7 h, respectively. The Cmax⁡ and AUC of 111In-AMBA were 7.57% ID/g and 66.39 h∗% ID/g, respectively. The effective dose appeared to be 0.11 mSv/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.