title: Molecular imaging, pharmacokinetics, and dosimetry of In-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(2)CO-G-4-aminobenzoyl-Q-W-A-V-G-H-L-M-NH(2) (AMBA) in vitro, MicroSPECT/CT imaging, and biological activities of (111)In-AMBA in PC-3 prostate tumor-bearing SCID mice. The uptake of (111)In-AMBA reached highest with 3.87 ± 0.65% ID/g at 8 h. MicroSPECT/CT imaging studies suggested that the uptake of (111)In-AMBA was clearly visualized between 8 and 48  h postinjection. The distribution half-life (t(1/2α)) and the elimination half-life (t(1/2β)) of (111)In-AMBA in mice were 1.53  h and 30.7  h, respectively. The C(max) and AUC of (111)In-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 (111)In-AMBA in the GRPR-overexpressed PC-3 tumor-bearing SCID mice. (111)In-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.
authors.affiliation: Isotope Application Division, Institute of Nuclear Energy Research, Taoyuan 32546, Taiwan.
authors.forename: Chung-Li
authors.initials: CL
authors.lastname: Ho
authors.forename: I-Hsiang
authors.initials: IH
authors.lastname: Liu
authors.forename: Yu-Hsien
authors.initials: YH
authors.lastname: Wu
authors.forename: Liang-Cheng
authors.initials: LC
authors.lastname: Chen
authors.forename: Chun-Lin
authors.initials: CL
authors.lastname: Chen
authors.forename: Wan-Chi
authors.initials: WC
authors.lastname: Lee
authors.forename: Cheng-Hui
authors.initials: CH
authors.lastname: Chuang
authors.forename: Te-Wei
authors.initials: TW
authors.lastname: Lee
authors.forename: Wuu-Jyh
authors.initials: WJ
authors.lastname: Lin
authors.forename: Lie-Hang
authors.initials: LH
authors.lastname: Shen
authors.forename: Chih-Hsien
authors.initials: CH
authors.lastname: Chang
mesh_terms: D000818:Animals; D001839:Bombesin / Q000378:metabolism; D045744:Cell Line, Tumor; D057809:HEK293 Cells; D006207:Half-Life; D006801:Humans; D007205:Indium Radioisotopes / Q000493:pharmacokinetics*; D007553:Isotope Labeling; D008297:Male; D051379:Mice; D016513:Mice, SCID; D057054:Molecular Imaging / Q000379:methods*; D009842:Oligopeptides / Q000493:pharmacokinetics*; D011471:Prostatic Neoplasms / Q000000981:diagnostic imaging*; D011874:Radiometry / Q000379:methods; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D018004:Receptors, Bombesin / Q000378:metabolism; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon / Q000379:methods; D014183:Transplantation, Heterologous
chemical_list: C512446:DO3A-CH2CO-G-4-aminobenzoyl-Q-W-A-V-G-H-L-M-NH2; D007205:Indium Radioisotopes; D009842:Oligopeptides; D019275:Radiopharmaceuticals; D018004:Receptors, Bombesin; D001839:Bombesin