Multimodality Imaging and Preclinical Evaluation of 177Lu-AMBA for Human Prostate Tumours in a Murine Model

AMBA (DO3A-CH(2)CO-G-(4-aminobenzoyl)-QWAVGHLM-NH(2)) is a bombesin (BN)-like peptide having high affinity with gastrin-releasing peptide receptors (GRPr).(177)Lu-AMBA is currently undergoing clinical trial as a systemic radiotherapy for hormone refractory prostate cancer (HRPC) patients. This study...

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Bibliographic Details
Published in:Anticancer research 2010-10, Vol.30 (10), p.4039-4048
Main Authors: LIU, I-Hsiang, CHANG, Chih-Hsien, LEE, Te-Wei, HO, Chung-Li, CHIU, Shu-Pei, LEE, Wan-Chi, CHANG, Tsui-Jung, CHEN, Liang-Cheng, WU, Yu-Hsien, CHUANG, Cheng-Hui, FU, Ying-Kai
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Cell Line, Tumor
Humans
Isotope Labeling
Luminescent Measurements - methods
Lutetium
Male
Medical sciences
Mice
Mice, SCID
Nephrology. Urinary tract diseases
Oligopeptides - blood
Oligopeptides - pharmacokinetics
Prostatic Neoplasms - blood
Prostatic Neoplasms - diagnostic imaging
Prostatic Neoplasms - metabolism
Radioisotopes
Radiopharmaceuticals - blood
Radiopharmaceuticals - pharmacokinetics
Tissue Distribution
Tomography, Emission-Computed, Single-Photon - methods
Transplantation, Heterologous
Tumors
Tumors of the urinary system
Urinary tract. Prostate gland
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Description
Summary:AMBA (DO3A-CH(2)CO-G-(4-aminobenzoyl)-QWAVGHLM-NH(2)) is a bombesin (BN)-like peptide having high affinity with gastrin-releasing peptide receptors (GRPr).(177)Lu-AMBA is currently undergoing clinical trial as a systemic radiotherapy for hormone refractory prostate cancer (HRPC) patients. This study evaluated the biodistribution, pharmacokinetics, bioluminescent imaging (BLI) and microSPECT/CT imaging of (177)Lu-AMBA in PC-3M-luc-C6 luciferase-expressing human prostate tumour-bearing mice. Plasma stability of (177)Lu-AMBA could be maintained up to 55.67±6.07% at 24 h in a protection buffer. High positive correlations of PC-3M luc-C6 tumour growth in SCID mice between caliper measurement and BLI were observed (R(2)=0.999). Both the biodistribution and microSPECT/CT imaging in PC-3M-luc-C6 bearing-tumour mice showed that (177)Lu-AMBA in tumour uptake could be retained for 24 h. The distribution half-life (t(1/2α)) and the elimination half-life (t(1/2β)) of (177) Lu-AMBA in mice were 0.52 h and 26.6 h, respectively. These results indicated that BLI could be used to monitor the growth of tumour. High uptake of (177)Lu-AMBA in PC-3M-luc-C6 tumour-bearing mice by microSPECT/CT imaging can further evaluate the potential of (177)Lu-AMBA therapy for PC-3M-luc-C6 tumours.
ISSN:0250-7005
1791-7530