Pagou Margarita, Zerizer Imene, Al-Nahhas Adil
Hell J Nucl Med. 2009 May-Aug;12(2):102-5.
The development of gallium-68 -1,4,7,10-tetraazacyclodecane-1,4,7,10-tetraacetic acid ((68)Ga-DOTA) compounds was made possible due to the chemistry of (68)Ga, which matches the pharmacokinetics of many peptides, specially the chelators DOTA and DOTAderivatives with the formation of stable (68)Ga (3+) complexes. The availability of this tracer from a germanium-68-gallium-68 generator with a relatively long half-life makes it attractive to use in busy nuclear medicine departments, particularly those with limited access to cyclotrons. The recent clinical experience with (68)Ga-peptides includes imaging neuroendocrine tumours particularly carcinoid, as well as neuroectodermal tumours such as phaeochromocytoma and paraganglioma. In vitro and animal testing are still progressing alongside clinical studies, with promising results in the use of (68)Ga-DOTA-rhenium-cyclized alpha-melanocyte stimulating hormone (MSH) and (68)Ga-DOTA-napamide (NAP) in melanoma, (68)Ga-DOTA-PEG(4)-BN(7-14) (PESIN) for the imaging of bombesin receptor- positive tumours and (68)Ga-ethylene dicysteine-metronidazole (EC-MN) for imaging tumour hypoxia. In addition to tumours, (68)Ga- DOTA peptide inhibitor of vascular peptide protein 1(VAP-P1) is being assessed for imaging inflammatory reaction. An additional value following a positive scan is the use of beta emitters labelled to the same peptides for radionuclide treatment. In conclusion, the recent introduction of (68)Ga-peptides, made available by a convenient (68)Ga/(68)Ge generator, could greatly contribute to the management of a wide range of clinical conditions including tumours and inflammation.
镓-68 - 1,4,7,10 - 四氮杂环十二烷-1,4,7,10 - 四乙酸((68)Ga - DOTA)化合物的研发得益于镓-68的化学性质,其与许多肽的药代动力学相匹配,特别是螯合剂DOTA及其衍生物能形成稳定的(68)Ga(3+)络合物。这种示踪剂可从半衰期相对较长的锗-68 - 镓-68发生器获得,这使得它在繁忙的核医学科室颇具吸引力,尤其是那些难以使用回旋加速器的科室。近期(68)Ga - 肽的临床经验包括对神经内分泌肿瘤特别是类癌的成像,以及对神经外胚层肿瘤如嗜铬细胞瘤和副神经节瘤的成像。体外和动物试验仍与临床研究同步进行,在黑色素瘤中使用(68)Ga - DOTA - 铼 - 环化α - 黑素细胞刺激素(MSH)和(68)Ga - DOTA - 萘酰胺(NAP)、用于胃泌素释放肽受体阳性肿瘤成像的(68)Ga - DOTA - 聚乙二醇(4)- BN(7 - 14)(PESIN)以及用于肿瘤缺氧成像的(68)Ga - 乙二胱氨酸 - 甲硝唑(EC - MN)方面都取得了有前景的结果。除肿瘤外,正在评估用于血管肽蛋白1(VAP - P1)成像的(68)Ga - DOTA肽抑制剂对炎症反应的成像。阳性扫描后的一个额外价值是使用标记相同肽的β发射体进行放射性核素治疗。总之,由便捷的(68)Ga/(68)Ge发生器提供的(68)Ga - 肽的近期引入,可为包括肿瘤和炎症在内的广泛临床病症的管理做出巨大贡献。