Verbruggen A M
Laboratory of Radiopharmaceutical Chemistry I.F.W., University Hospital Gasthuisberg, K.U. Leuven, Belgium.
Eur J Nucl Med. 1990;17(6-8):346-64. doi: 10.1007/BF01268027.
In the past four years most of the effort in radiopharmaceutical chemistry has been devoted to compounds for positron emission tomography, but widespread use of this technique is still compromised by its high cost. On the other hand, steady progress has also been made in the development of technetium-99m-labelled radiopharmaceuticals. A variety of 99mTc-labelled agents is now available or in clinical evaluation for the study of brain perfusion (99mTc-labelled HMPAO, ECD, MRP20), myocardial perfusion (99mTc-labelled MIBI, teboroxime and phosphines) and renal function (99mTc-MAG3, 99mTc-L,L-EC). Different direct reduction methods and indirect conjugation methods have been developed to label antibodies or their fragments efficiently with 99mTc with preservation of immunoreactivity. However, the strict requirements of the regulatory authorities with respect to purification and quality of these preparations limit their use drastically in clinical practice. Radiopharmaceuticals labelled with beta-emitting radionuclides for radioimmunotherapy and palliative treatment of skeletal metastases are receiving increasing interest. Numerous agents are now available for imaging inflammation, but more clinical experience is required to determine which of them is the most appropriate. The growing importance of radiolabelled receptor-imaging agents is apparent from the commercial availability of the first such compound in Europe.
在过去四年里，放射性药物化学领域的大部分工作都致力于正电子发射断层扫描用化合物，但该技术的广泛应用仍因成本高昂而受到限制。另一方面，锝-99m标记放射性药物的研发也取得了稳步进展。现在有多种99mTc标记的试剂可用于或正在进行脑灌注研究（99mTc标记的HMPAO、ECD、MRP20）、心肌灌注研究（99mTc标记的MIBI、替硼肟和膦）以及肾功能研究（99mTc-MAG3、99mTc-L,L-EC）的临床评估。已经开发出不同的直接还原法和间接偶联法，能在保留免疫反应性的情况下用99mTc有效地标记抗体或其片段。然而，监管部门对这些制剂的纯化和质量有严格要求，这极大地限制了它们在临床实践中的应用。用于放射免疫治疗和骨骼转移姑息治疗的β发射放射性核素标记的放射性药物正受到越来越多的关注。现在有许多用于炎症成像的试剂，但还需要更多临床经验来确定哪种试剂最合适。从欧洲第一种此类化合物的商业供应情况可以明显看出，放射性标记受体成像剂的重要性日益增加。
