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使用碳-11标记的工具化合物以支持药物研发。

Use of carbon-11 labelled tool compounds in support of drug development.

作者信息

Boscutti Giulia, Huiban Mickael, Passchier Jan

机构信息

Imanova Ltd., Burlington Danes Building, Imperial College London, Hammersmith Hospital, Du Cane Road, London W12 0NN, UK.

Imanova Ltd., Burlington Danes Building, Imperial College London, Hammersmith Hospital, Du Cane Road, London W12 0NN, UK.

出版信息

Drug Discov Today Technol. 2017 Nov;25:3-10. doi: 10.1016/j.ddtec.2017.11.009. Epub 2017 Dec 1.

DOI:10.1016/j.ddtec.2017.11.009
PMID:29233265
Abstract

The pharmaceutical industry is facing key challenges to improve return on R&D investment. Positron emission tomography (PET), by itself or in combination with complementary technologies such as magnetic resonance imaging (MRI), provides a unique opportunity to confirm a candidate's ability to meet the so-called 'three pillars' of drug development. Positive confirmation provides confidence for go/no-go decision making at an early stage of the development process and enables informed clinical progression. Whereas fluorine-18 has probably gained wider use in the community, there are benefits to using carbon-11 given the greater flexibility the use of this isotope permits in adaptive clinical study design. This review explores the scope of available carbon-11 chemistries and provides clinical examples to highlight its value in PET studies in support of drug development.

摘要

制药行业在提高研发投资回报率上面临着关键挑战。正电子发射断层扫描(PET)本身或与诸如磁共振成像(MRI)等互补技术相结合,为确认候选药物满足药物开发所谓“三大支柱”的能力提供了独特机会。得到肯定的确认可为开发过程早期的继续/终止决策提供信心,并有助于做出明智的临床推进决策。虽然氟-18可能在业界得到了更广泛的应用,但使用碳-11也有好处,因为这种同位素在适应性临床研究设计中的使用具有更大的灵活性。本综述探讨了可用的碳-11化学方法的范围,并提供临床实例以突出其在支持药物开发的PET研究中的价值。

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