肿瘤放射示踪剂的开发——与药理学的接口。
Development of radiotracers for oncology--the interface with pharmacology.
机构信息
Comprehensive Cancer Imaging Centre, Imperial College London Hammersmith Campus, Du Cane Road, London, UK.
出版信息
Br J Pharmacol. 2011 Aug;163(8):1565-85. doi: 10.1111/j.1476-5381.2010.01160.x.
Abstract
There is an increasing role for positron emission tomography (PET) in oncology, particularly as a component of early phase clinical trials. As a non-invasive functional imaging modality, PET can be used to assess both pharmacokinetics and pharmacodynamics of novel therapeutics by utilizing radiolabelled compounds. These studies can provide crucial information early in the drug development process that may influence the further development of novel therapeutics. PET imaging probes can also be used as early biomarkers of clinical response and to predict clinical outcome prior to the administration of therapeutic agents. We discuss the role of PET imaging particularly as applied to phase 0 studies and discuss the regulations involved in the development and synthesis of novel radioligands. The review also discusses currently available tracers and their role in the assessment of pharmacokinetics and pharmacodynamics as applied to oncology.
摘要
正电子发射断层扫描（PET）在肿瘤学中的作用日益增大，特别是作为早期临床试验的组成部分。作为一种非侵入性的功能成像方式，PET 可以通过利用放射性标记化合物来评估新型治疗药物的药代动力学和药效动力学。这些研究可以在药物开发过程的早期提供关键信息，这些信息可能会影响新型治疗药物的进一步开发。PET 成像探针也可用作临床反应的早期生物标志物，并在给予治疗剂之前预测临床结果。我们讨论了 PET 成像的作用，特别是将其应用于 0 期研究，以及讨论了新型放射性配体的开发和合成所涉及的规定。该综述还讨论了目前可用的示踪剂及其在评估肿瘤学中应用的药代动力学和药效动力学中的作用。
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