摘要
在抗癌药的开发过程中，先导化合物的优化是一个反复的过程。在这过程中，小分子抑制剂或因其绑定特定目标的能力而被选中的生物化合物被合成、测试和优化。我们可以使用以监视放射性同位素标记的化合物的分布和药动为目的的核医学技术的分子成像，以此大大加速上述过程。正电子发射体层摄影（PET）和单光子发射计算机体层摄影（SPECT）可用于量化四维（空间和时间）临床信息，证明肿瘤的出现和监视先导化合物的治疗反应。这篇综述讨论了与活组织检查样品的组织学分析相比，核医学成像的临床前和临床价值。我们还讨论了核医学成像关于治疗反应评估，放射性示踪剂生物分布、肿瘤积累、毒性和药动参数的作用，其中提到微剂量给药研究，预定位策略和药动建模。
关键词: 生物分布，癌症，药物释放，动力学成像，微剂量给药，PET，预定位，SPECT。
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