The impact of radiochemistry in drug projects: The use of C‐14 labeled in the AZD8529, AZD7325 and AZD6280 projects,Journal of Labelled Compounds and Radiopharmaceuticals

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The impact of radiochemistry in drug projects: The use of C‐14 labeled in the AZD8529, AZD7325 and AZD6280 projects
Journal of Labelled Compounds and Radiopharmaceuticals ( IF 0.9 ) Pub Date : 2021-01-07 , DOI: 10.1002/jlcr.3902
Lee Kingston ₁ , Chungang Gu ₂ , Jian Guo ₂ , Steve Swallow ₃ , Charles S Elmore ₁

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Understanding the metabolic transformations of a potential drug molecule is important to understanding the safety profile of a drug candidate. Liquid chromatography-mass spectrometry is a standard method for detecting metabolites in the drug discovery stage, but this can lead to an incomplete understanding of the molecule's metabolism. In this manuscript, we highlight the role radiolabeling played in determining the metabolism and in quantifying the metabolites of AZD8529, AZD7325, and AZD6280. A quantitative whole body autoradiography study can detect covalent adducts in vivo as was the case with AZD5248 in which the compound bound to the aorta. Ultimately another compound free of aortic binding was developed, AZD7986.

中文翻译：

放射化学在药物项目中的影响：在 AZD8529、AZD7325 和 AZD6280 项目中使用标记的 C-14

了解潜在药物分子的代谢转化对于了解候选药物的安全性非常重要。液相色谱-质谱法是在药物发现阶段检测代谢物的标准方法，但这可能导致对分子代谢的不完全了解。在这份手稿中，我们强调了放射性标记在确定代谢和量化 AZD8529、AZD7325 和 AZD6280 代谢物方面的作用。定量全身放射自显影研究可以检测体内共价加合物，就像 AZD5248 的情况一样，其中化合物与主动脉结合。最终开发了另一种无主动脉结合的化合物 AZD7986。

更新日期：2021-01-07

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