Biotransformation has a huge impact on the efficacy and safety of drugs. Ultimately the effects of metabolism can be the lynchpin in the discovery and development cycle of a new drug. This article discusses the impact and application of biotransformation of drugs by mammalian systems, microorganisms, and recombinant enzymes, covering active and reactive metabolites, the impact of the gut microbiome on metabolism, and how insights gained from biotransformation studies can influence drug design from the combined perspectives of a CRO specializing in a range of biotransformation techniques and pharma biotransformation scientists. We include a commentary on how biology-driven approaches can complement medicinal chemistry strategies in drug optimization and the in vitro and surrogate systems available to explore and exploit biotransformation.

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生物转化：代谢在药物发现中的影响和应用

生物转化对药物的有效性和安全性有着巨大的影响。最终，代谢的影响可能是新药发现和开发周期的关键。本文讨论了哺乳动物系统、微生物和重组酶对药物生物转化的影响和应用，涵盖活性和反应性代谢物、肠道微生物组对代谢的影响，以及从生物转化研究中获得的见解如何影响药物设计。专业从事一系列生物转化技术的 CRO 和制药生物转化科学家的观点。我们包括关于生物学驱动的方法如何补充药物优化和体外药物化学策略的评论 和替代系统可用于探索和利用生物转化。