Annual review highlights mechanistic advances in drug bioactivation and covalent binding in preclinical discovery, indicating expanding strategies to mitigate drug-induced toxicity.
This year marks the fifth installment of the annual review on bioactivation and reactivity. This series evolved from the broader biotransformation and bioactivation review that started a decade ago, reflecting the increasing importance and interest in this area for drug discovery and development. This year's review features 19 articles that reflect the latest findings and advances in bioactivation and reactivity research. This collection of articles is organized into four general themes: (1) mechanistic insights into CYP-mediated bioactivation, enzyme inhibition, and covalent binding, (2) non-CYP-mediated bioactivation, (3) biological drivers of drug-induced toxicity, and (4) advancements in reactive metabolite trapping.
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Liu et al. (2026) studied this question.
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