Related Experiment Video
Updated: Aug 6, 2026

Free Radicals in Chemical Biology: from Chemical Behavior to Biomarker Development
Published on: April 15, 2013
Bioactivation and reactivity research advances - 2025 year in review
Joyce Liu1, Upendra A Argikar2, Pietro Brunetti3
1Department of Drug Metabolism and Pharmacokinetics, Genentech, Inc, South San Francisco, CA, USA.
None:
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.
Related Concept Videos
Bioactivation and Tissue Toxicity
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...
Targets for Drug Action: Overview
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Factors Affecting Drug Biotransformation: Biological
Species differences: Variations in enzyme systems across species can cause disparities in drug metabolism. For instance, humans may metabolize certain drugs faster than rodents, altering therapeutic effects.
Strain differences: Genetic variations within a species can result in differing enzyme activity, impacting drug response and toxicity. For example, some mouse strains may...
Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems
Drug Biotransformation: Overview
