Bioactivation and reactivity research advances - 2021 year in review

Area of Science:

• Pharmacology and Toxicology
• Medicinal Chemistry

Background:

• Annual review on biotransformation and bioactivation expanded to a dedicated edition on bioactivation and reactivity.
• Increased contributions from academic and industry experts in the field.

Purpose of the Study:

• Highlight influential articles on covalent inhibitors, reactive metabolite formation, enzyme inactivation, and drug safety.
• Provide a focused review on bioactivation and reactivity for researchers.
• Advance understanding of drug safety through mechanistic insights.

Main Methods:

• Literature review of selected influential articles.
• Categorization of reviewed articles into two main sections: reactivity/enzyme inactivation and bioactivation mechanisms/safety.
• Synthesis of findings from expert contributions.

Main Results:

• Identification of significant developments in covalent inhibitor design.
• Elucidation of mechanisms underlying reactive metabolite formation.
• Analysis of enzyme inactivation pathways and their implications for drug safety.
• Compilation of critical information into structured sections for clarity.

Conclusions:

• The dedicated review provides a comprehensive overview of bioactivation and reactivity.
• Understanding these mechanisms is crucial for developing safer and more effective drugs.
• Continued collaboration between academia and industry is vital for advancing the field.