Modifying the chemical characteristics of a molecule to maximize its antimicrobial activity and improve its pharmacological properties.

Lead optimization builds on hit expansion, focusing on lead compounds with the most promising properties. Modifications focus on key areas such as improving the binding of the lead compound to the antibacterial protein target, optimizing the toxicology profile, and ensuring suitable availability within target tissues in the body.

Lead optimization generates one or more candidates for clinical evaluation.


Video definition by Alan Hennessey, GARDP (Switzerland).