Published on
October 21, 2025
Category
Terry's Corner
Irreversible drugs change the rules of engagement.
Unlike reversible ligands, their impact can persist long after the compound is gone — creating durable pharmacological effects that reshape how pharmacokinetics and pharmacodynamics intersect. In modern discovery programs, that’s a decisive advantage (or a hidden liability) in candidate selection.
In this week’s lesson, you’ll unpack:
Why low offset rates can mimic covalent effects without forming actual bonds.
How target depletion and replenishment kinetics define the therapeutic window.
How persistent binding alters structured tissue penetration — and why that matters for tumor targeting and beyond.
These tactical frameworks are used to optimize molecules, sharpen PK/PD strategy, and mitigate downstream safety surprises before they appear in IND-enabling studies.
Understanding irreversible interactions can mean the difference between a stalled program and a strategic breakthrough. Those who master kinetic pharmacology set the pace.
🟢 Join Terry’s Corner and sharpen your pharmacology toolkit.
✳️ Terry's Corner | Dr. GPCR Ecosystem
#GPCR #DrGPCR #Pharmacology #DrugDiscovery #MedicinalChemistry #PKPD #ReceptorKinetics #DrugDevelopment
