Receptor Occupancy Theory

Receptor occupancy theory quantitates pharmaceutical effect dependencies on target receptor binding extent. Maximal effect achievement requires <100% receptor occupancy due to receptor reserve. Spare receptors enable efficacy despite partial occupancy. Competitive antagonism increases ligand concentration required for occupancy. Dose-response curves reflect occupancy relationships.

Regulatory submissions employ occupancy theory supporting dose selection. Clinical efficacy correlates with predicted occupancy. Biomarker assessment measures receptor occupancy directly. Emerging imaging visualises receptor occupancy. Post-approval monitoring confirms occupancy predictions.