The evasive nature of drug efficacy: implications for drug discovery

摘要: The efficacy of a drug is generally determined by the drug's ability to promote quantifiable biological response. In context classical receptor-occupancy theory, considered an intrinsic property ligand/receptor pair, and it often assumed be same for all responses evoked this pair. recognition that single receptor can engage different signalling pathways various drugs binding might differentially influence each these led reassessment concept. Of particular notice fact ligands behave as agonists toward given pathway act, through receptor, antagonists or even inverse on in cell. These observations, variously referred 'ligand-directed trafficking signalling' (LDTRS), 'functional selectivity', 'biased agonism', 'ligand-biased efficacy', 'collateral efficacy' 'pluridimensional have important implications molecular definition process discovery.