Pharmacological onomastics: what's in a name?

Area of Science:

• Pharmacology
• Drug Discovery
• Molecular Biology

Background:

• Traditional drug classification relies on primary receptor targets and actions (agonism/antagonism).
• Emerging evidence reveals drugs activating a single receptor can have multiple, often subtle, efficacies.
• This complexity challenges current drug naming conventions and classification systems.

Purpose of the Study:

• To address the challenges in drug classification and nomenclature arising from drugs with multiple or collateral efficacies.
• To explore the need for revised drug labeling strategies that account for nuanced pharmacological actions.

Main Methods:

• Review of current understanding of drug-receptor interactions and cellular responses.
• Analysis of newly identified drug efficacies, including pathway selectivity and receptor internalization.
• Consideration of allosteric modulator complexities based on co-binding ligands.

Main Results:

• Some agonists selectively activate specific cellular pathways or exhibit cell-type-specific phenotypic behavior.
• Certain antagonists can actively induce receptor internalization without causing receptor activation.
• Allosteric modulator effects are influenced by the identity of co-binding ligands, complicating classification.

Conclusions:

• Accurate classification and naming of novel selective drugs may require detailing specific receptor partners (e.g., G-protein type, beta-arrestin) or pathways.
• For allosteric modulators, identification of co-binding ligands is crucial for precise labeling.
• Linking distinct phenotypic behaviors to specific molecular properties offers opportunities to better correlate clinical effects with pharmacological actions.