2agonister

2agonister, or 2-agonists, is a term used in pharmacology to describe ligands that activate two receptor targets. The phrase is often synonymous with “dual agonist” or “bispecific agonist,” but it is not uniformly standardized across languages or journals. In English-language pharmacology, “dual agonist” is more common, while “2agonister” appears in some Nordic literature and discussions.

Mechanism and scope: A 2agonister binds to two receptor subtypes with meaningful affinity, producing coordinated signaling and potentially a more integrated physiological effect than a single-target drug. The two targets may be within the same receptor family (for example, two GPCR subtypes) or across different families (for example, GLP-1 and GIP receptors). Design challenges include achieving balanced potency at both targets, avoiding excessive activation of one pathway, and matching pharmacokinetic properties.

Examples: Endogenous catecholamines such as adrenaline activate multiple adrenergic receptors and can be described as natural multi-target agonists. Clinically, tirzepatide is a dual agonist of GLP-1 and GIP receptors used for type 2 diabetes and obesity. Other research-oriented examples include GLP-1/glucagon dual agonists (such as cotadutide), explored for metabolic diseases.

Clinical implications and challenges: Dual agonists aim to harness synergistic therapeutic effects and may simplify regimens. However, balancing activities at two receptors, managing safety and tolerability, and achieving appropriate pharmacokinetic profiles remain key considerations for development and regulatory approval.