receptortargeted

Receptortargeted is a term used to describe strategies that direct diagnostic or therapeutic agents to specific cellular receptors with the goal of increasing selectivity and efficacy. In this approach, ligands such as antibodies, antibody-drug conjugates, small molecules, peptides, or aptamers bind to target receptors on the surface or inside cells, facilitating selective binding and sometimes uptake or modulating signaling.

Receptor targeting is used in diagnostics, therapeutics, and imaging. Delivery systems place receptor ligands on nanoparticles or drug conjugates so that they accumulate in tissues that overexpress the target receptor, often via receptor-mediated endocytosis. Examples include cancer therapies that target HER2, EGFR, or other overexpressed receptors, as well as imaging agents that bind somatostatin receptors or other tumor-associated receptors.

Advantages include improved tumor selectivity, reduced off-target toxicity, and the ability to modulate receptor-mediated pathways. Challenges include heterogeneity of receptor expression within and between patients, receptor downregulation or mutation leading to resistance, off-target interactions, and complexities of manufacturing and regulatory approval. Additionally, the pharmacokinetics of receptor-targeted agents can be influenced by receptor density, internalization rate, and recycling dynamics.

Receptor targeting is a component of precision medicine, complementing genomic and molecular profiling to tailor therapy or diagnostics to the receptor landscape of a disease. See also receptor-mediated endocytosis, targeted therapy, and molecular imaging.