Adhesion GPCRs are a large class of surface proteins that recognize chemical and mechanical stimuli in the body. The rapidly expanding body of knowledge on the therapeutic targeting of these receptors is raising hopes for clinical application in the near future. Although no medicinal products targeting these receptors have yet been approved, several adhesion GPCR modulators are available and show potential for translation into clinical use. Modulators are crucial for the regulation of metabolic pathways and play a major role in pharmacology by enabling the targeted control of receptor activity.