The distributions of olfactory receptors (ORs) are widely available throughout our body, not compartmentalized in nasal parts, which are known as Ectopic olfactory receptors (EORs). Their functions are diverse but the majority of them are yet to be determined. ORs in non-olfactory tissues transduce their signals via different pathways that vary depending on their placements. As they are G-protein coupled receptors (GPCR), they stimulate Golf protein following the activation with specific ligands. They are involved in several cellular processes like chemotaxis, tissue repairing, hair growth, cell proliferation, energy metabolism, inflammation, apoptosis, etc. All these functions make them prospective therapeutic targets. The transformed expression level of ORs in the healthy and cancerous cells might open a new door to detect and diagnose cancer in the early stages. Ligand-based activation can also block the cancer pathway. This review summarizes the therapeutic potential of the EORs including their manifold functions outlined till date.