Liver X Receptors (LXRs) are nuclear hormone receptors with a pivotal role in lipid metabolism regulation. LXRs, specifically LXRα and LXR , control cholesterol homeostasis, dyslipidemia, and atherosclerosis, making them attractive therapeutic targets for lipid disorders. Synthetic LXR agonists and Selective LXR Modulators (SLiMs) have been developed, showing promise in preclinical models, although side effects remain a concern. Additionally, LXRs are emerging as therapeutic candidates beyond lipid disorders. They may influence neurodegenerative diseases by modulating inflammation and amyloid-beta metabolism and impact cancer and metabolic disorders through cell proliferation and glucose metabolism regulation. Challenges include mitigating side effects, achieving tissue-specific targeting, and conducting robust clinical trials. In conclusion, LXRs hold vast therapeutic potential in addressing lipid disorders and extending to diverse medical conditions, but ongoing research is crucial for unlocking their full therapeutic benefits.