Purpose of Review <p>Guggulsterone (GS), a bioactive sterol derived from the Commiphora species, has acquired significant attention in pharmacological research due to its diverse therapeutic properties. Traditionally used in Ayurvedic medicine, GS exhibits potent anti-inflammatory, antioxidant, and lipid-lowering effects.</p> Recent Findings <p>Recent studies have elucidated its mechanisms of action, including modulation of nuclear receptors such as farnesoid X receptor (FXR), peroxisome proliferator-activated receptor-γ (PPARγ) and liver X receptor (LXR), leading to improved metabolic profiles and potential benefits in conditions like hyperlipidemia and obesity. Additionally, GS demonstrates promising anticancer activity through the induction of apoptosis and inhibition of tumor growth in various cancer models. Its neuroprotective effects have also been explored, showing potential in the management of diverse neurodegenerative diseases.</p> Summary <p> This review aims to consolidate current findings on the pharmacological activities of GS, highlighting its therapeutic potential and underlying mechanisms while addressing the need for further clinical research to validate its efficacy and safety in human populations.</p> Graphical Abstract <p></p>