Lupeol (LUP), a naturally occurring pentacyclic triterpene, is found in various fruits, vegetables, and medicinal plants and is evident to possess diverse pharmacological activities. This study aimed to consolidate its findings based on updated database reports. Findings suggest that LUP and some of its derivatives have promising biological roles, including anticancer effects. Notably, LUP induces apoptosis and cell cycle arrest in cancer cells while sparing normal cells, highlighting its selective cytotoxicity. By modifying pathways such as NF-κB and phosphatidyl inositol 3-kinase (PI3K)/Akt, LUP demonstrates anticancer activity, reducing LDL oxidation by 34.4% and causing cancer cells to undergo apoptosis while leaving healthy cells unaffected. Moreover, it has strong antioxidant and anti-inflammatory properties; thus, it may act against conditions like arthritis, asthma, and cardiovascular diseases. It has broad-spectrum antimicrobial activities and can be used as an alternative to conventional antibiotics. LUP and its nanoformulations (PEGylated liposomes) improved biopharmaceutical profiles in test systems. It also showed neuroprotective effects, particularly against Alzheimer's and Parkinson's diseases. Taken together, LUP has multi-target therapeutic approaches against various diseases and pathological conditions, advocating for its inclusion in future clinical trials.