Troleandomycin is primarily used as an antibiotic, particularly effective against Gram-positive bacteria. It has been used in the treatment of respiratory tract infections, skin infections, and other bacterial infections sensitive to macrolide antibiotics. Due to its ability to inhibit certain liver enzymes, especially cytochrome P450, it has also been used in research settings to study drug metabolism and drug-drug interactions. This enzyme inhibition can affect the breakdown of other drugs, making it useful for probing metabolic pathways, though this property also limits its clinical use due to potential interactions. Its application in human medicine has declined over time due to the availability of newer macrolides with better safety profiles.