Ramoplanin is primarily used as an antibacterial agent, especially effective against Gram-positive bacteria, including multidrug-resistant strains such as vancomycin-resistant enterococci (VRE) and methicillin-resistant Staphylococcus aureus (MRSA). It functions by inhibiting bacterial cell wall synthesis, specifically blocking peptidoglycan formation at an early stage, which leads to cell death.

Due to its mechanism of action and limited systemic absorption when administered orally, ramoplanin is being investigated for use in decolonizing patients carrying resistant pathogens in the gastrointestinal tract, helping to prevent the spread of these organisms in hospital settings. It has shown promise in clinical trials for the treatment and prevention of Clostridioides difficile infection (CDI), where it targets the causative bacteria while sparing much of the normal gut flora.

Its poor oral bioavailability limits systemic use but makes it suitable for targeted gastrointestinal applications, reducing the risk of systemic side effects. Research continues into its potential as a prophylactic agent in high-risk populations and as part of infection control strategies in healthcare environments.