Zoliflodacin: Advancing oral therapy for multidrug-resistant gonorrhea – Clinical evidence and future perspective

Abstract The emergence of multidrug-resistant Neisseria gonorrhoeae worldwide has significantly compromised current treatment regimens and raised concerns about the future of gonorrhea treatment. As resistance emerges to several antibiotics, including extended-spectrum cephalosporins, there is a need for a new agent with a novel mechanism of action. Zoliflodacin is a first-in-class oral spiropyrimidinetrione exclusively developed for the treatment of uncomplicated gonorrhea. It exerts bactericidal activity by selectively inhibiting the GyrB subunit of bacterial DNA gyrase, a distinct mechanism of fluoroquinolones, so it reduces the likelihood of cross-resistance. Clinical trials and postmarketing surveillance indicate that a single oral dose of zoliflodacin provides a high rate of microbiological cure of urogenital infections. However, it is less effective at pharyngeal sites due to poor tissue penetration. Zoliflodacin is generally well-tolerated with mild-to-moderate adverse effects. In conclusion, zoliflodacin is a promising new agent for oral treatment of multidrug-resistant N. gonorrhoeae .