Pathogenic microorganisms and viruses cause outbreaks and pandemics that affect millions of people worldwide. Despite recent advances in pharmacology and medicine, the ability of infectious diseases to spread in the modern era is accelerating due to various factors contributing to increased human-to-human and human-animal contacts. With the global rise of drug resistance among pathogens and frequently occurring viral outbreaks, alternative drugs and therapies that specifically inhibit microbial virulence or regulate immune responses are attracting growing interest. The present review focuses on itaconate and its derivatives as potential anti-pathogenic agents. It summarizes the current state of research on itaconate metabolism in bacteria, fungi and mammals. This is followed by a comprehensive review of recent advances studying itaconate and its derivatives as anti-inflammatory, immunoregulatory, antimicrobial and antiviral compounds, along with their mechanisms of action. Finally, the review emphasises the existing challenges and future research directions for the application of itaconate and its derivatives as anti-pathogenic agents.