The review systematizes and analyzes the literature data about the pharmacodynamic effects alongside the established antibacterial properties of the antibiotic substance — fusidic acid from the fusidane class. According to several sources, the substance is characterized with its anti-inflammatory, immunosuppressive, anticancer, and antiviral activities. It has been proven that fusidic acid can inhibit lymphocyte activation and the production of pro-inflammatory cytokines in lymphocytes, mononuclear cells, and leukocyte chemotaxis. It inhibits the activation and proliferation of T-lymphocytes in response to phytohemagglutinin and the development of septic shock in response to S. aureus enterotoxin and LPS. The cytoprotective action of fusidic acid on pancreatic islet cells is demonstrated in a model of insulin and glial cells exposed to a cytotoxic substance. When applied externally, its anti-inflammatory effect is comparable to that of low- and moderately-active glucocorticosteroids. The efficacy of fusidic acid in reducing inflammation-induced edema of epidermal proliferation and decreasing the synthesis of critical pro-inflammatory cytokines is comparable to that of dexamethasone at equivalent concentrations. The immunomodulatory and anti-inflammatory properties of this antibiotic substance are clinically significant, enhancing its antibacterial effect, facilitating quicker relief of inflammation, resolution of inflammatory infiltrates, improvement of patient’s quality of life by expediting the removal of unpleasant sensations associated with inflammation and mitigating the repercussions of the inflammatory process.