Staphylococcus aureus is a major human pathogen capable of causing various diseases, from skin infections to life-threatening pneumonia and toxic shock syndrome. S. aureus exoproteins, including superantigens, contribute significantly to the pathogenesis of this organism. Antibiotics inhibit growth, but often provide no protection from S. aureus exoproteins. With the emergence of antibiotic-resistant S. aureus, new therapeutic options to treat or prevent S. aureus-associated diseases are critical. Most S. aureus infections begin on the skin or mucosal surfaces from direct inflammatory or cytotoxic effects of exotoxins. Therefore, antitoxin therapies that prevent toxin production and prevent their effects on host cells are being researched. Current treatments for staphylococcal diseases and recent developments in antitoxin therapeutic agents and vaccines are reviewed.