The acute lung injury (ALI)/acute respiratory distress syndrome (ARDS) is a clinical syndrome that affects both medical and surgical patients. To date, despite improved understanding of the pathogenesis of ALI/ARDS, pharmacological modalities have been unsuccessful in decreasing mortality. However, several pharmacological agents for ARDS are in development and have shown great promise. In addition to the anti-inflammatory category including late corticosteroids, inhaled nitric oxide, alveolar surfactant, and vasodilators are being evaluated. Replacements of anticoagulation mediators have also suggested beneficial effects on the patient outcome. This article provides an overview of pharmacological treatments of ALI/ARDS.