Lubiprostone is a novel chloride channel 2 activator indicated for the treatment of chronic idiopathic constipation in adults and constipation-predominant irritable bowel syndrome (IBS-C) in adult women. It is effective for chronic constipation at a dose of 24 mcg twice daily and for IBS-C at a dose of 8 mcg twice daily. Lubiprostone is well-tolerated, with nausea and headache being the most commonly reported adverse drug reactions. It also has a low potential for drug-drug interactions. Lubiprostone is a potential treatment for both disorders, which have few treatment options available. Studies of longer duration will help more firmly establish its use for these chronic conditions.