Beta-blockers, once considered contraindicated in patients with heart failure, are now the standard of care in such patients. This change is the result of several large-scale clinical trials, including Cardiac Insufficiency Bisoprolol Study II (CIBIS-II), Metoprolol CR/XL Randomized Intervention Trial in Congestive Heart Failure (MERIT-HF), and the Carvedilol Prospective Randomized Cumulative Survival (COPERNICUS) trial, that have demonstrated significant morbidity and mortality benefits of beta-blockers in patients with heart failure caused by left ventricular systolic dysfunction. beta-blockade also improves quality of life and causes regression of cardiac remodeling, a phenomenon characteristic of chronic heart failure. This article provides an overview of the history of beta-blockade in the treatment of heart failure, beginning with the early misconception that beta-blockers are detrimental to patients with heart failure. Mechanistic and early clinical trials are reviewed, along with the results from CIBIS-II, MERIT-HF, and COPERNICUS. Barriers to the use of beta-blocker therapy also are discussed.