Left ventricular (LV) remodeling (ie, enlargement and functional deterioration occurring over time) is among the main mechanisms of progression in heart failure (HF). LV dilatation and dysfunction are major negative prognostic markers in patients with HF. Treatments that are effective in limiting or even reversing this process can be expected to provide clinical benefit. Changes in LV dimensions rather than in ejection fraction should be used to monitor remodeling. Ejection fraction can be influenced by transient loading conditions and by agents that stimulate contractility at the expense of increased oxygen demand, whereas dimensional changes probably reflect structural modifications occurring in the myocardium. The neurohormonal antagonists that have been demonstrated to reduce mortality and morbidity in HF (angiotensin-converting enzyme inhibitors [ACE], beta-blockers, angiotensin receptor blockers, and aldosterone antagonists) are also able to inhibit or reverse remodeling. In reverse remodeling, beta-blockers appear to be superior to the other classes of drugs, with a stronger correlation between dose and effect, but it must be remembered that they have been tested as an addition to background therapy that may include ACE inhibitors. With regard to nonpharmacologic strategies, biventricular pacing is associated with functional improvement and reverse remodeling in patients with advanced HF and electromechanical dyssynchrony, and it recently has been demonstrated to improve survival in a randomized clinical trial.