Left ventricular remodeling refers to a series of structural, cellular, molecular, metabolic, and functional changes that occur when the myocardium is subjected to abnormal mechanical and neurohormonal stresses. In chronic heart failure with reduced ejection fraction, remodeling is characterized at the whole heart level by left ventricular dilation and transition of chamber shape from elliptical to spherical. These morphological changes are associated with distortion of the natural ventricular architecture and shifting of key structures; notably, the papillary muscles and mitral valve apparatus, into abnormal positions. Thus, remodeling is not only a consequence of the initial hemodynamic and metabolic insults that lead to heart failure but also serves to propagate the very same process, contributing to the progressive loss of ventricular function over time. Accordingly, restoring the normal ventricular size and halting or reversing the remodeling process has been an important target for many different heart failure therapies. This review discusses these different treatment options and highlights the need to combine treatments directed at the structural and hemodynamic abnormalities associated with heart failure in order to effectively reverse remodel the left ventricle.