Restenosis limits the success of percutaneous transluminal coronary interventions. Coronary artery stenting decreases restenosis, improves outcomes, and is currently the most commonly used percutaneous coronary intervention in the United States. However, in-stent restenosis continues to occur at an unacceptable rate. In-stent restenosis is a neointimal hyperplastic response resulting primarily from vascular smooth muscle cell proliferation. Treatment with anti-proliferative agents presents a logical approach to eradicating restenosis, however, these drugs are highly toxic. Coating stents with anti-proliferative agents allows local delivery of high doses and avoids systemic side effects. In 2001, the results of two clinical trials, RAVEL and ELUTES, using sirolimus- and paclitaxil-coated stents demonstrated nearly complete elimination of in-stent restenosis. These dramatic results represent a tremendous advance in the treatment of coronary heart disease.