Percutaneous coronary intervention has been hampered by restenosis since its inception. Many research projects including the use of various devices and systemic drug administration have shown disappointing results. The clinical data reported from trials with sirolimus- and paclitaxel- eluting stents have been very promising, such that stents with the capability of drug elution are currently attracting the medical community for the prevention of restenosis. Based on the mechanism of action of the drugs released from the stent and the target of the restenotic process, there may be 4 therapeutic objectives: anti-inflammatory, anti-proliferative, anti-migratory, and pro-endothelial healing. There are many candidate agents for drug-eluting stents, however, it now becomes clear that not all drug-eluting stents are equally effective. This article describe candidate agents which have been tested or currently under investigation, and summarize the latest information.