Restenosis drug discovery--a formidable task.

Restenosis is a complicated disease. Neointima formation and unfavorable remodeling seem to contribute to the development of restenosis after angioplasty. Remodeling, a relatively new hypothesis, might be more crucial than neointima formation, although the two could well be inter-related. Stenting prevents unfavorable remodeling to some extent and lowers restenosis rates as compared to conventional balloon angioplasty. However, restenosis still occurs at too high a rate with stent angioplasty. A great many drugs have been tested in humans for the prevention of restenosis and failed, as most addressed the neointima formation problem only. Future drug design for restenosis should address both remodeling and neointima formation and some antioxidants, such as probucol, have shown promising results in this respect.