Resveratrol (3,5,4'-trihydroxy-trans-stilbene) is a phenol phytoalexin derived from grapes, berries, and other plants possessing a spectrum of pharmacologic properties. Resveratrol has been shown to modulate LDL levels, a major risk factor for cardiovascular disease; to interfere with or inhibit oncogenesis and tumor proliferation in in vivo animal cancer models and in human tumor cells in vitro; to significantly extend the lifespan of the yeast Saccharomyces cerevisiae, Caenorhabditis elegans, and the fruit fly Drosophila melanogaster; and to produce wide-ranging benefits in animal models of obesity and diabetes. Resveratrol has gained mainstream attention as “the red wine pill,” with widespread claims made of human health benefits that have outpaced the existing evidence. Over the past few years, many clinical trials have been conducted to evaluate the health effects of resveratrol in humans, in the treatment of cancer, cardiovascular disease, obesity, diabetes, osteopenia and osteoporosis, and other diseases. Considerable work is also underway exploring the optimization of resveratrol delivery and bioavailability in nutraceutical and pharmaceutical paradigms.