The new age of nutraceuticals is now embracing the centuries old herbal extract of Ginkgo biloba (Mantissa Plantarum Altera, 1771, Ginkgoceae). The standardized preparation of the Ginkgo leaf extract (EGb 761) contained 2 main bioactive constituents, flavonoid glycosides (24%) and terpene lactones (6%), along with less than 5 ppm of the allergenic component, ginkgolic acid. The Ginkgo leaf extract has been reported to have neuroprotective, anticancer, cardioprotective, stress alleviating, and memory enhancing effects and possible effects on tinnitus, geriatric complaints, and psychiatric disorders. The therapeutic mechanisms of action of the Ginkgo leaf extract are suggested to be through its antioxidant, antiplatelet, antihypoxic, antiedemic, hemorrheologic, and microcirculatory actions, where the flavonoid and the terpenoid constituents may act in a complementary manner. Toxicity studies show that the Ginkgo leaf extract is relatively safe for consumption, although a few side effects have been reported, that is, intracerebral hemorrhage, gastrointestinal disturbances, headaches, dizziness, and allergic skin reactions. The use of Ginkgo leaf extract may be promising for treatment of certain conditions, although its long-term use still needs to be evaluated.