Zingiber officinale Rosc. (Zingiberacae), commonly known as ginger, is a perennial and herbaceous plant with long cultivation history. Ginger rhizome is one of the most popular food spices with unique pungent flavor and is prescribed as a well-known traditional Chinese herbal medicine. To date, over 160 constituents, including volatile oil, gingerol analogues, diarylheptanoids, phenylalkanoids, sulfonates, steroids, and monoterpenoid glycosides compounds, have been isolated and identified from ginger. Increasing evidence has revealed that ginger possesses a broad range of biological activities, especially gastrointestinal-protective, anti-cancer, and obesity-preventive effects. In addition, gingerol analogues such as 6-gingerol and 6-shogaol can be rapidly eliminated in the serum and detected as glucuronide and sulfate conjugates. Structural variation would be useful to improve the metabolic characteristics and bioactivities of lead compounds derived from ginger. Furthermore, some clinical trials have indicated that ginger can be consumed for attenuating nausea and vomiting during early pregnancy; however, there is not sufficient data available to rule out its potential toxicity, which should be monitored especially over longer periods. This review provides an up-to-date understanding of the scientific evidence on the development of ginger and its active compounds as health beneficial agents in future clinical trials.