Worldwide, tea is one of the most widely consumed beverages. Green tea consumption is especially popular in China, Japan and other Asian countries. It has been found to be rich in polyphenolic compounds, of which catechins are the major constituents. A large number of clinical and preclinical studies have explored its pharmacologic activities. It holds promise as an antioxidant, anti-inflammatory, antibacterial, antiarteriosclerotic, cardioprotective, neuroprotective and anticarcinogenic agent, to name a few. This review summarizes the pharmacodynamics and pharmacokinetics of green tea polyphenols and explores their future as novel drugs for both health and disease conditions.