Tea is an infusion of the leaves of the Camellia sinensis plant and is the most widely consumed beverage in the world after water. The main chemical components in teas are phenolic compounds (tea polyphenols, mainly tea catechins). A large number of in vitro and in vivo scientific studies have supported that the tea polyphenols can provide a number of health benefits such as, reducing the incidence of coronary heart disease, diabetes and cancer. Recently, tea polyphenols have proven highly attractive as lead compounds for drug discovery programs. A clear understanding of chemistry, stability, pharmacokinetics and metabolic fate of tea will be significant to elucidate many medicinal effects by biochemical theory and pharmaceutical development. This article reviews the current literature on the pharmacoknetics and biotransformation of tea catechins. The half-lives of tea polyphenols are 2-4h and their absorption and elimination are rapid in humans. The peak times (tmax) are 1 and 3 h after oral administration and the peak plasma concentrations are low μM range. It has been reported that catechins are easily metabolized by enzyme and microbe, and the main metabolic pathways are methylation, glucuronidation, sulfation, ring-fission metabolism, and so on. The information is important to discuss some of the challenges and benefits of pursuing this family of compounds for drug discovery.