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20(S)-Protopanaxadiol (dammar-24-ene-3β, 12β, 20S-triol) is the aglycone of protopanaxadiol-containing ginsenosides such as ginsenoside Rbl, Rb2, Rd, Rg3 and Rh2.A lot of studies have revealed that it has antitumour activity and is a potential therapeutic agent in the prevention and treatment of cancer.The aim of the lresent study was to investigate the preclinical pharmacokinetics of 20(S)-protopanaxadiol in rats and beagle dogs by LC/MS/MS, to rationally evaluate the efficiency and security of 20(S)-protopanaxadiol, and to offer some inspirations for the clinical studies.