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Rho123 was administered to mice, and the fluorescence level in CD8<jats:sup>+<\/jats:sup> cells was measured. Cepharanthine hydrochloride (CH) and verapamil (VER), two P\u2010gp inhibitors, were administered to mice 1 hour prior to Rho123 administration <jats:italic>in vivo<\/jats:italic> or added to peripheral blood 1 hour prior to Rho123 addition <jats:italic>ex vivo<\/jats:italic>. The tumor inhibition effect of 5\u2010fluorouracil\/adriamycin\/cisplatin (FAP) protocol plus CH was also investigated. A concentration\u2010 or dose\u2010response relationship was shown between the concentration and dose of CH and Rho123 accumulation or the antitumor activity. 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