Aim To investigate the effect of bezafibrate on reversing cholesterol transport from macrophage to feces in vivo, serum lipid profiles of mice were tested after bezafibrate administration. The ³H-cholesterol contents in serum, liver and feces in mice were measured to explore the effect of bezafibrate on reversing cholesterol transport from macrophage to feces in vivo. Methods 28 male C57BL/6 mice were randomly divided into four groups and treated with ordinary diet or plus different dosage （0.1%, 0.25% and 0.5%） of bezafibrate for 4 weeks, then these mice were injected intraperitoneally with ³H-cholesterol-labeled and cholesterol-loaded RAW264.7 macrophages （0.5 mL/mice, the amount of cells achieve 5.0×10⁶）. Serum lipid profiles were determined by enzymatic method. Serum and liver tissues were harvested at 24 h, feces were collected. And all samples were analyzed for the appearance of ³H-tracer （as the percentage of the total injected counts）. Results Bezafibrate （0.1%, 0.25% and 0.5%） dose-dependently and increased the level of high density lipoprotein cholesterol （HDLC） and reduced the level of triglyceride （TG）. After 24 hours of being intrapentoneally injected, the serum ³H-cholesterol levels in the mice treated with different dosage of bezafibrate （0.1%, 0.25% and 0.5%） were significantly higher by 100%, 131% and 110% compared with those in the control （P＜0.05）, the liver ³H-cholesterol levels in the mice treated with different dosage of bezafibrate （0.1%, 0.25% and 0.5%） were significantly higher 86.4%, 52.3%, 51.6% compared with those in the control （P＜0.05）, the feces ³H-cholesterol levels in the mice treated with different dosage of bezafibrate （0.1%, 0.25% and 0.5%） were significantly higher by 110%, 140% and 160% compared with those in the control （P＜0.05）. Conclusions Bezafibrate significantly and dose-dependently reduces the level of TG and increases the level of HDLC, bezafibrate promotes cholesterol reverse transport in vivo, accelerates clearance of cholesterol via feces, so it will be in favor of the prevention of atherosclerosis.