OBJECTIVE： To investigate the effects of tacrolimus combined with valsartan in immunosuppressive regimen on renal function， lipid metabolism and matrix metalloproteinase 2 （MMP-2）， MMP-9， tissue inhibitors of matrix metalloproteinases 2 （TIMP-2） and transforming growth factor-β （TGF-β） in patients with chronic allograft dysfunction （CAD）. METHODS： CAD patients admitted to nephrology department of our hospital from Mar. 2016 to Jun. 2018 were enrolled in group A， B， and C according to the random number table， 34 cases in each group. Group A was given cyclosporin A+Mycophenolate capsules+Prednisone acetate tablets； group B was treated with tacrolimus+Mycophenolate capsules+Prednisone acetate tablets； group C was treated with valsartan on the basis of group B； they were treated for continuous 3 months. Renal function indexes （24 h urinary protein， Scr）， lipid metabolism indicators （TC， TG， HDL， LDL） and the levels of MMP-2， MMP-9， TIMP-2 and TGF-β were compared among those groups. RESULTS： Before treatment， there was no statistical significance in above indexes among 3 groups （P＞0.05）. After treatment， 24 h urinary protein， Scr and TC levels of group A were still higher than normal level， while other lipid metabolism indexes were within normal range. 24 h urinary protein and TC level of group B were still higher than normal level， while Scr level was near the upper limit of the normal range， and other lipid metabolism indicators were within the normal range. Renal function indexes and lipid metabolism indexes of group C were within normal range， while renal function indexes levels of it were lower than those of group B （P＜0.05）； there was no statistical significance in lipid metabolism indexes， compared with group B （P＞0.05）. Compared with before treatment， TGF-β level of group A was significantly increased （P＜0.05）； there was no statistical significance in MMP-2， MMP-9 or TIMP-2 levels （P＞0.05）. TGF-β level of group B and group C was increased significantly （P＜0.05）， while the levels of MMP-2， MMP-9 and TIMP-2 were decreased significantly （P＜0.05）. CONCLUSIONS： Tacrolimus combined with valsartan can effectively delay renal dysfunction and improve lipid metabolism in CAD patients. The mechanism may be related to the inhibition of TIMP-2， MMP-2， MMP-9 and TGF-β expression.