Background and objectives: Sarpogrelate has been shown to reduce albuminuria in diabetic nephropathy. For examination of whether this is based on the same mechanisms as angiotensin II receptor blockers or thiazolidinedione, effects of sarpogrelate on atherosclerotic inflammatory molecules and their relations to albuminuria in patients who had diabetes and had already been treated with angiotensin II receptor blockers and with or without thiazolidinedione were examined.Design, setting, participants, & measurements: Forty patients who had diabetes with nephropathy and arteriosclerosis obliterans and had already been treated with angiotensin II receptor blocker (n ؍ 40) were randomly assigned to sarpogrelate (300 mg/d; n ؍ 20) or aspirin group (100 mg/d; n ؍ 20). Plasma monocyte chemoattractant protein-1 and urinary albumin-tocreatinine ratio and monocyte chemoattractant protein-1 were measured at baseline and 16 wk after administration.Results: Only the sarpogrelate group showed increases in plasma adiponectin and decreases in both plasma and urinary monocyte chemoattractant protein-1 and albumin-to-creatinine ratio levels. Moreover, percentage change of monocyte chemoattractant protein-1 level correlated positively to that of albumin-to-creatinine ratio. Even when the sarpogrelate group was further divided into two groups with (n ؍ 9) or without thiazolidinedione (n ؍ 11), changes in monocyte chemoattractant protein-1 or albumin-to-creatinine ratio did not differ.Conclusions: Sarpogrelate can reduce albuminuria and plasma and urinary monocyte chemoattractant protein-1 levels while increasing plasma adiponectin in diabetic nephropathy. These effects seem to be mediated via mechanisms that are different from those of angiotensin II receptor blocker or thiazolidinedione.