ObjectiveTo systematically review the effectiveness and safety of argatroban for patients with acute ischemic stroke. MethodsPubMed (1966 to 2013.12), EMbase (1966 to 2013.12), CENTRAL (2013.12), CBM (1978 to 2013.12), VIP (1989 to 2013.12), CNKI (1980 to 2013.12) and CDFD (for masters and Phds, 1999 to 2013.12) were electronically searched for randomized controlled trials (RCTs) on argatroban for patients with acute ischemic stroke. Meanwhile, relevant data were retrieved by hand search and the data from pharmaceutical factories (TIPR Pharmaceutical Responsible Co. Ltd) were collected. Two reviewers independently screened literature, extracted data, and assessed the methodological quality of the included studies. Then, meta-analysis was performed using RevMan 5.2 software. ResultsA total of 11 RCTs involving 889 patients were finally included. The results of meta-analysis showed that the argatroban group was better than the control group in improving patients' neurologic impairment scores (SMD=0.71, 95%CI 0.56 to 0.88, P < 0.000 01), and the effectiveness of neurological function (total result:OR=2.65, 95%CI 1.84 to 3.80, P < 0.000 01; placebo-controlled trial:OR=2.18, 95%CI 1.27 to 3.72, P=0.004; non-placebo-controlled trial:OR=3.09, 95%CI 1.89 to 5.06, P < 0.000 01), all with significant differences. No significant difference was found between the argatroban group and the control group in the long/short-term motilities or dependence rates as well as in the incidence of adverse reaction (OR=1.55, 95%CI 0.60 to 4.01, P=0.37). ConclusionCurrent evidence shows that argatroban could improve neurologic impairment of patients with acute ischemic stroke without severe bleeding events or other adverse reaction. However, further studies are needed to confirm its effects on reducing rates of death and disability in treating acute ischemic stroke.