ObjectiveTo systematically review the therapeutic effects and safety of new platelet inhibition regimens targeting P2Y12-receptors (prasugrel/ticagrelor) in patients with acute coronary syndrome (ACS). MethodsSuch databases as PubMed (1980 to 2013.7), EMbase (1980 to 2013.5), The Cochrane Library (Issue 7, 2013), CBM (1990 to 2013.7), CNKI (1994 to 2013.7), VIP (1989 to 2013.7) and WanFang Data (1980 to 2013.7) were electronically searched to collect the randomized controlled trials (RCTs) about comparing prasugrel/ticagrelor with clopidogrel in treating patients with ACS. Two reviewers screened literature according to the inclusion and exclusion criteria, extracted data, and assessed the methodological quality of the included studies. Then meta-analysis was performed using RevMan 5.2 software. ResultsFive studies involving 43 452 patients were finally included. The results of meta-analysis showed that:compared with standard clopidogrel, prasugrel/ticagrelor reduced the incidences of myocardial infarction (OR=0.83, 95%CI 0.77 to 0.89, P < 0.000 01), cardiovascular death (OR=0.86, 95%CI 0.78 to 0.94, P=0.002), and stent thrombosis (OR=0.61, 95%CI 0.38 to 0.97, P=0.04); while no advantage was found in reducing the incidences of stroke (OR=1.06, 95%CI 0.88 to 1.26, P=0.54), intracranial hemorrhage (OR=1.18, 95%CI 0.81 to 1.71, P=0.39), and severe bleeding after thrombolysis due to myocardial infarction (OR=1.17, 95%CI 0.94 to 1.47, P=0.16). ConclusionNew platelet inhibition regimens targeting P2Y12-receptors for ACS could effectively decrease the incidences of myocardial infarction, cardiovascular death, and stent thrombosis events. However, compared with clopidogrel, it could not improve the clinical outcomes of patients with stroke and intracranial hemorrhage. Additionally, due to the increased risk of non-CABG related bleeding, more attention should be paid to the application of new platelet inhibition regimens.