Objective This study assessed the efficacy and safety of platelet GP IIb/IIIa receptor antagonists for treating patients with AIS. Methods A systematic search was conducted across PubMed, Embase, Web of Science, the Cochrane Library, CNKI, VIP and the Wanfang database to evaluate the safety and efficacy of tirofiban compared to conventional antiplatelet agents (aspirin and/or clopidogrel) for treating patients with AIS during the inception to June 2024. Results A total of 1948 patients from 12 publications were included. Compared with conventional antiplatelet agents, tirofiban reduced patients" 24 h to 72 h National Institutes of Health Stroke Scale (NIHSS) scores [ SMD (95% CI )=-1.58 (-2.29, -0.86), P<0.001], 7 d to 14 d NIHSS scores [ SMD (95% CI )=-1.53 (-2.24, - 0.82), P<0.001], and modified Rankin Scale ( mRS) score at 90 d [ WMD (95% CI )=-0.96 (-1.45, -0.47), P<0.001], which increased the proportion of patients with a good prognosis (mRS score of 0 to 2) at 90 d [ RR (95% CI )=1.12 (1.02,1.23) , P<0.001]. Subsequently, we analyzed the subgroups according to the time of bridging conventional antiplatelet drugs, which were divided into 24h, 48h and 72h. The results showed that although bridging conventional antiplatelet drugs after 72h of tirofiban treatment was superior to the control group in neurological outcome, the difference was not statistically significant. There was no statistically significant difference in the incidence of cerebral hemorrhage, incidence of other bleeding, incidence of thrombocytopenia, and mortality between the two groups. Conclusion Compared with conventional antiplatelet agents, tirofiban improved the neurologic prognosis of patients without increasing their incidence of adverse events.