Abstract Objective: To investigate the correlation between serum neopterin, homocysteine (Hcy) and the risk of developing ischemic stroke (IS) in patients with transient ischemic attack (TIA). Methods: Ninety-two TIA patients were prospectively recruited at the First Affiliated Hospital of the Medical College, Shihezi University, Xinjiang Autonomous Region China. Of the included patients, 27 developed ischemic stroke (IS group) and other 65 cases did not (TIA group). Peripheral venous blood was obtained within 24 hours of TIA diagnosis. Serum neopterin, Hcy and serum lipid levels were tested and compared between IS and TIA groups. Results: Serum neopterin (6.38±1.76 ng/mL vs 5.39±1.51 ng/mL), Hcy (17.95±4.10 μmol/L vs 15.30±3.66 μmol/L), TG (1.82±0.92 mmol/L vs 1.40±0.71 mmol/L) and LDL (3.31±0.67 mmol/L vs 2.69±0.62 mmol/L) of IS group were significantly higher than those of TIA group (p<0.05). The AUC of serum neopterin, Hcy, TG and LDL for predicting the risk of developing IS in patients with TIA were 0.68 (95%CI: 0.55-0.81, 0.68 (95%CI: 0.57-0.80), 0.64 (95%CI: 0.51-0.78) and 0.75 (95%CI: 0.63-0.86), respectively. Conclusion: Serum neopterin, Hcy, TG and LDL are promising serological markers for predicting the increased risk of developing IS for patients with TIA.