Background and Objective Diabetes mellitus has become a major public health problem in China. This open-label, prospective, multicentre, post-marketing surveillance study was conducted to investigate the efficacy and safety of nateglinide in combination with metformin in Chinese patients with type 2 diabetes (T2DM). Patients and Methods A total of 892 patients with T2DM were included in the study, of whom 361 subjects had been pretreated with metformin and 531 subjects had not previously been treated with any oral antihyperglycaemic agent. All enrolled patients received 120 mg of nateglinide three times daily within 15 minutes before meals together with metformin (with no restrictions on dosage or frequency of administration) for 12 weeks. Physical examination, laboratory tests and relevant tests in terms of efficacy were performed, and adverse events and subject compliance were documented and monitored. Results From baseline to week 12, glycosylated haemoglobin (HbA(1c)) was reduced by 1.52 % +/- 1.25 % (mean +/- SD), fasting plasma glucose (FPG) by 1.92 +/- 1.78 mmol/L, and 2-h post-prandial plasma glucose (2-h PPG) by 4.55 +/- 2.93 mmol/L (all p < 0.01); 61.66 % of subjects achieved the HbA1c goals of <7 %. A total adverse events incidence of 2.47 % was observed, including an incidence of 1.68 % treatment-emergent adverse events. The incidence of hypoglycaemia was 1.57 %. Other nateglinide-related adverse events (including gastrointestinal disorders, rash and allergic dermatitis) were also reported. There were no serious adverse effects. Conclusion The combination of nateglinide and metformin is a safe and effective means of achieving glycaemic target in Chinese patients with T2DM.