Background: There are multiple antidiabetic drugs in China, which vary in efficacy and safety. However, no clinical study exists comparing all the alternative drugs simultaneously. This study aims to estimate and compare the efficacy of alternative classes of antidiabetic drugs in the regimen of monotherapy for Chinese patients with type 2 diabetes (T2DM). Methods: Systematic literature review was conducted by retrieving databases including CNKI, WanFang, CQVIP, PubMed, Embase, Web-of-Science, ScienceDirect and Cochrane Library, to identify randomized controlled trials (1990-2016) comparing the efficacy of 'antidiabetic drug monotherapy' vs 'placebo/lifestyle intervention' in Chinese T2DM patients. Three-lines eight-classes of antidiabetic drugs were included based on Chinese guideline: 1st line drug (metformin), 2nd line drug (I±-glycosidase inhibitor, sulfonylurea, glinide, DPP-4 inhibitor, thiazolidinedione), 3rd line drug (insulin, GLP-1 receptor agonist). Meta-analyses were used to estimate the efficacy of antidiabetic drug vs placebo/lifestyle intervention. Findings: 99,072 records were identified through database search, with 46 studies finally included. Overall, compared with placebo/lifestyle intervention, metformin, 2nd line drug and 3rd line drug reduced HbA1c level by 1·04%, 0·72% and 1·22%, BMI level by 1·77kg/m2, 0·24kg/m2 and 1·14kg/m2, TC level by 0·64mmol/l, 0·10mmol/l and 0·58mmol/l, SBP level by 3·13mmHg, 1·37mmHg and 3·00mmHg; while increased HDL-C level by 0·19mmol/l, 0·09mmol/l and 0·15mmol/l, respectively. In 2nd line drugs, the top three treatments for reducing HbA1c level were sulfonylurea (WMD:-1·19;95%CI:-1·56,-0·82), α-glycosidase inhibitor (WMD:-0·90;95%CI:-1·32,-0·47), thiazolidinedione (WMD:-0·80;95%CI:-1·31,-0·29); for reducing BMI level were α-glycosidase inhibitor (WMD:-0·64;95%CI:-1·46,0·17), DPP-4 inhibitor (WMD:-0·27;95%CI:-1·12,0·57), thiazolidinedione (WMD:0·11;95%CI:-0·96,1·17); for reducing TC level were DPP-4 inhibitor (WMD:-0·18;95%CI:-0·35,-0·01), α±-glycosidase inhibitor (WMD:-0·30;95%CI:-1·28,0·68), thiazolidinedione (WMD:0·00;95%CI:-0·30,0·31); for increasing HDL-C level were thiazolidinedione (WMD:0·19;95%CI:0·12,0·26), sulfonylurea (WMD:0·02;95%CI:-0·18,0·22), DPP-4 inhibitor (WMD:0·01;95%CI:-0·05,0·06); for reducing SBP level were α-glycosidase inhibitor (WMD:-3·20;95%CI:-8·39,1·99), DPP-4 inhibitor (WMD:-1·85;95%CI:-4·17,0·47), thiazolidinedione (WMD:1·60;95%CI:-5·22,8·42). In 3rd line drugs, insulin (WMD:-2·37;95%CI:-3·79,-0·95) was superior to GLP-1 receptor agonist (WMD:-1·18;95%CI:-1·45,-0·91) in reducing HbA1c level, while no data for the comparison on other outcomes. Interpretation: Pharmacological monotherapies have better efficacy than placebo/lifestyle intervention in Chinese T2DM patients. Funding: None. Declaration of Interest: We declare no competing interests.