OBJECTIVE： To systematically review the effectiveness and safety of methotrexate （MTX） in the treatment of rheumatoid arthritis， and provide evidence-based reference for clinical treatment. METHODS： Retrieved from Medline， EMBase， Cochrane Library， PubMed， CJFD， CBM， VIP and Wanfang Database， randomized controlled trials （RCT） about MTX in the treatment of rheumatoid arthritis were collected， Meta-analysis was performed after data extraction and quality evaluation. RESULTS & CONCLUSIONS： 33 effectiveness evaluation were included， involving 8 253 patients， and 53 safety evaluation were included， involving 4 803 patients. Results of analysis show， the efficacy of MTX was not higher than leflunomide in the treatment of rheumatoid arthritis， superior to cyclosporine A， and similar to sulfasalazine. In addition， MTX shows similar efficacy with etanercept（7.5-20 mg per week）， golimumab， adalimumab or rituximab， but less effective than trastuzumab. The incidence of adverse reactions of MTX is high， but mainly mild or moderate， and the most common adverse reactions are gastrointestinal symptoms. Oral administration of MTX is more secure than intramuscular injection and subcutaneous injection.