Rheumatoid arthritis (RA) is characterized by chronic synovial inflammation due 
to unknown causes. Conventional synthetic disease-modifying antirheumatic drugs 
(csDMARDs), biological DMARDs (bDMARDs), and tofacitinib, a targeted sDMARD, can 
be used to treat RA. In clinical trials, molecular-targeted therapies showed a 
significant reduction in RA symptoms and provided pain relief for patients with 
active RA. Even if patients did not show clinical improvement with combination 
therapy with a bDMARD and methotrexate (MTX), some patients showed a significant 
inhibition in structural damage. The clinical efficacies of tofacitinib were 
shown to be equivalent to adalimumab, a bDMARD, in patients with RA treated with 
MTX. MTX is the first-line agent for the treatment of RA. Higher doses of MTX 
might be needed to maintain the effects of bDMARDs. Patients receiving some 
bDMARDs have been shown to have a higher risk for serious infections; thus, 
pre-screening for infections is important before beginning treatment with 
bDMARDs. The rates of patients maintaining targeted levels of disease activity 
after stopping bDMARDs are relatively low. It is uncertain whether remission or 
low disease activity can be maintained after stopping molecular-targeted 
therapies. The development of bDMARDs and targeted-molecular sDMARDs has 
provided a wide range of treatment options for RA. Patients with active RA 
should be treated with a treat-to-target strategy after assessment of risks and 
benefits.