Archives of Pharmacal Research

, Volume 38, Issue 5, pp 575–584 | Cite as

IL-6 inhibitors for treatment of rheumatoid arthritis: past, present, and future

  • Go Woon Kim
  • Na Ra Lee
  • Ryo Han Pi
  • Yee Seul Lim
  • Yu Mi Lee
  • Jong Min Lee
  • Hye Seung Jeong
  • Sung Hyun Chung


Rheumatoid arthritis (RA) is a chronic inflammatory disease characterized by polyarthritis. Numerous agents with varying mechanisms are used in the treatment of RA, including non-steroidal anti-inflammatory drugs, disease-modifying anti-rheumatic drugs, and some biological agents. Studies to uncover the cause of RA have recently ended up scrutinizing the importance of pro-inflammatory cytokine such as tumor necrosis factor α (TNF-α) and interleukin (IL)-6 in the pathogenesis of RA. TNF-α inhibitors are increasingly used to treat RA patients who are non-responsive to conventional anti-arthritis drugs. Despite its effectiveness in a large patient population, up to two thirds of RA patients are found to be partially responsive to anti-TNF therapy. Therefore, agents targeting IL-6 such as tocilizumab (TCZ) attracted significant attention as a promising agent in RA treatment. In this article, we review the mechanism of anti-IL-6 in the treatment of RA, provide the key efficacy and safety data from clinical trials of approved anti-IL-6, TCZ, as well as six candidate IL-6 blockers including sarilumab, ALX-0061, sirukumab, MEDI5117, clazakizumab, and olokizumab, and their future perspectives in the treatment of RA.


Rheumatoid arthritis Interleukin-6 (IL-6) Disease-modifying anti-rheumatic drugs (DMARDs) Tumor necrosis factor α (TNF-α) Tocilizumab (TCZ) 



This study was supported by Technology Development Program of the Ministry for Food, Agriculture, Forest, and Fisheries of Republic of Korea (project number 114010031HD030).


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Copyright information

© The Pharmaceutical Society of Korea 2015

Authors and Affiliations

  • Go Woon Kim
    • 1
  • Na Ra Lee
    • 1
  • Ryo Han Pi
    • 1
  • Yee Seul Lim
    • 1
  • Yu Mi Lee
    • 1
  • Jong Min Lee
    • 1
  • Hye Seung Jeong
    • 1
  • Sung Hyun Chung
    • 1
  1. 1.Department of Pharmacology and Clinical Pharmacy, College of PharmacyKyung Hee UniversitySeoulRepublic of Korea

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