Tocilizumab: A Review in Rheumatoid Arthritis

Drugs. 2017 Nov;77(17):1865-1879. doi: 10.1007/s40265-017-0829-7.


Intravenous (IV) and subcutaneous (SC) tocilizumab (RoActemra®), an IL-6 receptor antagonist, are approved (± methotrexate) in numerous countries throughout the world, for the treatment of adults with moderate to severe active rheumatoid arthritis (RA). Extensive clinical experience has firmly established the short- and long-term efficacy and safety of tocilizumab [monotherapy or in combination with conventional synthetic DMARDs (csDMARDs)] in adults with early-stage and longer-duration established RA. In the clinical trial and real-world settings, tocilizumab monotherapy or combination therapy provided rapid and sustained improvements in clinical and radiographic outcomes and health-related quality of life. The safety profile of tocilizumab is consistent over time and, in general, is consistent with that of other immunomodulatory agents. This narrative review, written from an EU perspective, summarizes the clinical use of IV and SC tocilizumab in RA. Given its low risk of immunogenicity, the flexibility of IV and SC administration and the convenience of the once-weekly, self-administered, SC regimen, tocilizumab provides an effective treatment for severe, active and progressive RA in adults not previously treated with methotrexate and an effective biologic first- or subsequent-line treatment for moderate to severe active RA in adults who have either responded inadequately to or were intolerant of previous therapy with ≥ 1 csDMARD or TNF inhibitor.

Publication types

  • Review

MeSH terms

  • Antibodies, Monoclonal, Humanized / pharmacology
  • Antibodies, Monoclonal, Humanized / therapeutic use*
  • Antirheumatic Agents / pharmacology
  • Antirheumatic Agents / therapeutic use*
  • Arthritis, Rheumatoid / drug therapy*
  • Arthritis, Rheumatoid / physiopathology
  • Humans
  • Methotrexate / pharmacology
  • Methotrexate / therapeutic use
  • Receptors, Interleukin-6 / antagonists & inhibitors*
  • Receptors, Interleukin-6 / metabolism


  • Antibodies, Monoclonal, Humanized
  • Antirheumatic Agents
  • Receptors, Interleukin-6
  • tocilizumab
  • Methotrexate