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Table 1 Biologic DMARDs for the treatment of RAa

From: Evaluating the efficacy of sequential biologic therapies for rheumatoid arthritis patients with an inadequate response to tumor necrosis factor-α inhibitors

Generic drug name (brand name, year of FDA approval)

Structure and mechanism of action

Mode and frequency of administration

TNF-α inhibitors

  

   Infliximab (Remicade, 1999)

Chimeric monoclonal antibody that binds to TNF-α and blocks its interaction with cell surface receptors

Intravenous infusion every 8 weeks

   Etanercept (Enbrel, 1998)

Soluble human fusion recombinant protein that binds to TNF-α and blocks its interaction with cell surface receptors

Subcutaneous injection weekly or twice weekly

   Adalimumab (Humira, 2002)

Recombinant human monoclonal antibody that binds to TNF-α and blocks its interaction with cell surface receptors

Subcutaneous injection every 2 weeks (or weekly if methotrexate is not taken concurrently)

   Golimumab (Simponi, 2009)

Human monoclonal antibody that binds to TNF-α and blocks its interaction with cell surface receptors

Subcutaneous injection monthly

   Certolizumab pegol (Cimzia, 2009)

Recombinant, humanized, pegylated Fab' of a monoclonal antibody that binds to TNF-α and blocks its interaction with cell surface receptors

Subcutaneous injection every 2 or 4 weeks, if dosed at 200 mg or 400 mg, respectively.

Other biologic DMARDs

  

   Abatacept (Orencia, 2005)

Soluble fusion protein that inhibits the costimulation of T-cells

Intravenous infusion every 4 weeks

   Anakinra (Kineret, 2001)

Recombinant IL-1 receptor antagonist that inhibits the binding of IL-1 to its receptor, thereby allowing regulation of IL-1 activity

Subcutaneous injection daily

   Rituximab (Rituxan, 2006)

Chimeric monoclonal antibody that binds to the cell surface protein CD20 and selectively depletes B-cells.

Intravenous infusion: two infusions separated by 2 weeks every 24 weeks or based on clinical evaluation

   Tocilizumab (Actemra, 2010)

Humanized IL-6 receptor that inhibits the binding of IL-6 to its receptor, preventing IL-6 signal transduction

Intravenous infusion every 4 weeks

  1. aDMARDs, disease-modifying antirheumatic drugs; Fab', fragment antigen-binding region; RA, rheumatoid arthritis; FDA, Food and Drug Administration; TNF, tumor necrosis factor; IL, interleukin.