Tocilizumab

Products

Tocilizumab is commercially available as a concentrate for the preparation of an infusion solution and as a solution for injection in a prefilled syringe and in a prefilled pen (Actemra, RoActemra in some countries). It has been approved in many countries since 2008.

Structure and properties

Tocilizumab is a recombinant humanized IgG1 monoclonal antibody against the human interleukin-6 receptor (IL-6R). It has a molecular mass of approximately 148 kDa.

Effects

Tocilizumab (ATC L04AC07) has selective immunosuppressive and anti-inflammatory properties. The effects are based on binding to the IL-6 receptor and inhibition of signal transduction. This abrogates the effects of the proinflammatory and immunostimulatory cytokine interleukin-6 (IL-6).

Indications

  • Rheumatoid arthritis
  • Polyarticular juvenile idiopathic arthritis
  • Systemic juvenile idiopathic arthritis
  • Castleman’s disease (not in all countries).

Dosage

According to the SmPC. The drug is administered as an intravenous infusion or subcutaneous injection.

Contraindications

  • Hypersensitivity
  • Combination with TNF-alpha inhibitors

For complete precautions, see the drug label.

Interactions

Tocilizumab should not be combined with TNF-alpha inhibitors. It may increase the activity of CYP450 isozymes, causing appropriate interactions.

Adverse effects

The most common potential adverse effects include respiratory infections, nasopharyngitis, headache, hypertension, and elevated liver enzyme levels (ALT). Tocilizumab may increase the risk for serious infectious diseases, especially in combination with immunosuppressants.