Actemra (tocilizumab)

What is tocilizumab, and how does it work (mechanism of action)?

Tocilizumab is an injectable synthetic (man-made) protein that binds to interleukin-6 (IL-6) in the body and blocks the effects of IL-6 in patients with rheumatoid arthritis. Inflammation is the body's reaction to injury and is a necessary process for the repair of injury. IL-6 is a protein that the body produces when there is inflammation. IL-6 promotes inflammation and the signs of inflammation, which, in the case of arthritis, includes fever as well as pain, tenderness, and swelling of the joints. The unchecked inflammation of rheumatoid arthritis eventually leads to destruction of the joints. Tocilizumab binds to IL-6 in the body and thereby blocks the effects of IL-6. As a result, inflammation and its consequences in the joints are reduced, and the progressive destruction of the joints is slowed or prevented. The FDA approved tocilizumab in January 2010.

What brand names are available for tocilizumab?

Actemra

Is tocilizumab available as a generic drug?

No

Do I need a prescription for tocilizumab?

Yes

What are the side effects of tocilizumab?

The most common adverse effects of tocilizumab in clinical studies were:

• respiratory tract infections,
• headaches,
• hypertension (high blood pressure), and
• elevations in liver tests suggesting liver injury.

Injection site reactions (rash, redness, swelling, itching) may also occur. Use of tocilizumab has been associated with serious infections such as:

• tuberculosis,
• sepsis (bacteria in the blood) and
• fungal infections.

Individuals with active infections should not be treated with tocilizumab. Tocilizumab may worsen or cause new diseases of the nervous system. In studies, some patients who used tocilizumab developed cancer. Other side effects include:

• reduced levels of white blood cells or platelets,
• reactivation of herpes zoster infection (shingles), and
• hypersensitivity (allergic) reactions.

In studies, gastrointestinal perforation was observed in patients with diverticulitis.

What is the dosage for tocilizumab?

The recommended dose of tocilizumab is 4-8 mg/kg administered as a single 60 minute intravenous infusion every 4 weeks.

Which drugs or supplements interact with tocilizumab?

Tocilizumab has not been studied in combination with other similar drugs that block other chemicals that promote inflammation, for example, drugs that block TNF (for example, adalimumab  [Humira]). Combining anakinra (Kineret), abatacept (Orencia), rituximab (Rituxan) with other antirheumatic drugs similar to tocilizumab resulted in a reduction in white blood cells in the blood (neutropenia), serious infections and no additional benefit. Tocilizumab may interfere with the effectiveness of vaccines. Live vaccines, including attenuated vaccines, should not be given to patients receiving tocilizumab.

Is tocilizumab safe to take if I'm pregnant or breastfeeding?

There are no adequate studies of tocilizumab in pregnant women.
It is not known whether tocilizumab is excreted in breast milk.

What else should I know about tocilizumab?

What preparations of tocilizumab are available?

Injection: 20 mg/ml

How should I keep tocilizumab stored?

Tocilizumab should be stored refrigerated at 2 to 8 C (36 to 46 F).

Summary

Tocilizumab (Actemra) is a man-made synthetic protein (injectable) prescribed for the treatment of rheumatoid arthritis. Side effects, drug interactions, patient safety and pregnancy information should be reviewed prior to taking any medication.