Biologic Medications for RA: The Big Picture

Patient Expert

Patients living with rheumatoid arthritis have many choices when it comes to medication designed to prevent inflammation and further joint damage.   In this post we will be discussing the biologic drugs, or "biologics."   Protein-based and derived from living cells cultured in a laboratory, biologics target specific parts of the immune system rather than the entire immune system as do the traditional systemic drugs (ie. methotrexate, sulfasalazine, cyclosporine).

The biologics (often monoclonal antibodies) act by blocking the action of a specific type of immune cell (T-cell or B-cell lymphocytes) or by blocking proteins in the immune system such as interleukin-1, interleukin-6, or tumor necrosis factor-alpha (TNF-alpha).   These cells and proteins play major roles in the development of inflammatory autoimmune diseases such as rheumatoid arthritis.

As an RA patient who also has multiple sclerosis (MS), I cannot use one of the anti-TNF drugs as they are contraindicated in patients with known demyelinating diseases such as MS.   Because of this I had not thoroughly researched them before, but with the approvals of Cimzia, Simponi and Actemra, it seems to be a good time to learn how the drugs compare.

Cimzia (certolizumab pegol), Simponi (golimumab), Enbrel (etanercept), Humira (adalimumab), and Remicade (infliximab) are drugs which block the action of TNF-alpha, a pro-inflammatory immune system mediator (cytokine) produced by adipose tissue (fat) in the body and other types of cells.   Kineret (anakinra) blocks the activity of interleukin-1 (IL1), a pro-inflammatory cytokine which stimulates T-cells.   Actemra (tocilizumab) is also an interleukin receptor inhibitor, specifically aimed at interleukin-6 (IL6).   Orencia (abatacept) is an immunomodulator which blocks the activity of T-cells, a type of immune cell in the body that causes swelling and joint damage in people who have arthritis.   Rituxan (rituximab) is a monoclonal antibody therapy which targets the protein CD20 found on pre-B and mature B-cell lymphocytes.

I started using Rituxan in November 2009 while continuing to use methotrexate. You can read about my first infusion experience, the second Rituxan infusion, insurance coverage and an assistance program I participated in.

Did you know that the first of these medications were FDA-approved over 10 years ago?   Enbrel and Remicade were approved for use in RA in 1998 and 1999, respectively.   Kineret and Humira were approved in 2001 and 2002, while Orencia and Rituxan were approved in 2005 and 2006.   Simponi and Cimzia were approved in 2009.   Actemra was approved in January 2010.

The biologics are taken by subcutaneous injection or by IV infusion.   Cimzia, Simponi, Enbrel, Humira and Kineret are injected under the skin in the legs, abdomen or arms, typically by the individual with arthritis or a family member.   Actemra, Rituxan, Remicade and Orencia are given through IV infusion in a doctor's office, infusion center, or hospital.

Biologics can increase the risk of infection.   Do not take biologics if your immune system is significantly compromised or you have an active infection.   Screening for tuberculosis (TB), hepatitis B, or other infectious diseases is required before starting treatment with several of these drugs.   Regular blood testing may be required while using any of the biologics to check for liver problems or low blood counts.

Most common side effects for biologics, specifically anti-TNF medications, include: upper respiratory infections; flu-like symptoms; rash and injection site reactions.   According to the patient prescription guides, these side effects are generally mild and in most cases do not cause individuals to stop taking the medication.   If you develop any sign of an infection such as a fever, cough or flu-like symptoms or have any cuts or open sores, you should contact your doctor.   New or worsening psoriasis has been seen in patients using TNF blockers.

Serious side effects for TNF blockers include: heart failure; allergic reactions; nervous system disorders, such as multiple sclerosis, seizures, or inflammation of the nerves of the eyes; blood disorders; and certain types of cancer.   Rarely, people may develop lupus-like symptoms, such as a rash on the cheeks or other parts of the body, sensitivity to the sun, new joint or muscle pain, becoming very tired, chest pain or shortness of breath, swelling of the feet, ankles, and/or legs.

You must NOT receive vaccinations using a live virus when you are taking biologic medications.

In a follow-up post, we will be exploring in greater detail the biologics which have been approved since 2006 including Cimzia, Simponi, Actemra, Rituxan, and Orencia.

Click here to view a spreadsheet I created detailing and comparing the nine biologic medications prescribed for RA.