Font Size

Immunosuppressive Medicines for Lupus


Generic NameBrand Name
azathioprine (AZA)Imuran, Benlysta, Cytoxan, Rheumatrex, CellCept
belimumabImuran, Benlysta, Cytoxan, Rheumatrex, CellCept
cyclophosphamideImuran, Benlysta, Cytoxan, Rheumatrex, CellCept
methotrexate (MTX)Imuran, Benlysta, Cytoxan, Rheumatrex, CellCept
mycophenolate mofetilImuran, Benlysta, Cytoxan, Rheumatrex, CellCept

Depending on the drug, an immunosuppressive medicine may be given in pill form, weekly injections, or by intravenous (IV) pulse therapy (injection given monthly).

Azathioprine, cyclophosphamide, and methotrexate sodium are also referred to as cytotoxic medications.

How It Works

Lupus (systemic lupus erythematosus, or SLE) is an autoimmune disease, in which the immune system attacks the body's own tissues as though they were foreign substances. Immunosuppressive medicines, including cytotoxics, reduce inflammation and suppress the immune system. In higher doses, cytotoxic medicines are also used to treat certain forms of cancer.

Why It Is Used

Azathioprine, mycophenolate, and cyclophosphamide are the most common immunosuppressive medicines used to treat severe kidney disease associated with lupus.

Methotrexate is used to control skin rash and joint pain caused by lupus. It may be tried to allow less corticosteroid medicine to be used.1 Methotrexate is more commonly used to treat rheumatoid arthritis.

Immunosuppressive medicines can be used with corticosteroids for severe, extensive skin rashes or other severe symptoms that do not respond to other therapy. Corticosteroids are often gradually reduced as symptoms are controlled.

Pregnancy and immunosuppressants: Immunosuppressants can cause birth defects. Do not take immunosuppressants if you are pregnant. If you wish to become pregnant or father a child, talk with your doctor. Men or women taking immunosuppressants should stop taking them before trying to conceive a baby.

How Well It Works

Methotrexate may help control skin rashes and joint pain.2 There also are reported benefits for controlling more severe lupus symptoms, such as inflammatory conditions of the kidneys and tissues around the heart and lungs. But there has been little research in these areas.

Other immunosuppressive medicines are used for more severe lupus. Most studies have been done using one of the immunosuppressives, along with corticosteroids, for lupus that is causing serious kidney problems (lupus nephritis). But they are also used to try to control other serious symptoms of lupus, such as inflammation around the heart and lungs. Azathioprine, cyclophosphamide, and mycophenolate mofetil are the most commonly used medicines. They can take several weeks to reach full effectiveness, but they generally help decrease serious symptoms. As the immunosuppressive takes effect, the amount of corticosteroids can usually be decreased.2

Side Effects

Side effects of immunomodulator medicines include:

  • Nausea, vomiting, diarrhea, or stomach ulcers.
  • Rash.
  • General feeling of being ill (malaise).
  • Liver inflammation.

Rare side effects include:

  • Suppression of blood cell production (bone marrow suppression), which may increase the risk of infection or serious bleeding. Return to normal blood cell production may take several weeks after the medicine is stopped.
  • Fever
  • Inflammation of the pancreas (pancreatitis). This may occur with AZA.

Extremely rare side effects of azathioprine include a possible increased risk of cancer. Mycophenolate mofetil may increase the risk of cancer of the lymph system (lymphoma) and other types of cancer.

See Drug Reference for a full list of side effects. (Drug Reference is not available in all systems.)

What To Think About

Taking strong drugs such as azathioprine and cyclophosphamide along with corticosteroids seems to be more effective than taking corticosteroids alone in controlling severe lupus kidney disease, reducing tissue damage, and reducing the maintenance dose of corticosteroids.2

Combinations of both immunosuppressants and corticosteroids can be very effective but also increase the risk of side effects, so regular follow-up and monitoring by your health professional is essential.

Immunosuppressants can cause birth defects. Do not use take immunosuppressants if you are pregnant or wish to become pregnant. Do not father a child while you are taking it.

Immunosuppressive and cytotoxic medications have been associated with a small increase in the risk of developing certain cancers. But if you have severe, possibly life-threatening lupus, you may decide that a medication's risk is outweighed by its potential benefits.

Complete the new medication information form (PDF)Click here to view a form.(What is a PDF document?) to help you understand this medication.



  1. Tassiulas IO, Boumpas DT (2009). Clinical features and treatment of systemic lupus erythematosus. In GS Firestein et al., eds., Kelley's Textbook of Rheumatology, 8th ed., vol. 2, pp. 1263–1300. Philadelphia: Saunders Elsevier.

  2. Hahn BH (2008). Systemic lupus erythematosus. In AS Fauci et al., eds., Harrison's Principles of Internal Medicine, 17th ed., vol. 2, pp. 2075–2083. New York: McGraw-Hill Medical.


ByHealthwise Staff
Primary Medical ReviewerAnne C. Poinier, MD - Internal Medicine
Specialist Medical ReviewerStanford M. Shoor, MD - Rheumatology
Last RevisedMay 23, 2011

eMedicineHealth Medical Reference from Healthwise

This information does not replace the advice of a doctor. Healthwise disclaims any warranty or liability for your use of this information. Your use of this information means that you agree to the Terms of Use. How this information was developed to help you make better health decisions.

To learn more visit

© 1995-2012 Healthwise, Incorporated. Healthwise, Healthwise for every health decision, and the Healthwise logo are trademarks of Healthwise, Incorporated.

Medical Dictionary