Calcineurin inhibitors are topical and systemic immunosuppressants. They can help treat atopic dermatitis and autoimmune disorders such as lupus and psoriasis. They may also help prevent organ transplant rejection.

Examples of topical calcineurin inhibitors include pimecrolimus and tacrolimus ointments. Systemic calcineurin inhibitors include tacrolimus, cyclosporine, and voclosporin.

Calcineurin inhibitors work by blocking the protein calcineurin. Calcineurin plays a role in activating immune cells, such as T cells. By blocking calcineurin, the drugs prevent the activation of the immune cells, which in turn can help manage autoimmune conditions.

Read on to learn more about some common types of calcineurin inhibitors, the conditions they can treat, possible side effects, and more.

Cyclosporine can help treat conditions such as:

Cyclosporine is also used off-label for certain conditions. “Off-label” use is when a drug is approved for one purpose but is prescribed for a different purpose. Off-label uses for cyclosporine include:

Doctors may recommend cyclosporine on its own or alongside other medications.

Doctors may also administer cyclosporine to help prevent organ transplant rejection. In particular, you may require cyclosporine if you have one of the following transplants:

You typically need to take oral cyclosporine daily. It’s available as a pill or in a liquid.

Cyclosporine is also available as eye drops to treat eye conditions such as dry eyes.

Doctors may recommend oral or intravenous (IV) tacrolimus alongside other immunosuppressants, such as azathioprine and mycophenolate, to help prevent organ transplant rejection.

In particular, doctors may recommend tacrolimus in cases of the following transplants:

  • kidney
  • liver
  • heart

Off-label use of tacrolimus can help prevent rejection of the following transplants:

  • pancreas
  • small intestine
  • cornea

It may also help lower the risk of pancreatitis following a liver transplant.

Topical tacrolimus in a 0.1% concentration can help treat atopic dermatitis in adults. Doctors may recommend topical tacrolimus in a 0.03% concentration for children ages 2 to 15 years.

Other conditions tacrolimus can help treat include:

Off-label, the medication may also help treat pediatric psoriasis that affects the face or genitals.

Topical pimecrolimus can help manage symptoms of mild or moderate atopic dermatitis. In the United States, it may be suitable for people over 2 years old.

Pimecrolimus can also help treat:

Voclosporin is an oral calcineurin inhibitor. In 2021, the Food and Drug Administration (FDA) approved it for the treatment of active lupus nephritis in adults.

Your doctor may recommend voclosporin alongside other immunosuppressants.

The side effects of calcineurin inhibitors can depend on the type of drug and whether it’s topical or systemic.

Topical calcineurin inhibitors

Skin irritation is the most common side effect of topical calcineurin inhibitors.

Other side effects of topical calcineurin inhibitors can include:

  • allergic contact dermatitis
  • folliculitis
  • rosacea-like dermatitis
  • acne
  • molluscum contagiosum
  • tinea incognito, which is a fungal skin infection
  • return of a previous infection

Systemic calcineurin inhibitors

Systemic or oral calcineurin inhibitors may cause skin-based side effects such as:

Other side effects can include:

  • heartburn
  • gas
  • diarrhea
  • muscle pain
  • joint pain
  • shaking
  • a burning or tingling sensation in the arms, hands, legs, or feet
  • cramps
  • ear problems
  • sleeping problems
  • depression

It’s important to let your doctor know about any side effects you experience. If side effects are severe, your doctor may recommend changing the type or dosage of medication.

Yes, calcineurin inhibitors can help treat autoimmune disorders. These include conditions such as lupus, rheumatoid arthritis, and psoriasis.

T cells can play a role in organ transplant rejection. By blocking calcineurin, a protein that plays a role in activating T cells, calcineurin inhibitors can help reduce the likelihood of transplant rejection.

T cells are a type of white blood cell, which is part of the immune system. The protein calcineurin plays a role in activating these cells. By blocking calcineurin, the protein is unable to activate the T cells, which in turn can help manage autoimmune conditions.

Learn about T-cell counts.

Yes, calcineurin inhibitors can treat some skin conditions. They can help manage symptoms of autoimmune skin conditions such as psoriasis and vitiligo. They can also treat atopic dermatitis, which develops from an overreaction of the immune system.

Calcineurin inhibitors are a type of immunosuppressant. Topical calcineurin inhibitors include tacrolimus and pimecrolimus. Systemic calcineurin inhibitors include cyclosporine, tacrolimus, and voclosporin.

Calcineurin inhibitors can help treat atopic dermatitis. They may also be suitable for autoimmune conditions such as lupus, psoriasis, and rheumatoid arthritis.

Doctors may recommend calcineurin inhibitors to help prevent transplant rejection.

As with any drug, calcineurin inhibitors can cause side effects. These can include skin irritation, acne, and contact dermatitis. Systemic calcineurin inhibitors can also cause side effects such as diarrhea, muscle or joint pain, cramps, and more.

Speak with your doctor for information about whether they recommend calcineurin inhibitors based on your individual circumstances. They can advise on the possible benefits and risks.