What to Know About Xeljanz (Tofacitinib)

Xeljanz (tofacitinib citrate) is an oral Janus kinase (JAK) inhibitor—a type of disease-modifying anti-rheumatic drug (DMARD)—used to treat moderately to severely active rheumatoid arthritis (RA) in adults. Typically prescribed after unsuccessful treatment with methotrexate, Xeljanz relieves joint pain, inflammation, and stiffness by decreasing immune system activity through a different therapeutic pathway than other DMARDs.

Xeljanz is available in both immediate- and extended-release formulations. There is no generic.

Uses

Xeljanz is approved to treat rheumatoid arthritis, psoriatic arthritis, and ulcerative colitis. It can be used alone (as monotherapy) or combined with methotrexate or other non-biologic DMARDs.

Approved by the U.S. Food and Drug Administration (FDA) in 2012, Xeljanz is considered a small-molecule medication, not a biologic drug. Biologics block pro-inflammatory cytokines from outside the cell while Xeljanz works from the inside.

Xeljanz inhibits the JAK pathway—a signaling pathway inside cells that plays a significant role in inflammation associated with rheumatoid arthritis. JAKs are intracellular enzymes that transmit signals that arise from cytokine or growth factor-receptor interactions on the cell membrane.

Before Taking

Xeljanz is indicated in rheumatoid arthritis treatment after methotrexate has failed to bring the disease into remission. Prior to prescribing Xeljanz, your doctor will go over your medical history including your current RA symptoms and previous treatment regimens.

In addition, your doctor will perform skin tests to check for tuberculosis and run blood tests to check your cholesterol levels, liver enzymes, and blood cell counts. Baseline levels will be recorded before starting therapy with Xeljanz so they can be referenced later. Periodic laboratory tests are recommended during the duration of treatment because Xeljanz may cause changes to certain types of white blood cells, hemoglobin, liver enzymes, and lipids.

You may also need to update your vaccinations prior to treatment with Xeljanz, as live-virus vaccines must be avoided while taking the drug. These vaccines include:

• Shingles
• FluMist influenza nasal spray
• Measles, mumps, and rubella
• Yellow fever

Precautions and Contraindications

Your doctor will go over the potential benefits and risks of this drug with you prior to prescribing the treatment. Xeljanz may pose more of a risk to people with certain conditions. Tell your doctor if you are age 50 or older, smoke, or have or have ever had:

• Cancer
• Diabetes
• High cholesterol
• High blood pressure
• HIV or AIDS
• Infections that are frequent, chronic, or come and go, whether systemic or local, such as open wounds, sores, and cold sores
• Liver disease
• Kidney transplant
• Lung disease
• Other immune system disorders
• Tuberculosis
• Gastrointestinal perforations

In addition, let your doctor know if you live or have ever lived in areas where the fungal infection histoplasmosis is more common, such as the Ohio or Mississippi River valleys, parts of Central and South America, Africa, Asia, and Australia.

Dosage

Regular Xeljanz is to be taken twice daily—5 milligrams (mg) per dose.

Xeljanz-XR, the extended-release version, comes as an 11-mg tablet that is taken once daily.

Xeljanz can be taken with or without food and should be swallowed whole. Do not chew, split, or crush it.

If you miss a dose, take it as soon as you remember unless it is almost time for the next dose. In that case, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one. Ask your doctor or pharmacist if you have any questions.

Side Effects

The most common adverse effects associated with Xeljanz, which occurred during the first three months of use in clinical trials, were:

• Upper respiratory tract infections
• Headache
• Diarrhea
• Stuffy or runny nose

Tell your doctor if these symptoms are severe or do not go away.

Xeljanz may increase your cholesterol levels. Your doctor will monitor your cholesterol closely while taking this medication.

Severe

There are also some serious side effects associated with taking Xeljanz. If you experience any of the following, call your doctor immediately or seek emergency medical treatment:

• Hives
• Swelling of face, eyes, lips, or throat
• Difficulty swallowing or breathing
• Stomach pain accompanied by fever and diarrhea or constipation
• Yellowing of the skin or eyes
• Loss of appetite
• Dark urine
• Clay-colored bowel movements
• Vomiting
• Rash
• Pale skin
• Shortness of breath

Warnings and Interactions 

Xeljanz carries a black box warning for serious and potentially deadly adverse events. These include:

• Serious infections leading to hospitalization or death, such as tuberculosis, bacterial, invasive fungi, viral, and other opportunistic infections
• Lymphoma and other malignancies
• Epstein-Barr virus–associated lymphoproliferative disorder

Xeljanz should not be taken alongside biologic drugs. These include:

• Enbrel (etanercept)
• Remicade (infliximab)
• Humira (adalimumab)
• Cimzia (certolizumab pegol)
• Simponi (golimumab)
• Orencia (abatacept)
• Actemra (tocilizumab)
• Rituxan (rituximab)

Some medications should be used with caution when taking Xeljanz and may require your doctor to alter your dosage or monitor you for side effects including liver damage. These include:

• Nonsteroidal anti-inflammatory medications (NSAIDs) such as aspirin, Advil or Motrin (ibuprofen), and Naprosyn or Aleve (naproxen)
• Kineret (anakinra)
• Azasan, Imuran (azathioprine)
• Gengraf, Neoral, Sandimmune (cyclosporine)
• Otrexup, Rasuvo, Trexall (methotrexate)
• Steroids including dexamethasone, Medrol (methylprednisolone), Prelone (prednisolone), and prednisone
• Diflucan (fluconazole)
• Onmel, Sporanox (itraconazole)
• Xolegel (ketoconazole)
• Carbatrol, Tegretol, Equetro (carbamazepine)
• Biaxin (clarithromycin)
• Crixivan (indinavir)
• Viracept (nelfinavir)
• Nefazodone
• Phenobarbital
• Dilantin/Phenytek (phenytoin)
• Mycobutin (rifabutin)
• Rifadin/Rimactane (rifampin)