Tofacitinib

What is Tofacitinib

• Tofacitinib (Xeljanz/Xeljanz XR/Xeljanz Oral Solution) is a Janus kinase (JAK) inhibitor used to treat moderate-to-severe rheumatoid arthritis.

Tofacitinib

Tofacitinib,JAK

What are the uses of this medicine?

• Xeljanz/Xeljanz XR/Xeljanz Oral Solution is a prescription medicine called a Janus kinase (JAK) inhibitor. Xeljanz/Xeljanz XR is used to treat adults with moderately to severely active rheumatoid arthritis in whom methotrexate did not work well or cannot be tolerated.
• Xeljanz/Xeljanz XR is used to treat adults with active psoriatic arthritis in which methotrexate or other similar medicines called nonbiologic disease-modifying antirheumatic drugs (DMARDs) did not work well or cannot be tolerated.
• Xeljanz/Xeljanz XR is used to treat adults with moderately to severely active ulcerative colitis when medicines called tumor necrosis factor (TNF) blockers did not work well or cannot be tolerated.
• Xeljanz/Xeljanz Oral Solution is used to treat patients 2 years of age and older with active polyarticular juvenile arthritis.

How does this medicine work?

• Tofacitinib (tow" fa sye' ti nib) is an orally available, specific inhibitor of Janus-associated kinases (mainly JAK1 and JAK3) that is used to treat moderate-to-severe rheumatoid arthritis.
• The Janus kinases are critical steps in immune activation as well as in hematopoiesis.
• Tofacitinib is a Janus kinase (JAK) inhibitor.
• JAKs are intracellular enzymes which transmit signals arising from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoiesis and immune cell function.
• Within the signaling pathway, JAKs phosphorylate and activate Signal Transducers and Activators of Transcription (STATs) which modulate intracellular activity including gene expression.
• Tofacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs.

Who Should Not Use this medicine ?

Limitations of Use:

• It is not known if Xeljanz/Xeljanz XR is safe and effective in people with Hepatitis B or C.
• Xeljanz/Xeljanz XR/Xeljanz Oral Solution is not recommended for people with severe liver problems.
• It is not known if Xeljanz/Xeljanz Oral Solution is safe and effective in children for treatment other than active polyarticular juvenile arthritis.
• It is not known if Xeljanz XR is safe and effective in children.
• Use of Xeljanz/Xeljanz Oral Solution in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine is not recommended.
• Use of Xeljanz/Xeljanz XR in combination with biological therapies for (ulcerative colitis) UC or with potent immunosuppressants such as azathioprine and cyclosporine is not recommended.

What drug interactions can this medicine cause?

• Dosage adjustment of Xeljanz/Xeljanz XR/Xeljanz Oral Solution is recommended when coadministered with Strong CYP2C19 Inhibitors (e.g., fluconazole).
• Dosage adjustment of Xeljanz/Xeljanz XR/Xeljanz Oral Solution is recommended when coadministered with Strong CP3A4 Inhibitors (e.g., ketoconazole).
• Coadministration of strong CYP3A4 Inducers (e.g., rifampin)with Xeljanz/Xeljanz XR/Xeljanz Oral Solution is not recommended.
• Coadministration of Immunosuppressive Drugs (e.g., azathioprine, tacrolimus, cyclosporine) with Xeljanz/Xeljanz XR/Xeljanz Oral Solution is not recommended.

Is this medicine FDA approved?

• Tofacitinib was approved for use in the United States in 2012.

How should this medicine be used?

Recommended dosage:

Rheumatoid Arthritis:

• Xeljanz 5 mg twice daily or Xeljanz XR 11 mg once daily.
• Recommended dosage in patients with moderate and severe renal impairment or moderate hepatic impairment is Xeljanz 5 mg once daily.

Psoriatic Arthritis (in combination with nonbiologic DMARDs):

• Xeljanz 5 mg twice daily or Xeljanz XR 11 mg once daily.
• Recommended dosage in patients with moderate and severe renal impairment or moderate hepatic impairment is Xeljanz 5 mg once daily.

Ulcerative Colitis: Induction:

• Xeljanz 10 mg twice daily or Xeljanz XR 22 mg once daily for 8 weeks; evaluate patients and transition to maintenance therapy depending on therapeutic response. If needed, continue Xeljanz 10 mg twice daily or Xeljanz XR 22 mg once daily for a maximum of 16 weeks.
• Discontinue Xeljanz 10 mg twice daily or Xeljanz XR 22 mg once daily after 16 weeks if adequate therapeutic response is not achieved.

Maintenance:

• Xeljanz 5 mg twice daily or Xeljanz XR 11 mg once daily.
• For patients with loss of response during maintenance treatment, Xeljanz 10 mg twice daily or Xeljanz XR 22 mg once daily may be considered and limited to the shortest duration, with careful consideration of the benefits and risks for the individual patient.
• Use the lowest effective dose needed to maintain response.
• Dosage adjustment is needed in patients with moderate and severe renal impairment or moderate hepatic impairment.

Polyarticular Course Juvenile Idiopathic Arthritis:

• Xeljanz/Xeljanz Oral Solution 5 mg twice daily or weight-based equivalent twice daily.
• Dosage adjustment is needed in patients with moderate and severe renal impairment or moderate hepatic impairment.

Administration:

• Take Xeljanz/Xeljanz Oral Solution 2 times a day with or without food.
• Take Xeljanz XR 1 time a day with or without food.
• Swallow Xeljanz XR tablets whole and intact. Do not crush, split, or chew.
• When you take Xeljanz XR, you may see something in your stool that looks like a tablet. This is the empty shell from the tablet after the medicine has been absorbed by your body.
• If you take too much Xeljanz/Xeljanz XR/Xeljanz Oral Solution, call your healthcare provider or go to the nearest hospital emergency room right away.
• For the treatment of psoriatic arthritis, take Xeljanz/Xeljanz XR in combination with methotrexate, sulfasalazine or leflunomide as instructed by your healthcare provider.
• Xeljanz XR should not be used instead of Xeljanz Oral Solution.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Xeljanz Tablets: 5 mg, 10 mg tofacitinib
• Xeljanz XR Tablets: 11 mg, 22 mg tofacitinib
• Xeljanz Oral Solution: 1 mg/mL tofacitinib

This medicine is available in fallowing brand namesː

• Xeljanz

What side effects can this medication cause?

The most common side effects of this medicine include:

Common side effects of Xeljanz/Xeljanz XR in rheumatoid arthritis patients and psoriatic arthritis patients include:

• upper respiratory tract infections (common cold, sinus infections)
• headache
• diarrhea
• nasal congestion, sore throat, and runny nose (nasopharyngitis)
• high blood pressure (hypertension)

Common side effects of Xeljanz/Xeljanz XR in ulcerative colitis patients include:

• nasal congestion, sore throat, and runny nose (nasopharyngitis)
• increased cholesterol levels
• headache
• upper respiratory tract infections (common cold, sinus infections)
• increased muscle enzyme levels
• rash
• diarrhea
• shingles (herpes zoster)

Common side effects of Xeljanz/Xeljanz Oral Solution in polyarticular juvenile arthritis patients include:

• upper respiratory tract infections (common cold, sinus infections)
• nasal congestion, sore throat, and runny nose (nasopharyngitis)
• headache
• fever
• nausea
• vomiting

Xeljanz/Xeljanz XR/Xeljanz Oral Solution may cause serious side effects including:

• Increased risk of death
• Serious infections
• Cancer and immune system problems
• Blood clots in the lungs, veins of the legs or arms, and arteries
• Tears (perforation) in the stomach or intestines
• Allergic reactions
• Changes in certain laboratory test results
• Hepatitis B or C activation infection

What special precautions should I follow?

• Avoid use of Xeljanz/Xeljanz XR/Xeljanz Oral Solution during an active serious infection, including localized infections.
• Thrombosis, including pulmonary, deep venous and arterial, some fatal are reported more commonly in patients treated with Xeljanz 10 mg twice daily compared to 5 mg twice daily. Avoid Xeljanz/Xeljanz XR/Xeljanz Oral Solution in patients at risk. Promptly evaluate patients with symptoms of thrombosis and discontinue Xeljanz/Xeljanz XR/Xeljanz Oral Solution.
• Events of gastrointestinal perforation have been reported in clinical studies with Xeljanz. Use with caution in patients that may be at increased risk.
• Reactions such as angioedema and urticaria that may reflect drug hypersensitivity have been observed in patients receiving Xeljanz/Xeljanz XR. If a serious hypersensitivity reaction occurs, promptly discontinue tofacitinib while evaluating the potential cause or causes of the reaction.
• Treatment with Xeljanz was associated with initial lymphocytosis. Monitor lymphocyte counts at baseline and every 3 months thereafter.
• Treatment with Xeljanz was associated with an increased incidence of neutropenia. Monitor neutrophil counts at baseline and after 4–8 weeks of treatment and every 3 months thereafter.
• Avoid use of live vaccines concurrently with Xeljanz/Xeljanz XR/Xeljanz Oral Solution.

What to do in case of emergency/overdose?

• There is no specific antidote for overdose with Xeljanz/Xeljanz XR/Xeljanz Oral Solution. In case of an overdose, it is recommended that the patient be monitored for signs and symptoms of adverse reactions.
• In a study in subjects with end stage renal disease (ESRD) undergoing hemodialysis, plasma tofacitinib concentrations declined more rapidly during the period of hemodialysis and dialyzer efficiency.

Can this medicine be used in pregnancy?

• Available data with Xeljanz/Xeljanz XR/Xeljanz Oral Solution use in pregnant women are insufficient to establish a drug associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes.
• There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to Xeljanz/Xeljanz XR/Xeljanz Oral Solution during pregnancy.
• To enroll or obtain information from the registry, patients can call the toll free number 1-877-311-8972.

Can this medicine be used in children?

• The safety and effectiveness of Xeljanz/Xeljanz Oral Solution for the treatment of active pcJIA have been established in patients 2 years to 17 years of age.
• Safety and efficacy of Xeljanz/Xeljanz Oral Solution in pediatric patients for indications other than pcJIA (Polyarticular Course Juvenile Idiopathic Arthritis) have not been established.
• The safety and effectiveness of Xeljanz XR in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Xeljanz 5 mg:

• Active ingredient: tofacitinib citrate
• Inactive ingredients: croscarmellose sodium, HPMC 2910/Hypromellose 6cP, lactose monohydrate, macrogol/PEG3350, magnesium stearate, microcrystalline cellulose, titanium dioxide, and triacetin.

Xeljanz 10 mg:

• Active ingredient: tofacitinib citrate
• Inactive ingredients: croscarmellose sodium, FD&C Blue #1/Brilliant Blue FCF Aluminum Lake, FD&C Blue #2/Indigo Carmine Aluminum Lake, HPMC 2910/Hypromellose 6cP, lactose monohydrate, macrogol/PEG3350, magnesium stearate, microcrystalline cellulose, titanium dioxide, and triacetin.

Xeljanz XR 11 mg:

• Active ingredient: tofacitinib citrate
• Inactive ingredients: cellulose acetate, copovidone, hydroxyethyl cellulose, hydroxypropyl cellulose, HPMC 2910/Hypromellose, magnesium stearate, red iron oxide, sorbitol, titanium dioxide, and triacetin. Printing ink contains ammonium hydroxide, ferrosoferric oxide/black iron, propylene glycol, and shellac glaze.

Xeljanz XR 22 mg:

• Active ingredient: tofacitinib citrate
• Inactive ingredients: cellulose acetate, copovidone, FD&C Blue #2 Aluminum Lake, hydroxyethyl cellulose, hydroxypropyl cellulose, HPMC 2910/Hypromellose, magnesium stearate, red iron oxide, sorbitol, titanium dioxide, triacetin, and yellow iron oxide. Printing ink contains ammonium hydroxide, ferrosoferric oxide/black iron oxide, propylene glycol, and shellac glaze.

Xeljanz Oral Solution:

• Active ingredient: tofacitinib citrate
• Inactive ingredients: grape flavor (natural), hydrochloric acid, lactic acid, purified water, sodium benzoate, sucralose, and xylitol.

Who manufactures and distributes this medicine?

• Packager: U.S. Pharmaceuticals

• Distributed by:

Pfizer labs

What should I know about storage and disposal of this medication?

• Store Xeljanz/Xeljanz XR at room temperature between 68°F to 77°F (20°C to 25°C).
• Store Xeljanz Oral Solution at room temperature between 68°F to 77°F (20°C to 25°C) in the original bottle and carton to protect from light.
• Safely throw away Xeljanz Oral Solution that is out of date or no longer needed. Use Xeljanz Oral Solution within 60 days of opening the bottle. Throw away (discard) remaining oral solution after 60 days.

Antirheumatic Agents

• Gold Preparations

• • Auranofin, Gold salts, Gold sodium thiomalate

• Interleukin receptor antagonists

• • Anakinira, Canakinumab, Rilonacept, Sarilumab, Tocilizumab

• Major immunosuppressive agents

• • Cyclosporine, Mycophenylate, Sirolimus, Tacrolimus

• Monoclonal antibodies

• • Adalimumab, Canakinumab, Certolizumab, Golimumab, Infliximab, Rituximab, Sarilumab, Tocilizumab, Ustekinumab

• Thiopurines

• • Azathioprine, Mercaptopurine, Thioguanine

• Tumor necrosis factor antagonists

• • Adalimumab, Certolizumab, Etanercept, Golimumab, Infliximab

• Tyrosine kinase inhibitors

• • Baricitinib, Tofacitinib

• Miscellaneous

• • Abatacept, Flavocoxid, Hydroxychloroquine, Leflunomide, Methotrexate, Penicillamine

• Dailymed label info on Tofacitinib
• FDA Tofacitinib

Tofacitinib Resources
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