Brand Name
Xeljanz
Generic Name
Tofacitinib
View Brand Information FDA approval date: November 08, 2012
Classification: Janus Kinase Inhibitor
Form: Tablet, Solution
What is Xeljanz (Tofacitinib)?
XELJANZ/XELJANZ XR/XELJANZ Oral Solution is a Janus kinase inhibitor indicated for: Rheumatoid Arthritis : XELJANZ/XELJANZ XR is indicated for the treatment of adult patients with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to methotrexate. Limitations of Use: Use of XELJANZ/XELJANZ XR in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine is not recommended. Psoriatic Arthritis : XELJANZ/XELJANZ XR is indicated for the treatment of adult patients with active psoriatic arthritis who have had an inadequate response or intolerance to methotrexate or other disease-modifying antirheumatic drugs . Limitations of Use: Use of XELJANZ/XELJANZ XR in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine is not recommended. Ulcerative Colitis : XELJANZ/XELJANZ XR is indicated for the treatment of adult patients with moderately to severely active ulcerative colitis , who have had an inadequate response or who are intolerant to TNF blockers. Limitations of Use: Use of XELJANZ/XELJANZ XR in combination with biological therapies for UC or with potent immunosuppressants such as azathioprine and cyclosporine is not recommended. Polyarticular Course Juvenile Idiopathic Arthritis : XELJANZ/XELJANZ Oral Solution is indicated for the treatment of active polyarticular course juvenile idiopathic arthritis in patients 2 years of age and older. Limitations of Use: Use of XELJANZ/XELJANZ Oral Solution in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine is not recommended. Rheumatoid Arthritis XELJANZ/XELJANZ XR is indicated for the treatment of adult patients with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to methotrexate. Limitations of Use: Use of XELJANZ/XELJANZ XR in combination with biologic disease-modifying antirheumatic drugs or with potent immunosuppressants such as azathioprine and cyclosporine is not recommended. Psoriatic Arthritis XELJANZ/XELJANZ XR is indicated for the treatment of adult patients with active psoriatic arthritis who have had an inadequate response or intolerance to methotrexate or other disease-modifying antirheumatic drugs . Limitations of Use: Use of XELJANZ/XELJANZ XR in combination with biologic DMARDs or with potent immunosuppressants such as azathioprine and cyclosporine is not recommended. Ulcerative Colitis XELJANZ/XELJANZ XR is indicated for the treatment of adult patients with moderately to severely active ulcerative colitis , who have an inadequate response or who are intolerant to TNF blockers. Limitations of Use: Use of XELJANZ/XELJANZ XR in combination with biological therapies for UC or with potent immunosuppressants such as azathioprine and cyclosporine is not recommended. Polyarticular Course Juvenile Idiopathic Arthritis XELJANZ/XELJANZ Oral Solution is indicated for the treatment of active polyarticular course juvenile idiopathic arthritis in patients 2 years of age and older. Limitations of Use: Use of XELJANZ/XELJANZ Oral Solution in combination with biologic DMARDs or with potent immunosuppressants such as azathioprine and cyclosporine is not recommended.
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Brand Information
XELJANZ (tofacitinib)
1CONTRAINDICATIONS
None.
2ADVERSE REACTIONS
The following clinically significant adverse reactions are described elsewhere in the labeling:
- Serious Infections
- Increased Risk of Mortality
- Malignancy and Lymphoproliferative Disorders
- Major Adverse Cardiovascular Events
- Thrombosis
- Gastrointestinal Perforations
- Hypersensitivity Reactions
- Laboratory Abnormalities
2.1Clinical Trials Experience
Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not predict the rates observed in a broader patient population in clinical practice.
The clinical studies described in this subsection were conducted using XELJANZ tablets (referred to as “XELJANZ” in this subsection of labeling) and/or XELJANZ oral solution.
2.2Postmarketing Experience
The following adverse reactions have been identified during post-approval use of XELJANZ (tablets and oral solution) and XELJANZ XR (extended-release tablets). Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Immune system disorders: Drug hypersensitivity (events such as angioedema and urticaria have been observed)
Skin and subcutaneous tissue disorders: Acne
3DRUG INTERACTIONS
Table 7 includes drugs with clinically significant drug interactions when concomitantly used with XELJANZ (tablets and oral solution) and XELJANZ XR (extended-release tablets) and instructions for preventing or managing them.
4OVERDOSAGE
There is no specific antidote for overdose with XELJANZ (tablets and oral solution) and XELJANZ XR (extended-release tablets). In case of an overdose, it is recommended that the patient be monitored for signs and symptoms of adverse reactions.
In a study in patients with end-stage renal disease (ESRD) undergoing hemodialysis, plasma tofacitinib concentrations declined more rapidly during the period of hemodialysis and dialyzer efficiency, calculated as dialyzer clearance/blood flow entering the dialyzer, was high [mean (SD) = 0.73 (0.15)]. However, due to the significant non-renal clearance of tofacitinib, the fraction of total elimination occurring by hemodialysis was small, and thus, limits the value of hemodialysis for treatment of overdose with XELJANZ/XELJANZ XR.
Consider contacting the Poison Help line (1-800-222-1222) or a medical toxicologist for additional overdose management recommendations.
5DESCRIPTION
XELJANZ (tofacitinib) tablets, XELJANZ XR (tofacitinib) extended-release tablets and XELJANZ (tofacitinib) oral solution are formulated with the citrate salt of tofacitinib, a JAK inhibitor.
Tofacitinib citrate is a white to off-white powder with the following chemical name: (3R,4R)-4-methyl-3-(methyl-7H-pyrrolo [2,3-d]pyrimidin-4-ylamino)-ß-oxo-1-piperidinepropanenitrile, 2-hydroxy-1,2,3-propanetricarboxylate (1:1).
The solubility of tofacitinib citrate in water is 2.9 mg/mL.
Tofacitinib citrate has a molecular weight of 504.5 Daltons (or 312.4 Daltons as the tofacitinib free base) and a molecular formula of C
XELJANZ tablets is supplied for oral administration as a:
- 5 mg white round, immediate-release film-coated tablet. Each tablet contains 5 mg of tofacitinib (equivalent to 8.08 mg of tofacitinib citrate) and the following inactive ingredients: croscarmellose sodium, HPMC 2910/Hypromellose 6cP, lactose monohydrate, macrogol/PEG3350, magnesium stearate, microcrystalline cellulose, titanium dioxide, and triacetin.
- 10 mg blue round, immediate-release film-coated tablet. Each tablet contains 10 mg of tofacitinib (equivalent to 16.16 mg of tofacitinib citrate) and the following 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 is supplied for oral administration as a:
- 11 mg pink, oval, extended-release film-coated tablet with a drilled hole at one end of the tablet band. Each tablet contains 11 mg of tofacitinib (equivalent to 17.77 mg tofacitinib citrate) and the following 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 oxide, propylene glycol, and shellac glaze.
- 22 mg beige, oval, extended-release film-coated tablet with a drilled hole at one end of the tablet band. Each tablet contains 22 mg of tofacitinib (equivalent to 35.54 mg tofacitinib citrate) and the following 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 is supplied for oral administration as a 1 mg/mL clear, colorless solution. Each 1 mL contains 1 mg of tofacitinib (equivalent to 1.62 mg of tofacitinib citrate) and the following inactive ingredients: grape flavor (natural), hydrochloric acid, lactic acid, purified water, sodium benzoate, sucralose, and xylitol.
6HOW SUPPLIED/STORAGE AND HANDLING
How Supplied Information for XELJANZ Tablets and XELJANZ XR
How supplied information for XELJANZ tablets and XELJANZ XR (extended-release tablets) is shown in Table 23.
How Supplied Information for XELJANZ Oral Solution
XELJANZ (tofacitinib) oral solution, 1 mg/mL is supplied in bottles (240 mL fill volume) (NDC 0069-1029-02) and is a clear, colorless solution that contains 1 mg of tofacitinib. Each high-density polyethylene (HDPE) bottle contains one press-in bottle adapter and one 5 mL oral dosing syringe with 3.2 mL, 4 mL, and 5 mL gradations. The press-in bottle adapter and oral dosing syringe are not made with natural rubber latex.
Storage and Handling for XELJANZ Tablets/XELJANZ XR
Store XELJANZ tablets and XELJANZ XR at 20°C to 25°C (68°F to 77°F). [See USP Controlled Room Temperature].
Do not repackage.
Storage and Handling for XELJANZ Oral Solution
Store at 20°C to 25°C (68°F to 77°F), excursions permitted between 15°C and 30°C (between 59°F and 86°F). [See USP Controlled Room Temperature].
Store in the original bottle and carton to protect from light.
Use contents of bottle within 60 days of opening.
Discard unused oral solution after 60 days.
7PATIENT COUNSELING INFORMATION
Advise patients to read the FDA-approved patient labeling (Medication Guide and Instructions for Use).
8INSTRUCTIONS FOR USE
XELJANZ® (ZEL' JANS')
(tofacitinib)
oral solution
(tofacitinib)
oral solution
Read this Instructions for Use before you start taking XELJANZ oral solution and each time you get a refill. There may be new information. This leaflet does not take the place of talking to your healthcare provider about your medical condition or treatment.
Important information about measuring XELJANZ oral solution:
Always use the oral dosing syringe that comes with XELJANZ oral solution to measure and take your prescribed dose. Ask your healthcare provider or pharmacist to show you how to measure your prescribed dose if you are not sure.
How should I store XELJANZ?
- Store XELJANZ oral solution at room temperature between 68°F to 77°F (20°C to 25°C).
- Always store XELJANZ oral solution in the original bottle and carton to protect from light.
Keep XELJANZ and all medicines out of the reach of children.
Use XELJANZ oral solution within 60 days of opening the bottle. Throw away (discard) remaining XELJANZ oral solution after 60 days.
To help you remember when to throw away your bottle of XELJANZ oral solution, you can write the date when you first start to use it on the carton and below:
Date of first use ____ / ____ / ____.
Before each use:
Wash your hands with soap and water and place the items from the carton on a clean, flat surface.
Each carton of XELJANZ oral solution contains:
- 1 press-in bottle adapter
- 1 bottle of XELJANZ oral solution
- 1 oral dosing syringe
Step 1. Remove bottle from carton
Open the carton and remove the bottle of XELJANZ oral solution.
Step 2. Open bottle
Open the bottle by pushing down on the child-resistant cap and turning it to the left (counter-clockwise) as shown. Remove the seal off the top of the bottle
Do not throw away the child-resistant cap.
Note: The bottle does not need to be shaken before use.
Step 3. Insert press-in bottle adapter (first time only)
Remove the press-in bottle adapter and oral dosing syringe from the plastic overwrap. With the bottle on a flat surface, push the ribbed end of the press-in bottle adapter all the way into the neck of the bottle with your thumbs while holding the bottle firmly.
Note: Do not remove the press-in bottle adapter from the bottle after it is inserted.
Step 4. Remove air from oral dosing syringe
Push the oral dosing syringe plunger all the way down to the tip of the syringe barrel to remove excess air.
Step 5. Insert the oral dosing syringe
Insert the oral dosing syringe tip into the upright bottle through the opening of the press-in bottle adapter until it is firmly in place.
Step 6. Withdraw dose from bottle
With the oral dosing syringe in place, turn the bottle upside down. Pull down on the plunger until the bottom of the plunger is even with the markings on the oral dosing syringe for your prescribed dose of oral solution.
If you see air bubbles in the oral dosing syringe, fully push the plunger in so that the oral solution flows back into the bottle. Then withdraw your prescribed dose of oral solution.
Step 7. Remove oral dosing syringe
Turn the bottle upright and place the bottle on a flat surface. Remove the oral dosing syringe from the press-in bottle adapter and bottle by pulling straight up on the oral dosing syringe barrel.
Step 8. Check the dose
Check that the correct dose was drawn up into the oral dosing syringe.
If the dose is not correct, insert the oral dosing syringe tip firmly into the press-in bottle adapter. Fully push in the plunger so that the oral solution flows back into the bottle. Repeat Step 6 and Step 7.
Step 9. Take the dose of XELJANZ
Place the tip of the oral dosing syringe into the inside of the cheek.
Slowly push the plunger all the way down to give all of the medicine in the oral dosing syringe. Make sure there is time to swallow the medicine.
Step 10. Close the bottle
Close the bottle tightly by turning the child-resistant cap to the right (clockwise), leaving the press-in bottle adapter in place.
Place the bottle back into the carton.
Close the carton to protect XELJANZ oral solution from light.
Step 11. Clean oral dosing syringe
Remove the plunger from the barrel by pulling the plunger and the barrel away from each other.
Rinse both with water after each use.
Allow to air dry. When the barrel and plunger are dry, put the oral dosing syringe back together by inserting the plunger into the barrel.
Store the oral dosing syringe with the XELJANZ oral solution.
Do not throw away the oral dosing syringe.
LAB-1422-3.0
This Instructions for Use has been approved by the U.S. Food and Drug Administration.
This Instructions for Use may have been updated. For the most recent Instructions for Use, please visit
9PRINCIPAL DISPLAY PANEL - 5 mg Tablet Bottle Label
PROFESSIONAL SAMPLE-NOT FOR SALE
ALWAYS DISPENSE WITH MEDICATION GUIDE
ALWAYS DISPENSE WITH MEDICATION GUIDE
NDC 63539-012-02
Pfizer
Xeljanz™
(tofacitinib tablets)
(tofacitinib tablets)
5 mg*
60 Tablets
10PRINCIPAL DISPLAY PANEL - 11 mg Tablet Bottle Label
PROFESSIONAL SAMPLE-NOT FOR SALE
ALWAYS DISPENSE WITH MEDICATION GUIDE
ALWAYS DISPENSE WITH MEDICATION GUIDE
NDC 63539-501-30
Pfizer
Xeljanz® XR
(tofacitinib) tablets
(tofacitinib) tablets
Extended Release Tablets
11 mg*
30 Tablets
11PRINCIPAL DISPLAY PANEL - 10 mg Tablet Bottle Label
PROFESSIONAL SAMPLE – NOT FOR SALE
ALWAYS DISPENSE WITH MEDICATION GUIDE
ALWAYS DISPENSE WITH MEDICATION GUIDE
NDC 63539-016-02
Pfizer
Xeljanz®
(tofacitinib) tablets
(tofacitinib) tablets
10 mg*
10mg Is Recommended Only In
Ulcerative Colitis
Ulcerative Colitis
60 Tablets
12PRINCIPAL DISPLAY PANEL - 22 mg Tablet Bottle Label
PROFESSIONAL SAMPLE-NOT FOR SALE
Pfizer
NDC 63539-502-30
Xeljanz
Extended Release Tablets
22 mg*
22mg Is Recommended Only In
30 Tablets
13PRINCIPAL DISPLAY PANEL - 240 mL Bottle Label
PROFESSIONAL SAMPLE – NOT FOR SALE
NDC 63539-029-01
ALWAYS DISPENSE WITH
Pfizer
Xeljanz
1 mg/mL
240 mL
14PRINCIPAL DISPLAY PANEL - 240 mL Bottle Carton
PROFESSIONAL SAMPLE – NOT FOR SALE
NDC 63539-029-02
ALWAYS DISPENSE WITH MEDICATION GUIDE
Pfizer
Xeljanz
1 mg/mL
Contents:
- Oral solution bottle
- 1 Oral dosing syringe
- 1 Press-in bottle adapter
- Prescribing Information
- Medication Guide
- Instructions for Use
240 mL
