Xeljanz 5 Mg (Tofacitinib) – 60 Tablets

Introduction to Xeljanz 5 mg

Xeljanz 5 mg (tofacitinib) is an oral Janus kinase (JAK) inhibitor that may be used alone or with other medications to treat inflammatory and autoimmune conditions such as rheumatoid arthritis, psoriatic arthritis, ulcerative colitis, ankylosing spondylitis, and polyarticular juvenile idiopathic arthritis.

 

As an immediate-release, film-coated tablet, it is typically taken twice daily and works by targeting the immune system pathways responsible for inflammation and joint damage.

 

Developed and manufactured by Pfizer, Xeljanz 5 mg has become an essential treatment for conditions such as moderate to severe rheumatoid arthritis, active psoriatic arthritis, ulcerative colitis, ankylosing spondylitis, and polyarticular-course juvenile idiopathic arthritis (pcJIA) in children aged 2 and older. Its oral formulation provides a convenient alternative to injectable therapies, allowing patients to manage symptoms more easily in daily life.

 

Xeljanz works by decreasing the activity of the immune system. It does this by blocking the activity of JAK enzymes (JAK1, JAK2, JAK3, TYK2) inside the cell – these enzymes are responsible for sending inflammatory signals in the body which are associated with cytokine release. Xeljanz’s mechanism of action of blocking these enzymes helps to decrease the immune reaction which causes rheumatoid arthritis, psoriatic arthritis, and ulcerative colitis.

 

With its proven efficacy and broad therapeutic applications, Xeljanz 5 mg offers hope for individuals seeking effective relief from chronic autoimmune conditions, combining convenience, precision, and advanced medical science in one tablet.

 

Xeljanz was FDA-approved on November 6, 2012, and was the first JAK inhibitor to be approved for rheumatoid arthritis.

 

What is Xeljanz 5 mg?

Xeljanz 5 mg is an oral JAK inhibitor that works by targeting immune system pathways to reduce inflammation. This medication is prescribed for multiple autoimmune conditions, including rheumatoid arthritis, psoriatic arthritis, ulcerative colitis, ankylosing spondylitis, and polyarticular-course juvenile idiopathic arthritis (pcJIA) in children aged 2 and older. The immediate-release 5 mg tablet is typically taken twice daily, while the extended-release version (Xeljanz XR) is taken once daily.

 

Medical Uses of Xeljanz 5 mg (Approved Indications)

Xeljanz or Xeljanz XR may be used to treat the following conditions in adults who are unable to take or did not respond to one or more tumor necrosis factor (TNF) inhibitor medication(s):

Rheumatoid Arthritis (RA)

Xeljanz 5 mg is used to treat moderate to severe rheumatoid arthritis, especially for people who haven’t had enough relief from methotrexate or other DMARDs. It works by targeting the JAK pathway, helping to reduce joint pain, swelling, and stiffness so you can move more comfortably and enjoy daily activities.

Psoriatic Arthritis (PsA)

For people with active psoriatic arthritis, Xeljanz 5 mg helps ease joint pain and swelling while protecting your joints from further damage. By gently regulating the immune system, it can improve your mobility and daily function, making it a convenient oral option compared to biologic DMARDs or TNF inhibitors.

Ulcerative Colitis (UC)

Xeljanz 5 mg is approved as a maintenance therapy for moderate to severe ulcerative colitis after an initial induction period. By modulating immune responses in the gut, it can help achieve and maintain remission, improve mucosal healing, and reduce the frequency of flare-ups.

Ankylosing Spondylitis (AS)

If you have active ankylosing spondylitis, Xeljanz 5 mg can help ease inflammation in the spine and joints, improving flexibility and reducing pain. Its oral formulation makes it a practical choice for managing symptoms and keeping you moving more freely.

Polyarticular-course Juvenile Idiopathic Arthritis (pcJIA)

For children aged 2 and older who weigh at least 40 kg, Xeljanz 5 mg can help manage polyarticular-course juvenile idiopathic arthritis (pcJIA). It works to reduce joint inflammation and improve daily activity, helping young patients maintain mobility and enjoy their everyday life.

 

How Xeljanz Works in the Body

Xeljanz 5 mg functions as a JAK inhibitor, targeting Janus kinase enzymes that play a critical role in immune system signaling. By interfering with these pathways, Xeljanz reduces inflammation and autoimmune activity, helping alleviate symptoms of RA, PsA, UC, AS, and pcJIA.

 

How the JAK-STAT pathway works

• 1. Cytokine receptor binding:
  In autoimmune conditions, cytokines (inflammatory proteins) bind to receptors on cells. 
• 2. JAK activation:
  This binding activates Janus kinases (JAKs) inside the cell. 
• 3. STAT activation:
  Activated JAKs then activate STAT (Signal Transducer and Activator of Transcription) proteins.

The immediate-release 5 mg tablet works quickly, while the extended-release Xeljanz XR provides sustained effects throughout the day. Both formulations are film-coated to ensure stability and patient-friendly dosing.

 

Regulatory History & Clinical Trials

When it comes to trust and safety, Xeljanz 5 mg has built its reputation through years of careful research and strict regulatory reviews. Since its launch, it has received multiple approvals around the world, each supported by large clinical trials that looked closely at both its benefits and potential risks.

Date	Regulatory Event	Details
November 6, 2012	FDA Approval (USA)	First approved for moderate to severe rheumatoid arthritis (RA) in adults who did not respond well to methotrexate.
December 2014	EMA Approval (Europe)	Approved by the European Medicines Agency for rheumatoid arthritis.
December 2017	FDA Approval	Expanded approval for psoriatic arthritis (PsA) in adults with active disease.
May 2018	FDA Approval	Approved for moderate to severe ulcerative colitis (UC) after induction therapy.
December 2019	FDA Approval	Approved for polyarticular-course juvenile idiopathic arthritis (pcJIA) in children aged 2 and older weighing ≥40 kg.
December 2021	FDA Boxed Warning Update	After results from the ORAL Surveillance study, the FDA strengthened warnings about risks of serious heart-related events, cancer, blood clots, and death for tofacitinib compared with TNF inhibitors.
2021	EMA Safety Update	EMA also issued restrictions and safety recommendations following similar trial results.

Key Clinical Trials

• ORAL Solo (2012): Demonstrated the effectiveness of Xeljanz as monotherapy in rheumatoid arthritis.
• ORAL Sync (2012): Showed significant improvement in RA patients already taking methotrexate.
• ORAL Surveillance (2019–2021): A long-term safety study comparing Xeljanz to TNF inhibitors, which highlighted higher risks of cardiovascular events, cancer, and blood clots, leading to stronger regulatory warnings.

In summary, Xeljanz 5 mg has been extensively studied and approved for a variety of conditions for nearly a decade. Although it has shown strong benefits in reducing inflammation and improving quality of life, both doctors and patients are advised to carefully consider the safety risks identified in clinical trials and follow the recommended observations.

 

Dosage & Administration of Xeljanz 5 Mg

When it comes to taking Xeljanz 5 mg, getting the dose exactly right is the key to feeling safe. Carefully follow doctor’s instructions to maximize its benefits while staying protected from side effects.

 

Xeljanz dosing for adults with rheumatoid arthritis, psoriatic arthritis, or ankylosing spondylitis

 

Xeljanz 5 mg twice a day

OR

Xeljanz XR 11 mg once a day.

 

Notes:

Moderate to severe renal impairment or moderate hepatic impairment. Reduce the dosage to Xeljanz 5mg once daily.

Psoriatic arthritis: use in combination with nonbiologic DMARDs. Some deep research  information are below:

Condition	Recommended Dose	Notes / Administration
Rheumatoid Arthritis (RA)	5 mg twice daily	Can be used alone or with methotrexate/other DMARDs.
Psoriatic Arthritis (PsA)	5 mg twice daily	For patients with inadequate response to other DMARDs.
Ulcerative Colitis (UC)	10 mg twice daily for first 8 weeks, then 5 mg twice daily for maintenance	Start with an induction dose, then switch to maintenance.
Ankylosing Spondylitis (AS)	5 mg twice daily	Helps manage pain, stiffness, and inflammation.
Polyarticular-course Juvenile Idiopathic Arthritis (pcJIA)	5 mg twice daily (for children ≥40 kg, aged 2 and older)	Oral solution or tablets can be used depending on the patient’s weight/age.
Renal or Hepatic Impairment	May require dose adjustment	The doctor will decide based on test results.
Elderly Patients	Use with caution	Higher risk of infections and complications.

Administration Tips

• Take Xeljanz 5 mg tablets with or without food.
• Swallow whole; do not crush or chew.
• Try to take it at the same time every day to maintain steady levels.
• Do not stop suddenly without your doctor’s advice.

 

Safety Profile & Warnings of Xeljanz 5 mg

Xeljanz 5 mg is an effective medication, but like all treatments, it comes with safety considerations that patients should be aware of. Understanding these warnings helps you use it safely and get the best results.

Key Safety Points

• Infection risk: Xeljanz can lower your immune defenses, making it easier to catch infections such as shingles, pneumonia, or urinary tract infections. Always report any signs of fever, cough, or unusual symptoms to your doctor.
• Blood clots: There’s a small risk of deep vein thrombosis (DVT) or pulmonary embolism (PE), especially in patients with pre-existing risk factors.
• Heart health: Patients with heart disease or risk factors should use Xeljanz cautiously, as it may increase the risk of heart attack or stroke.
• Cancer risk: Long-term use may slightly raise the chance of developing certain cancers, such as lymphoma or skin cancer.
• Blood disorders: Rarely, Xeljanz may affect blood cells, leading to low white or red blood cell counts.
• Liver issues: Liver enzyme levels may increase, so regular blood tests are essential.
• Gastrointestinal warnings: Xeljanz may rarely cause gastrointestinal perforations, particularly in patients with existing bowel issues.

Important Tips for Safe Use

• Screening before treatment: Tests for tuberculosis and hepatitis B/C are recommended before starting Xeljanz.
• Vaccinations: Avoid live vaccines during treatment.
• Regular monitoring: Blood tests and check-ups help detect early signs of side effects.
• Communication: Always tell your doctor about your full medical history, including heart, liver, or immune system conditions.

Benefits and Effectiveness of Xeljanz 5 mg

Living with conditions like rheumatoid arthritis or psoriatic arthritis often means daily struggles with pain, stiffness, and fatigue. Xeljanz 5 mg was designed to make life easier by addressing these challenges in a gentle yet effective way.

• Relieves pain and swelling – One of the most noticeable benefits is the reduction of joint pain, tenderness, and swelling. Many patients start to feel more comfortable moving around within just a few weeks.
• Improves mobility and flexibility – By calming down inflammation, Xeljanz helps restore easier movement in your joints, making day-to-day tasks less stressful.
• Slows disease progression – Beyond just easing symptoms, Xeljanz 5 mg works on a deeper level by slowing the damage that arthritis can cause over time. This means better long-term protection for your joints.
• Convenient oral treatment – Unlike injectable biologics, Xeljanz comes as a simple pill. No needles, no complicated schedules—just a tablet you can take at home.
• Better quality of life – With less pain and more mobility, many people report being able to return to activities they enjoy, whether it’s walking, working, or spending quality time with family.

Real-life experience: Many patients share that after just a few months on Xeljanz 5 mg, they could return to activities they had set aside for years. For one, it meant gardening without constant pain. For another, it meant being able to go on walks with their family again. These small victories add up to a big difference in quality of life.

In short, Xeljanz 5 mg doesn’t just treat the condition—it gives you back parts of your life that arthritis may have taken away. It’s about comfort, confidence, and the freedom to do more of what matters most.

 

Xeljanz 5 mg Side Effects and Risks

Like all powerful medicines, Xeljanz 5 mg can bring great benefits, but it also carries some risks. Knowing the possible side effects helps patients and caregivers stay prepared and safe.

 

Common Side Effects

The most common side effects of Xeljanz are:

• skin rash, acne, shingles
• upper respiratory tract infection or cold symptoms such as stuffy nose, sneezing, sore throat
• increased blood pressure
• diarrhea
• abnormal blood tests
• elevated cholesterol levels
• fever
• headache
• nausea, or vomiting.

Serious side effects and warnings

Xeljanz and Xeljanz XR carry a Boxed Warning for serious infections, death, cancer, cardiovascular events, and blood clots.

 

Serious infections: Since Xeljanz works by influencing your immune system, it may reduce your body’s natural defense against infections. This can lead to serious illnesses, including tuberculosis (TB) and infections from bacteria, fungi, or viruses that may spread throughout the body. In rare cases, these infections have resulted in death.

• Infections: Xeljanz can lower your immune system, making it easier to catch infections like shingles, pneumonia, or urinary tract infections.
• Blood clots: In rare cases, patients may experience deep vein thrombosis (DVT) or pulmonary embolism (PE).
• Heart-related issues: There may be a higher risk of heart attack or stroke, especially in patients with existing heart problems.
• Cancer risk: Long-term use has been linked with a slightly increased risk of certain cancers, such as lymphoma.
• Blood abnormalities: Changes in blood cell counts (like low white or red blood cells) can happen.

 

Monitoring and Safety Precautions

Regular monitoring is very important while taking Xeljanz 5 mg:

• TB and Hepatitis B/C screening before treatment.
• Blood tests: CBC, liver function tests, cholesterol levels.
• Blood pressure checks to monitor for hypertension.
• Vaccination guidance: Avoid live vaccines during therapy.
• Pregnancy and breastfeeding precautions: Xeljanz 5 mg should only be used under medical supervision. You have to wait 18 hours if you are breastfeeding.

Drug Interactions with Xeljanz

Xeljanz 5 mg may interact with certain medications, which may change its effectiveness or increase the risk of side effects. That’s why it’s very important to tell your doctor about all the medications, vitamins, or herbal supplements you’re taking.

 

Xeljanz 5 mg is metabolized via CYP3A4 and CYP2C19 pathways.

 

Medicines to Watch Out For

• Strong immune-suppressing drugs (like azathioprine, cyclosporine, or tacrolimus) can make your immune system too weak.
• Biologic DMARDs or TNF inhibitors (like adalimumab, etanercept, infliximab) → not safe to use together with Xeljanz.
• Strong CYP3A4 inhibitors (like ketoconazole, clarithromycin) → can raise the level of Xeljanz in your body, increasing side effects.
• Strong CYP3A4 inducers (like rifampin, carbamazepine, phenytoin) can lower the effect of Xeljanz, making it less effective.

Never start, stop, or change any medication while taking Xeljanz 5 mg unless your doctor approves.

 

Cost and Patient Access

Xeljanz 5 mg is a brand-name medicine, and it can be expensive compared to some other treatments. The exact price depends on where you live, your pharmacy, and your insurance coverage. As a unit pharmacy, the price of xeljanz 5 mg at our pharmacy is a relatively reasonable $4,500 USD. You can search and see if it is more expensive at other pharmacies, online or offline.

To make it more affordable:

• Insurance plans may cover part of the cost.
• Patient assistance programs and coupons from Pfizer (the manufacturer) can help reduce the price.
• Generic tofacitinib (in some countries) may be available at a lower cost.
• Trusted international online pharmacies can sometimes offer more affordable options.
• Sometimes Unit Pharmacy offers their customers, you can check it out.

In short, while Xeljanz 5 mg may seem expensive, there are several ways to make it more affordable – talk to your doctor or pharmacist about the best option for you. Sometimes they also recommend you a unit pharmacy.

 

Specialty Use and Prescribing Context

Xeljanz 5 mg is not a medicine that you can buy and use on your own. It is usually prescribed by specialist doctors, such as rheumatologists (for arthritis), gastroenterologists (for ulcerative colitis), or dermatologists (for psoriatic arthritis).

Doctors prescribe it when:

• Other medicines, like methotrexate or TNF inhibitors, did not work well or caused side effects.
• The patient has a moderate to severe condition that needs stronger treatment.
• Close monitoring (blood tests, health check-ups) can be done to keep treatment safe.

Xeljanz 5 mg is a specialty medicine given only under the guidance of an experienced doctor, especially for patients who need advanced treatment options.

 

Popular FAQ

Q: Is Xeljanz 5 mg safe long-term?
A: Long-term safety depends on monitoring for infections, cardiovascular risk, and cancer.

Q: How long does it take to see results?
A: Some patients notice improvements in joint pain or inflammation within weeks, but UC remission may take longer.

Q: Can I switch from biologics to Xeljanz?
A: Yes, but your doctor will evaluate risk, prior treatments, and immune status.

Q: Do I need regular blood tests while on Xeljanz?
A: Yes, CBC, liver, and lipid monitoring are essential.

Q: What are the alternatives if Xeljanz doesn’t work?
A: Options include TNF inhibitors, other biologic DMARDs, or combination therapies under specialist guidance.

 

Xeljanz ingredients

Active ingredient: tofacitinib citrate

Inactive ingredients:

• Xeljanz 5 mg: croscarmellose sodium, HPMC 2910/Hypromellose 6cP, lactose monohydrate, macrogol/PEG3350, magnesium stearate, microcrystalline cellulose, titanium dioxide, and triacetin.
• Xeljanz 10 mg: 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: cellulose acetate, copovidone, hydroxyethyl cellulose, hydroxypropyl cellulose, HPMC 2910/Hypromellose, magnesium stearate, red iron oxide, sorbitol, titanium dioxide, and triacetin. The printing ink contains ammonium hydroxide, ferrosoferric oxide/black iron, propylene glycol, and shellac glaze.
• Xeljanz XR 22 mg: 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. The printing ink contains ammonium hydroxide, ferrosoferric oxide/black iron oxide, propylene glycol, and shellac glaze.
• Xeljanz oral solution 1mg/mL: grape flavor (natural), hydrochloric acid, lactic acid, purified water, sodium benzoate, sucralose, and xylitol.

Availability

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

 

Storage

Store Xeljanz and 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). Use within 60 days of opening the bottle. Throw away (discard) the remaining solution after 60 days. Write the date when you first start to use the solution on the carton.

 

Keep it in the original bottle and carton to protect it from light.

 

Keep out of reach of children.

 

Conclusion

Xeljanz 5 mg has become a trusted treatment option for people living with autoimmune and inflammatory conditions such as rheumatoid arthritis, psoriatic arthritis, ulcerative colitis, ankylosing spondylitis, and juvenile idiopathic arthritis. Backed by strong clinical research and global regulatory approvals, it offers patients a convenient oral alternative to injections while helping reduce pain, inflammation, and long-term joint damage.

 

Like all powerful medicines, it requires careful monitoring and medical guidance to ensure safe and effective use. Patients should work closely with their specialist to find the right dosage, manage side effects, and monitor their overall health.

 

For those who have struggled with limited relief from other treatments, Xeljanz 5 mg provides new hope and better quality of life. With ongoing research and patient support programs, this therapy continues to open doors for individuals seeking comfort, mobility, and a healthier future.