Tofacitinib

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.

• Tofacitinib is a Janus kinase (JAK) inhibitor indicated for: Rheumatoid Arthritis: Tofacitinib extended-release tablets are indicated for the treatment of adult patients with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to one or more TNF blockers. Limitations of Use: Use of tofacitinib extended-release tablets in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine is not recommended.ICD-10: M06.9

• None.contraindicated

Administration Instructions Tofacitinib extended-release tablets are not interchangeable or substitutable with tofacitinib oral solution. ( 2.1 ) Changes between tofacitinib tablets and tofacitinib extended-release tablets should be made by the healthcare provider. ( 2.1 ) Do not initiate tofacitinib extended-release tablets if absolute lymphocyte count <500 cells/mm 3 , an absolute neutrophil count (ANC) < 1,000 cells/mm 3 or hemoglobin < 9 g/dL. ( 2.1 ) Recommended Dosage Rheumatoid Arthritis Tofacitinib extended-release tablets 11 mg once daily. ( 2.2 ) Psoriatic Arthritis (in combination with nonbiologic DMARDs) Tofacitinib extended-release tablets 11 mg once daily. ( 2.2 ) Ankylosing Spondylitis Tofacitinib extended-release tablets 11 mg once daily. ( 2.2 ) Dosage Adjustment See the full prescribing information for dosage adjustments by indication for patients receiving CYP2C19 and/or CYP3A4 inhibitors; in patients with moderate or severe renal impairment or moderate hepatic impairment; and patients with lymphopenia, neutropenia, or anemia. ( 2.2 , 8.7 , 8.8 ) Use of tofacitinib extended-release tablets in patients with severe hepatic impairment is not recommended in any patient population. ( 2.2 , 8.8 ) 2.1 Important Administration Instructions Tofacitinib extended-release tablets are not interchangeable or substitutable with tofacitinib oral solution. Changes between tofacitinib tablets and tofacitinib extended-release tablets should be made by the healthcare provider [see Dosage and Administration ( 2.2 )] .

Serious Infections: Avoid use of tofacitinib extended-release tablets during an active serious infection, including localized infections. ( 5.1 ) Gastrointestinal Perforations: Use with caution in patients that may be at increased risk. ( 5.6 ) Laboratory Monitoring: Recommended due to potential changes in lymphocytes, neutrophils, hemoglobin, liver enzymes and lipids. ( 5.8 ) Immunizations: Live vaccines: Avoid use with tofacitinib extended-release tablets ( 5.9 ) 5.1 Serious Infections Serious and sometimes fatal infections due to bacterial, mycobacterial, invasive fungal, viral, or other opportunistic pathogens have been reported in patients receiving tofacitinib. The most common serious infections reported with tofacitinib included pneumonia, cellulitis, herpes zoster, urinary tract infection, diverticulitis, and appendicitis. Among opportunistic infections, tuberculosis and other mycobacterial infections, cryptococcosis, histoplasmosis, esophageal candidiasis, pneumocystosis, multidermatomal herpes zoster, cytomegalovirus infections, BK virus infection, and listeriosis were reported with tofacitinib. Some patients have presented with disseminated rather than localized disease, and were often taking concomitant immunomodulating agents such as methotrexate or corticosteroids. Other serious infections that were not reported in clinical studies may also occur (e.g., coccidioidomycosis). Avoid use of tofacitinib extended-release tablets in patients with an active, serious infection, including localized infections.

The following clinically significant adverse reactions are described elsewhere in the labeling: Serious Infections [see Warnings and Precautions ( 5.1 )] Mortality [see Warnings and Precautions ( 5.2 )] Malignancy and Lymphoproliferative Disorders [see Warnings and Precautions ( 5.3 )] Major Adverse Cardiovascular Events [see Warnings and Precautions ( 5.4 )] Thrombosis [see Warnings and Precautions ( 5.5 )] Gastrointestinal Perforations [see Warnings and Precautions ( 5.6 )] Hypersensitivity [see Warnings and Precautions ( 5.7 )] Laboratory Abnormalities [see Warnings and Precautions ( 5.8 )] Most common adverse reactions are: Rheumatoid Arthritis, Psoriatic Arthritis, and Ankylosing Spondylitis : Reported during the first 3 months in rheumatoid arthritis placebo-controlled clinical trials and occurring in ≥2% of patients treated with tofacitinib monotherapy or in combination with DMARDs: upper respiratory tract infection, nasopharyngitis, diarrhea, and headache. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Ajanta Pharma USA Inc. at 855-664-7744 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical 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. Rheumatoid Arthritis The clinical studies described in the following sections were conducted using tofacitinib.

All information provided in this section is applicable to tofacitinib tablets/tofacitinib extended-release tablets as they contain the same active ingredient (tofacitinib). Lactation : Advise not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary The available data with tofacitinib from a pregnancy exposure registry that enrolled 11 exposed patients, pharmacovigilance, and published literature are insufficient to draw conclusions about a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. There are risks to the mother and the fetus associated with rheumatoid arthritis and UC in pregnancy (see Clinical Considerations). In animal reproduction studies, fetocidal and teratogenic effects were noted when pregnant rats and rabbits received tofacitinib during the period of organogenesis at exposures multiples of 73-times and 6.3-times the maximum recommended dose of 10 mg twice daily, respectively. Further, in a peri- and post-natal study in rats, tofacitinib resulted in reductions in live litter size, postnatal survival, and pup body weights at exposure multiples of approximately 73-times the recommended dose of 5 mg twice daily and approximately 36 times the maximum recommended dose of 10 mg twice daily, respectively (see Data). The background risks of major birth defects and miscarriage for the indicated populations are unknown.

Metabolism

Tofacitinib tablets Following oral administration of tofacitinib tablets, peak plasma concentrations are reached within 0.5-1 hour, elimination half-life is about 3 hours and a dose-proportional increase in systemic exposure was observed in the therapeutic dose range. Steady state concentrations are achieved in 24-48 hours with negligible accumulation after twice daily administration.

There is no specific antidote for overdose with tofacitinib. 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, 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 tofacitinib.

• Nov 6, 2012NDANDA203214Pf Prism Cv
• Feb 23, 2016NDANDA208246Pfizer
• Sep 25, 2020NDANDA213082Pfizer
• Aug 19, 2021ANDAANDA214264Zydus Pharms
• Mar 13, 2023ANDAANDA209738Micro Labs
• Mar 14, 2023ANDAANDA209829Zydus Pharms
• Sep 25, 2023ANDAANDA216878Hikma
• Jun 3, 2024ANDAANDA218462Aurobindo Pharma Ltd

1. 1Drug Ineffective44,33824%
2. 2Pain26,18314%
3. 3Arthralgia19,93911%
4. 4Condition Aggravated19,80911%
5. 5Rheumatoid Arthritis19,34210%
6. 6Fatigue17,0169.1%
7. 7Off Label Use15,3858.3%
8. 8Joint Swelling14,7237.9%
9. 9Headache13,6517.3%
10. 10Rash12,3186.6%
11. 11Drug Intolerance12,1346.5%
12. 12Malaise10,7105.8%
13. 13Abdominal Discomfort10,5265.7%
14. 14Pain In Extremity10,4205.6%
15. 15Nausea10,1205.4%

The 10 most recently updated of 313 ClinicalTrials.gov registrations naming Tofacitinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Comparison of Effectiveness and Safety of Tofacitinib Versus Upadacitinib as Add-on to Methotrexate in Rheumatoid Arthritis
  Not yet recruiting · Phase 4 · Interventional · 100 enrolled · Sheikh Zayed Federal Postgraduate Medical Institute
  NCT07636057updated 2026-06-09
• Utilization of a Microdevice for Psoriasis and Atopic Dermatitis
  Not yet recruiting · Phase 4 · Interventional · 10 enrolled · University of California, San Francisco
  NCT07352566updated 2026-06-03
• A Study on the Efficacy and Safety of JAK Inhibitors Versus Calcineurin Inhibitors as Initial Therapy for Interstitial Lung Disease Associated With Antisynthetase Syndrome
  Recruiting · Interventional · 80 enrolled · China-Japan Friendship Hospital
  NCT07406932updated 2026-06-03
• Observational Study To Assess The Effectiveness and Treatment Adherence Of Tofacitinib of Ulcerative Colitis In Clinical Practice In Sweden
  Completed · Observational · 102 enrolled · Pfizer
  NCT04338204updated 2026-06-03
• Evaluation of Oral Tofacitinib in Children Aged 2 to 17 Years Old Suffering From Moderate to Severe Ulcerative Colitis
  Active not recruiting · Phase 3 · Interventional · 118 enrolled · Pfizer
  NCT04624230updated 2026-06-02
• Trial of Sequential Medications AfteR TNFi Failure in Juvenile Idiopathic Arthritis
  Recruiting · Phase 3 · Interventional · 400 enrolled · Duke University
  NCT06654882updated 2026-06-01
• A Phase 3 Study Comparing TLL-018 to Tofacitinib in RA Subjects With Inadequate Response or Intolerance to bDMARDs
  Active not recruiting · Phase 3 · Interventional · 459 enrolled · Hangzhou Highlightll Pharmaceutical Co., Ltd
  NCT06020144updated 2026-05-22
• Modulation of the Immune System in Down Syndrome for Improved Outcomes and Neurodevelopment - 1
  Recruiting · Phase 2 · Interventional · 92 enrolled · University of Colorado, Denver
  NCT07598643updated 2026-05-20
• A Long-term Extension Clinical Study of TLL-018 in Patients With Rheumatoid Arthritis
  Recruiting · Phase 3 · Interventional · 350 enrolled · Hangzhou Highlightll Pharmaceutical Co., Ltd
  NCT06887127updated 2026-05-20
• Safety of Tofacitinib, an Oral Janus Kinase Inhibitor, in Primary Sjogren Disease
  Recruiting · Phase 2 · Interventional · 60 enrolled · National Institute of Dental and Craniofacial Research (NIDCR)
  NCT07281456updated 2026-05-19

Frequently asked questions

How does Tofacitinib work?

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.

What is Tofacitinib used for?

According to FDA labeling, Tofacitinib carries indications including: Tofacitinib is a Janus kinase (JAK) inhibitor indicated for: Rheumatoid Arthritis: Tofacitinib extended-release tablets are indicated for the treatment of adult patients with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to one or more TNF blockers. Limitations of Use: Use of tofacitinib extended-release tablets in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine is not recommended.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Tofacitinib?

Tofacitinib is classified as Janus-associated kinase (JAK) inhibitors, Janus Kinase Inhibitor, Janus Kinase Inhibitors, Decreased Hematopoiesis, Decreased Immunologic Activity.

What are the brand names for Tofacitinib?

Tofacitinib is marketed under brand names including Xeljanz.

What are the contraindications for Tofacitinib?

Tofacitinib labeling lists contraindications including: None.. Always consult the full prescribing information and a clinician.