TOFACITINIB 1 mg/mL Solution
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Janus Kinase Inhibitor class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Tofacitinib is used to treat rheumatoid arthritis (condition in which the body attacks its own joints causing pain, swelling, and loss of function), psoriatic arthritis (a condition that causes joint pain and swelling and scales on the skin), ulcerative colitis (a condition which causes swelling and sores in the lining of the colon [large intestine] and rectum), and polyarticular juvenile idiopathic arthritis (PJIA; a type of childhood arthritis that affects five or more joints during the first six months of the condition, causing pain, swelling, and loss of function). Tofacitinib is in a clas...
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
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UNII 6X543N684K
A natural flavoring derived from grapes that enhances taste appeal. It's used in medicines to improve flavor and make medications more palatable, especially for children or patients who need better taste acceptance.
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UNII QTT17582CB
A strong acid used to adjust and maintain the proper pH level in liquid medicines, ensuring stability and preventing breakdown of active ingredients.
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UNII 33X04XA5AT
Lactic acid is a naturally occurring organic acid derived from milk or plant sources. It lowers and maintains pH in formulations, helps preserve the product, and can enhance ingredient stability and absorption.
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UNII 6DC9Q167V3
Propylene glycol is a clear liquid derived from petroleum or vegetable sources. It acts as a solvent, humectant, and preservative in medicines, helping dissolve active ingredients and maintain product stability.
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UNII OJ245FE5EU
Sodium benzoate is a salt derived from benzoic acid, a preservative. It's added to medicines to prevent growth of bacteria, fungi, and other microorganisms that could spoil the product.
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UNII 55X04QC32I
A strong alkaline chemical used to adjust and maintain the pH balance of liquid medicines. It helps keep the medicine stable and ensures it stays effective during storage.
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UNII 96K6UQ3ZD4
Sucralose is a synthetic sweetener made from sugar. It's added to medicines to improve taste without adding calories, helping make bitter or unpleasant-tasting drugs easier to take.
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UNII 059QF0KO0R
Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.
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UNII VCQ006KQ1E
Xylitol is a naturally occurring sugar alcohol derived from plants. It's used in medicines as a sweetener, bulking agent, and to improve taste, especially in liquid formulations and chewable tablets.
9 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per mL | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · quarterly | No Part D plan price is available for this NDC in our data. | |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| tofacitinib solution 1 mg/mL 00054-0821-58 | Hikma | 1 bottle | — | AA | FDA listed | — |
| Xeljanz 1 mg/mL 00069-1029-02 | Pfizer | 1 bottle | — | AA | FDA listed | — |
| Xeljanz 1 mg/mL 63539-0029-02 | U.S. | 1 bottle | — | AA | FDA listed | — |
| Tofacitinib 1 mg/mLthis 70095-0008-02 | Sun | 1 bottle | — | AA | FDA listed | — |
| Tofacitinib 1 mg/mL 71085-0099-24 | IPG | 1 bottle | — | AA | FDA listed | — |
| Tofacitinib 1 mg/mL 72205-0121-81 | Novadoz | 240 ml | — | AA | FDA listed | — |
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⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 70095-0008-02 You're viewing this | 1 BOTTLE in 1 CARTON (70095-008-02) / 240 mL in 1 BOTTLE | 2026-06-03 | Active |
🧭 About this NDC listing & data coverage
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| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
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📄 Full prescribing information FDA SPL
🚨 Boxed Warning ▾
WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS, and THROMBOSIS SERIOUS INFECTIONS Patients treated with tofacitinib oral solution are at increased risk for developing serious bacterial, fungal, viral, and opportunistic infections, including tuberculosis (TB), that may lead to hospitalization or death [ see Warnings and Precautions (5.1) and Adverse Reactions (6.1) ]. Most patients who developed these infections were taking concomitant immunosuppressants such as methotrexate or corticosteroids.
Reported infections included: Active TB, which may present with pulmonary or extrapulmonary disease. Patients should be tested for latent TB before tofacitinib oral solution use and during therapy. Treatment for latent infection should be initiated prior to tofacitinib oral solution use.
Invasive fungal infections, including cryptococcosis and pneumocystosis. Patients with invasive fungal infections may present with disseminated, rather than localized, disease. Bacterial, viral, including herpes zoster, and other infections due to opportunistic pathogens.
The risks and benefits of tofacitinib oral solution treatment should be carefully considered prior to initiating therapy in patients with chronic or recurrent infection. Patients should be closely monitored for the development of signs and symptoms of infection during and after tofacitinib oral solution treatment, including the possible development of TB in patients who tested negative for latent TB infection prior to initiating therapy. If a serious infection develops, interrupt tofacitinib oral solution until the infection is controlled [see Warnings and Precautions (5.1) ] .
MORTALITY In a large, randomized, postmarketing safety study in rheumatoid arthritis (RA) patients 50 years of age and older with at least one cardiovascular (CV) risk factor comparing XELJANZ tablets 5 mg or 10 mg twice a day to tumor necrosis factor (TNF) blockers, a higher rate of all-cause mortality, including sudden CV death, was observed with XELJANZ tablets 5 mg or 10 mg twice a day [see Warnings and Precautions (5.2) ] . A tofacitinib oral solution 10 mg twice daily dosage is not recommended for the treatment of psoriatic arthritis (PsA), or polyarticular course juvenile idiopathic arthritis (pcJIA) [see Dosage and Administration (2.4) ] .
MALIGNANCIES Malignancies, including lymphomas and solid tumors, have occurred in patients treated with XELJANZ tablets and other Janus kinase inhibitors used to treat inflammatory conditions. In RA patients, a higher rate of malignancies (excluding non-melanoma skin cancer (NMSC)) was observed in patients treated with XELJANZ tablets 5 mg or 10 mg twice a day compared with TNF blockers [see Warnings and Precautions (5.3) ] . Lymphomas and lung cancers were observed at a higher rate in patients treated with XELJANZ tablets 5 mg or 10 mg twice a day in RA patients compared to those treated with TNF blockers.
Patients who are current or past smokers are at additional increased risk. MAJOR ADVERSE CARDIOVASCULAR EVENTS RA patients 50 years of age and older with at least one cardiovascular risk factor, treated with XELJANZ tablets 5 mg or 10 mg twice daily, had a higher rate of major adverse cardiovascular events (MACE) (defined as cardiovascular death, myocardial infarction, and stroke), compared to those treated with TNF blockers. Patients who are current or past smokers are at additional increased risk.
Discontinue tofacitinib oral solution in patients that have experienced a myocardial infarction or stroke [see Warnings and Precautions (5.4) ] . THROMBOSIS Thrombosis, including pulmonary embolism, deep venous thrombosis, and arterial thrombosis have occurred in patients treated with XELJANZ tablets and other Janus kinase inhibitors used to treat inflammatory conditions. Many of these events were serious and some resulted in death.
RA patients 50 years of age and older with at least one cardiovascular risk factor treated with XELJ…
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Tofacitinib oral solution is a Janus kinase (JAK) inhibitor. Tofacitinib oral solution is indicated for the treatment of pediatric patients 2 years of age and older with: Active psoriatic arthritis ( PsA), who have had an inadequate response or intolerance to one or more TNF blockers. Active polyarticular course juvenile idiopathic arthritis (pcJIA), who have had an inadequate response or intolerance to one or more TNF blockers.
Limitations of Use : Use of tofacitinib oral solution for PsA, or pcJIA in combination with biologic DMARDs or potent immunosuppressants such as azathioprine and cyclosporine is not recommended. ( 1.2 , 1.4 )
1.2Psoriatic Arthritis Tofacitinib oral solution is indicated for the treatment of pediatric patients 2 years of age and older with active psoriatic arthritis (PsA), who have had an inadequate response or intolerance to one or more TNF blockers. Limitations of Use Use of tofacitinib oral solution in combination with biologic DMARDs or with potent immunosuppressants such as azathioprine and cyclosporine is not recommended.
1.4Polyarticular Course Juvenile Idiopathic Arthritis Tofacitinib oral solution is indicated for the treatment of pediatric patients 2 years of age and older with of active polyarticular course juvenile idiopathic arthritis (pcJIA), who have had an inadequate response or intolerance to one or more TNF blockers. Limitations of Use Use of tofacitinib oral solution in combination with biologic DMARDs or with potent immunosuppressants such as azathioprine and cyclosporine is not recommended.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Recommended Evaluations and Immunization Prior to Treatment Initiation Prior to initiating tofacitinib oral solution, consider performing an active and latent TB evaluation, viral hepatitis screening, a complete blood count, and updating immunizations. Avoid tofacitinib oral solution initiation 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 ) Important Administration Instructions XELJANZ XR (extended-release tablets) is not substitutable with tofacitinib oral solution.
( 2.2 ) Switching between tofacitinib oral solution and XELJANZ XR should be made by the healthcare provider. ( 2.2 ) Recommended Dosage Pediatric Patients 2 Years of Age and Older with PsA or pcJIA Who Weigh At Least 10 kg Tofacitinib oral solution 5 mg twice daily for those ≥ 40 kg or weight-based equivalent twice daily for those < 40 kg. ( 2.4 ) Dosage in Patients with Renal Impairment or Hepatic Impairment Use of tofacitinib oral solution in patients with severe HI is not recommended.
( 2.4 , 8.7 ) See full prescribing information (FPI) for recommended dosage in patients with moderate or severe RI or moderate HI. ( 2.4 , 8.6 , 8.7 ) Dosage Modification See the full prescribing information for dosage modification by indication for patients who concomitantly use CYP2C19 and/or CYP3A4 inhibitors and patients with lymphopenia, neutropenia, or anemia. ( 2.4 , 7 )
2.1Recommended Evaluations and Immunization Prior to Treatment Initiation Prior to initiating tofacitinib oral solution, consider performing the following: Active and latent tuberculosis (TB) infection evaluation: If the patient has latent TB, treat for TB prior to tofacitinib treatment [see Warnings and Precautions (5.1) ]. Viral hepatitis screening in accordance with clinical guidelines [see Warnings and Precautions (5.1) ]. A complete blood count: Avoid initiation of tofacitinib treatment in patients with a lymphocyte count less than 500 cells/mm 3 , absolute neutrophil count less than 1,000 cells/mm 3 , or hemoglobin level less than 9 g/dL [see Warnings and Precautions (5.9) ].
Baseline hepatic function evaluation: tofacitinib is not recommended for patients with severe hepatic impairment [see Use in Specific Populations (8.7) and Clinical Pharmacology (12.3) ]. Update immunizations according to current immunization guidelines. The interval between live vaccinations and initiation of tofacitinib should be in accordance with current vaccination guidelines regarding immunosuppressive agents [see Warnings and Precautions (5.10) ].
2.2Important Administration Instructions XELJANZ XR (extended-release tablets) is not substitutable with tofacitinib oral solution. Switching between tofacitinib oral solution and XELJANZ XR should be made by the healthcare provider. Dose interruption is recommended for management of lymphopenia, neutropenia, and anemia [see Warnings and Precautions (5.9) and Adverse Reactions (6.1) ] .
Interrupt use of tofacitinib if a patient develops a serious infection until the infection is controlled [see Warnings and Precautions (5.1) ] . Take tofacitinib oral solution with or without food [see Clinical Pharmacology (12.3) ] .
2.4Recommended Dosage in Pediatric Patients 2 Years of Age and Older with Psoriatic Arthritis or Polyarticular Course Juvenile Idiopathic Arthritis Table 2 displays the recommended body weight-based dosages for XELJANZ tablets and tofacitinib oral solution in pediatric patients 2 years of age and older with PsA or pcJIA [see Indication and Usage (1.2 , 1.4) ] with and without renal impairment (including those who are undergoing hemodialysis) or hepatic impairment [see Use in Specific Populations (8.6 , 8.7) ]. The table also includes recommended dosage modification for pediatric patients concomitantly using CYP2C19 and/or CYP3A4 inhibitors [see Drug Interactions (7) and Clinical Pharmacology (12.3) ] , and pediatric patients with lymphopenia, neutrop…
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Tofacitinib oral solution: 1 mg/mL of tofacitinib: Clear, colorless oral solution. Tofacitinib oral solution: 1 mg/mL ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS None. None. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Serious Infections : Avoid use of tofacitinib oral solution during an active serious infection, including localized infections. ( 5.1 ) Gastrointestinal Perforations : Promptly evaluate patients at increased risk for gastrointestinal perforation who present with new onset abdominal symptoms. ( 5.6 ) Hypoglycemia in Patients with Diabetes : Consider increased monitoring of blood glucose; advise patients with diabetes to notify their healthcare provider if they develop signs or symptoms of hypoglycemia.
(5.8) Laboratory Monitoring : Recommended due to potential changes in lymphocytes, neutrophils, hemoglobin, liver enzymes and lipids. ( 5. 9) Vaccinations : Avoid use of live vaccines concurrently with tofacitinib.
( 5. 10)
5.1Serious Infections Serious and sometimes fatal infections may occur with tofacitinib oral solution. 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, urinary tract infection, cellulitis, herpes zoster, bronchitis, septic shock, diverticulitis, gastroenteritis, appendicitis, and sepsis.
Among opportunistic infections, tuberculosis and other mycobacterial infections, cryptococcosis, histoplasmosis, esophageal candidiasis, pneumocystosis, multi−dermatomal 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 oral solution in patients with an active, serious infection, including localized infections. The risks and benefits of treatment should be considered prior to initiating tofacitinib oral solution in patients: with chronic or recurrent infection who have been exposed to tuberculosis with a history of a serious or an opportunistic infection who have resided or traveled in areas of endemic tuberculosis or endemic mycoses; or with underlying conditions that may predispose them to infection. Closely monitor patients for the development of signs and symptoms of infection during and after treatment with tofacitinib oral solution.
Interrupt tofacitinib oral solution if a patient develops a serious infection, an opportunistic infection, or sepsis. In patients who develop a new infection during treatment with tofacitinib oral solution, promptly complete diagnostic testing appropriate for an immunocompromised patient; initiate appropriate antimicrobial therapy, and monitor the patients closely. Caution is also recommended in patients with a history of chronic lung disease, or in those who develop interstitial lung disease, as they may be more prone to infections.
Risk of infection may be higher with increasing degrees of lymphopenia and consideration should be given to lymphocyte counts when assessing individual patient risk of infection. Discontinuation and monitoring criteria for lymphopenia are recommended [see Dosage and Administration (2.4) ]. Tuberculosis Evaluate and test patients for latent or active tuberculosis (TB) infection prior to and per applicable guidelines during administration of tofacitinib oral solution.
Consider anti-TB therapy prior to administration of tofacitinib oral solution in patients with a past history of latent or active TB in whom an adequate course of treatment cannot be confirmed, and for patients with a negative test for latent TB but who have risk factors for TB infection. Consultation with a physician with expertise in the treatment of TB is recommended to aid in the decision about whether initiating anti-TB therapy is appropriate for an individual patient. Monitor patients close…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Serious Infections [see Warnings and Precautions (5.1) ] Increased Risk of 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 Reactions [see Warnings and Precautions (5.7) ] Hypoglycemia in Patients with Diabetes [see Warnings and Precautions (5.8)] Laboratory Abnormalities [see Warnings and Precautions (5.9) ] Most common adverse reactions are: PsA: Reported in ≥2% of adult patients treated with XELJANZ tablets monotherapy or in combination with DMARDs: upper respiratory tract infection (URI), nasopharyngitis, diarrhea, and headache.
( 6.1 ) PcJIA : Consistent with common adverse reactions reported in adult patients with RA. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Sun Pharmaceutical Industries, Inc., at 1-800-818-4555 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical 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 tablets” in this subsection of labeling) and/or tofacitinib oral solution.
Adverse Reactions in Adults with Rheumatoid Arthritis In RA Safety Study 1, 1,455 adults were treated with XELJANZ tablets 5 mg twice daily, 1,456 adults were treated with 10 mg twice daily, and 1,451 adults were treated with a TNF blocker for a median of 4 years [see Clinical Studies (14.6) ] . The safety of XELJANZ tablets was also evaluated in two Phase 2 and five Phase 3 double-blind, placebo-controlled, multicenter trials in patients with RA. In these trials, adults were randomized to receive: XELJANZ tablets (monotherapy) 5 mg twice daily (292 patients) or 10 mg twice daily (306 patients), In combination with DMARDs (including methotrexate), XELJANZ tablets 5 mg twice daily (1,044 patients) or 10 mg twice daily (1,043 patients and Placebo (809 patients).
All seven trials included provisions for patients taking placebo to receive treatment with XELJANZ tablets at Month 3 or Month 6 either by patient response (based on uncontrolled disease activity) or by design, so that adverse events cannot always be unambiguously attributed to a given treatment. Therefore, some analyses that follow include patients who changed treatment by design or by patient response from placebo to XELJANZ tablets in both the placebo and XELJANZ tablets group of a given interval. Comparisons between placebo and XELJANZ tablets groups were based on the first 3 months of exposure, and comparisons between XELJANZ tablets 5 mg twice daily and XELJANZ tablets 10 mg twice daily were based on the first 12 months of exposure.
The long-term safety population includes all adults with RA who participated in a double-blind, placebo-controlled trial (including earlier development phase studies) and then participated in one of two long-term safety studies. The design of the long-term safety studies allowed for modification of XELJANZ tablets doses according to clinical judgment. This limits the interpretation of the long-term safety data with respect to dose.
The most common serious adverse reactions were serious infections [see Warnings and Precautions (5.1) ] . The proportion of patients who discontinued treatment due to any adverse reaction during the 0 to 3 months exposure in the double-blind, placebo-controlled trials was 4% for XELJANZ tablets-treated patients and 3%…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Table 7 includes drugs with clinically significant drug interactions when concomitantly used with tofacitinib oral solution and instructions for preventing or managing them. Table 7: Clinically Significant Interactions Affecting Tofacitinib Oral Solution When Concomitantly Used with Other Drugs Strong CYP3A4 Inhibitors (e.g., ketoconazole) Clinical Impact Increased exposure to tofacitinib Intervention Dosage modification of tofacitinib oral solution is recommended [see Dosage and Administration (2) , Clinical Pharmacology , Figure 3 (12.3) ] Moderate CYP3A4 Inhibitors Concomitantly Used with Strong CYP2C19 Inhibitors (e.g., fluconazole) Clinical Impact Increased exposure to tofacitinib Intervention Dosage modification of tofacitinib oral solution is recommended [see Dosage and Administration (2) , Clinical Pharmacology , Figure 3 (12.3) ] Strong CYP3A4 Inducers (e.g., rifampin) Clinical Impact Decreased exposure to tofacitinib and may result in loss of or reduced clinical response Intervention Concomitant use with tofacitinib oral solution is not recommended [see Clinical Pharmacology , Figure 3 (12.3) ] Immunosuppressive Drugs (e.g., azathioprine, tacrolimus, cyclosporine) Clinical Impact Risk of added immunosuppression; concomitant use of tofacitinib oral solution with biologic DMARDs or potent immunosuppressants has not been studied in patients with PsA or pcJIA.
Intervention Concomitant use with tofacitinib oral solution is not recommended [see Indications and Usage (1) , Clinical Pharmacology , Figure 3 (12.3) ] See FPI for clinically significant drug interactions. ( 2 , 7 )
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS Lactation : Advise not to breastfeed. ( 8.2 )
8.1Pregnancy Risk Summary The available data with XELJANZ Tablets/tofacitinib oral solution and XELJANZ XR (extended-release tablets) from a pregnancy exposure registry that enrolled 11 exposed pregnant females, 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 RA 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 dosage of 5 mg twice daily and approximately 36 times the maximum recommended dosage of 10 mg twice daily, respectively (see Data) . The background risks of major birth defects and miscarriage for the indicated populations are unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.
The background risks in the U.S. general population of major birth defects and miscarriages are 2 to 4% and 15 to 20% of clinically recognized pregnancies, respectively. Clinical Considerations Disease-Associated Maternal and/or Embryo/Fetal Risk: Published data suggest that increased disease activity is associated with the risk of developing adverse pregnancy outcomes in women with RA or UC. Adverse pregnancy outcomes include preterm delivery (before 37 weeks of gestation), low birth weight (less than 2,500 grams) infants, and small for gestational age at birth.
Data Animal In a rat embryofetal developmental study, in which pregnant rats received tofacitinib during organogenesis, tofacitinib was teratogenic at exposure levels approximately 146 times the recommended dose of 5 mg twice daily, and approximately 73 times the maximum recommended dose of 10 mg twice daily (on an AUC basis at oral doses of 100 mg/kg/day in rats). Teratogenic effects consisted of external and soft tissue malformations of anasarca and membranous ventricular septal defects, respectively; and skeletal malformations or variations (absent cervical arch; bent femur, fibula, humerus, radius, scapula, tibia, and ulna; sternoschisis; absent rib; misshapen femur; branched rib; fused rib; fused sternebra; and hemicentric thoracic centrum).
In addition, there was an increase in post-implantation loss, consisting of early and late resorptions, resulting in a reduced number of viable fetuses. Mean fetal body weight was reduced. No developmental toxicity was observed in rats at exposure levels approximately 58 times the recommended dose of 5 mg twice daily, and approximately 29 times the maximum recommended dose of 10 mg twice daily (on an AUC basis at oral doses of 30 mg/kg/day in pregnant rats).
In a rabbit embryofetal developmental study in which pregnant rabbits received tofacitinib during the period of organogenesis, tofacitinib was teratogenic at exposure levels approximately 13 times the recommended dose of 5 mg twice daily, and approximately 6.3 times the maximum recommended dose of 10 mg twice daily (on an AUC basis at oral doses of 30 mg/kg/day in rabbits) in the absence of signs of maternal toxicity. Teratogenic effects included thoracogastroschisis, omphalocele, membranous ventricular septal defects, and cranial/skeletal malformations (microstomia, microphthalmia), mid-line and tail defects.
In addition, there was an increase in post-implantation loss associated with late resorptions. No developmental toxicity was observed in rabbits at exposure levels approximately 3 ti…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary The available data with XELJANZ Tablets/tofacitinib oral solution and XELJANZ XR (extended-release tablets) from a pregnancy exposure registry that enrolled 11 exposed pregnant females, 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 RA 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 dosage of 5 mg twice daily and approximately 36 times the maximum recommended dosage of 10 mg twice daily, respectively (see Data) . The background risks of major birth defects and miscarriage for the indicated populations are unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.
The background risks in the U.S. general population of major birth defects and miscarriages are 2 to 4% and 15 to 20% of clinically recognized pregnancies, respectively. Clinical Considerations Disease-Associated Maternal and/or Embryo/Fetal Risk: Published data suggest that increased disease activity is associated with the risk of developing adverse pregnancy outcomes in women with RA or UC. Adverse pregnancy outcomes include preterm delivery (before 37 weeks of gestation), low birth weight (less than 2,500 grams) infants, and small for gestational age at birth.
Data Animal In a rat embryofetal developmental study, in which pregnant rats received tofacitinib during organogenesis, tofacitinib was teratogenic at exposure levels approximately 146 times the recommended dose of 5 mg twice daily, and approximately 73 times the maximum recommended dose of 10 mg twice daily (on an AUC basis at oral doses of 100 mg/kg/day in rats). Teratogenic effects consisted of external and soft tissue malformations of anasarca and membranous ventricular septal defects, respectively; and skeletal malformations or variations (absent cervical arch; bent femur, fibula, humerus, radius, scapula, tibia, and ulna; sternoschisis; absent rib; misshapen femur; branched rib; fused rib; fused sternebra; and hemicentric thoracic centrum).
In addition, there was an increase in post-implantation loss, consisting of early and late resorptions, resulting in a reduced number of viable fetuses. Mean fetal body weight was reduced. No developmental toxicity was observed in rats at exposure levels approximately 58 times the recommended dose of 5 mg twice daily, and approximately 29 times the maximum recommended dose of 10 mg twice daily (on an AUC basis at oral doses of 30 mg/kg/day in pregnant rats).
In a rabbit embryofetal developmental study in which pregnant rabbits received tofacitinib during the period of organogenesis, tofacitinib was teratogenic at exposure levels approximately 13 times the recommended dose of 5 mg twice daily, and approximately 6.3 times the maximum recommended dose of 10 mg twice daily (on an AUC basis at oral doses of 30 mg/kg/day in rabbits) in the absence of signs of maternal toxicity. Teratogenic effects included thoracogastroschisis, omphalocele, membranous ventricular septal defects, and cranial/skeletal malformations (microstomia, microphthalmia), mid-line and tail defects.
In addition, there was an increase in post-implantation loss associated with late resorptions. No developmental toxicity was observed in rabbits at exposure levels approximately 3 times the recommended dose of 5 mg twice daily, and approximately 1.5 times th…
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness of tofacitinib oral solution in pediatric patients for indications, other than in patients with active pcJIA and PsA, have not been established. The safety and effectiveness of tofacitinib oral solution have not been established in pediatric patients less than 2 years of age. Polyarticular Course Juvenile Idiopathic Arthritis (pcJIA) The safety and effectiveness of tofacitinib oral solution for the treatment of active pcJIA have been established in pediatric patients 2 years of age and older who have had an inadequate response or intolerance to one or more TNF blockers.
Use of tofacitinib oral solution for this indication is supported by evidence from adequate and well-controlled studies of XELJANZ tablets in adults with RA, pharmacokinetic (PK) data from adult patients with RA, and with additional safety, efficacy, and PK data from a clinical trial of tofacitinib in pediatric patients 2 years and older with active pcJIA (Study pcJIA-I) [see Adverse Reactions (6.1) , Clinical Pharmacology (12.3) , and Clinical Studies (14.4) ] . Adverse reactions observed in pediatric patients with pcJIA who received tofacitinib were consistent with those reported in adults with RA [see Adverse Reactions (6.1) ] .
Psoriatic Arthritis The safety and effectiveness of tofacitinib oral solution for the treatment of active PsA have been established in pediatric patients 2 years of age and older who have had an inadequate response or intolerance to one or more TNF blockers. Use of tofacitinib for this indication is supported by evidence from well-controlled studies of tofacitinib tablets in adults with PsA, PK data from adults with PsA, and PK data from a clinical trial of tofacitinib in 225 pediatric patients with JIA, and safety data from 280 pediatric patients 2 years of age and older with JIA [see Adverse Reactions (6.1) , Clinical Pharmacology (12.3) , and Clinical Studies (14.2) ].
Following administration of the recommended tofacitinib dosage in pediatric patients 2 years of age and older with PsA, tofacitinib plasma exposures are predicted to be comparable to those observed in adults with PsA based on population PK modeling and simulation [see Clinical Pharmacology (12.3) ]. Systemic Juvenile Idiopathic Arthritis The safety and effectiveness of tofacitinib for the treatment of pediatric patients with systemic juvenile idiopathic arthritis (sJIA) have not been established. Additional pediatric information describing a clinical study in which efficacy was not demonstrated is approved for Pfizer Inc.’s Xeljanz (tofacitinib) oral solution.
However, due to Pfizer Inc.’s marketing exclusivity rights, this drug product is not labeled with that information.
🧓 Geriatric Use ▾
8.5Geriatric Use Of the 3,315 adults who were enrolled in clinical trials with RA, a total of 505 patients were 65 years of age and older, including 71 patients 75 years and older. The frequency of serious infection among XELJANZ tablets-treated patients 65 years of age and older was higher than among those adults under the age of 65. Of the 783 XELJANZ tablet-treated patients in clinical trials of patients with PsA, a total of 72 (9.2%) patients were 65 years of age and older, including 2 (0.3%) patients 75 years and older.
These clinical studies did not include sufficient numbers of patients aged 65 years and older with PsA to determine if they respond differently from younger adult patients.
🆘 Overdosage ▾
10 OVERDOSAGE There is no specific antidote for overdose with tofacitinib 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 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 tofacitinib. Consider contacting the Poison Help line (1-800-222-1222) or a medical toxicologist for additional overdose management recommendations.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action 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. JAK enzymes transmit cytokine signaling through pairing of JAKs (e.g., JAK1/JAK3, JAK1/JAK2, JAK1/TyK2, JAK2/JAK2). Tofacitinib inhibited the in vitro activities of JAK1/JAK2, JAK1/JAK3, and JAK2/JAK2 combinations with IC50 of 406, 56, and 1377 nM, respectively.
However, the relevance of specific JAK combinations to therapeutic effectiveness is not known.
12.2Pharmacodynamics Treatment with tofacitinib was associated with dose-dependent reductions of circulating CD16/56+ natural killer cells, with estimated maximum reductions occurring at approximately 8 to 10 weeks after initiation of therapy. These changes generally resolved within 2 to 6 weeks after discontinuation of treatment. Treatment with tofacitinib was associated with dose-dependent increases in B cell counts.
Changes in circulating T-lymphocyte counts and T-lymphocyte subsets (CD3+, CD4+ and CD8+) were small and inconsistent. The clinical significance of these changes is unknown. Total serum IgG, IgM, and IgA levels after 6-month dosing in patients with rheumatoid arthritis (RA) were lower than in patients who received placebo; however, changes were small and not dose-dependent.
After treatment with tofacitinib in patients with RA, rapid decreases in serum C-reactive protein (CRP) were observed and maintained throughout dosing. Changes in CRP observed with tofacitinib treatment do not reverse fully within 2 weeks after discontinuation, indicating a longer duration of pharmacodynamic activity compared to the pharmacokinetic half-life. Similar changes in T cells, B cells, and serum CRP have been observed in patients with active psoriatic arthritis (PsA) although reversibility was not assessed.
Total serum immunoglobulins were not assessed in patients with active PsA.
12.3Pharmacokinetics Following oral administration of XELJANZ tablets and tofacitinib oral solution, peak plasma concentrations were reached within 0.5 hour to 1 hour, elimination half-life was about 3 hours and a dose-proportional increase in systemic exposure was observed in the therapeutic dosage range. Steady state concentrations were achieved in 24 to 48 hours with negligible accumulation after twice daily administration. Absorption Tofacitinib The absolute oral bioavailability of tofacitinib is 74%.
Coadministration of tofacitinib with a high-fat meal resulted in no changes in AUC while C max was reduced by 32%. In clinical trials, tofacitinib was administered without regard to meals [see Dosage and Administration (2.2) ] . Distribution After intravenous administration, the volume of distribution was 87 L.
The protein binding of tofacitinib is approximately 40%. Tofacitinib binds predominantly to albumin and does not appear to bind to a1-acid glycoprotein. Tofacitinib distributes equally between red blood cells and plasma.
Metabolism and Excretion Clearance mechanisms for tofacitinib are approximately 70% hepatic metabolism and 30% renal excretion of the parent drug. The metabolism of tofacitinib is primarily mediated by CYP3A4 with minor contribution from CYP2C19. In a human radiolabeled study, more than 65% of the total circulating radioactivity was accounted for by unchanged tofacitinib, with the remaining 35% attributed to 8 metabolites, each accounting for less than 8% of total radioactivity.
The pharmacologic activity of tofacitinib is attributed to the parent molecule. Pharmacokinet…
🧬 Mechanism of Action ▾
12.1Mechanism of Action 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. JAK enzymes transmit cytokine signaling through pairing of JAKs (e.g., JAK1/JAK3, JAK1/JAK2, JAK1/TyK2, JAK2/JAK2). Tofacitinib inhibited the in vitro activities of JAK1/JAK2, JAK1/JAK3, and JAK2/JAK2 combinations with IC50 of 406, 56, and 1377 nM, respectively.
However, the relevance of specific JAK combinations to therapeutic effectiveness is not known.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING How supplied information for tofacitinib oral solution is shown in Table 23. Table 23: How Supplied Information for Tofacitinib Oral Solution Bottle Fill Volume (mL) NDC Number Tofacitinib oral solution 1 mg/mL Clear, colorless solution 240 mL NDC 70095-008-02 Tofacitinib oral solution Tofacitinib oral solution 1 mg/ mL is a clear, colorless solution that contains 1 mg of tofacitinib. It is packaged in HDPE bottles as follows: Each bottle is packaged with 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. Store at 20º to 25ºC (68º to 77ºF); excursions permitted to 15° to 30°C (59° to 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.
📋 Description ▾
11 DESCRIPTION Tofacitinib oral solution is 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-yl)amino)-ß-oxo-1-piperidinepropanenitrile, 2-hydroxy-1,2,3-propanetricarboxylate (1:1). The solubility of tofacitinib citrate in water is 2.38 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 16 H 20 N 6 O•C 6 H 8 O 7 . The chemical structure of tofacitinib citrate is: Tofacitinib oral solution is supplied for oral administration as a 1 mg/mL clear, colorless solution. Each 1 mL of tofacitinib oral solution contains 1 mg of tofacitinib (equivalent to 1.62 mg of tofacitinib citrate) and the following inactive ingredients: grape flavor (natural), hydrochloric acid, L-lactic acid, purified water, sodium benzoate, sodium hydroxide, sucralose, and xylitol.
Grape flavor (natural) contains propylene glycol and natural flavor. chem stru
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise patients to read the FDA-approved patient labeling ( Medication Guide and Instructions for Use ). Serious Infections Inform patients that tofacitinib oral solution may lower the ability of their immune system to fight infections. Advise patients not to start taking tofacitinib if they have an active infection.
Instruct patients to contact their healthcare provider immediately during treatment if symptoms suggesting infection appear to ensure rapid evaluation and appropriate treatment [see Warnings and Precautions (5.1) ] . Advise patients that the risk of herpes zoster, some cases of which can be serious, is increased in patients treated with tofacitinib [see Warnings and Precautions (5.1) ] . Malignancies and Lymphoproliferative Disorders Inform patients that tofacitinib may increase their risk of certain cancers, and that lymphoma and other cancers have been observed in patients taking tofacitinib.
Instruct patients to inform their healthcare provider if they have ever had any type of cancer [see Warnings and Precautions (5.3) ] . Major Adverse Cardiovascular Events Inform patients that tofacitinib may increase their risk of major adverse cardiovascular events (MACE) defined as myocardial infarction, stroke, and cardiovascular death. Instruct all patients, especially current or past smokers or patients with other cardiovascular risk factors, to be alert for the development of signs and symptoms of cardiovascular events [see Warnings and Precautions (5.4) ] .
Thrombosis Advise patients to stop taking tofacitinib and to call their healthcare provider right away if they experience any symptoms of thrombosis (sudden shortness of breath, chest pain worsened with breathing, swelling of leg or arm, leg pain or tenderness, red or discolored skin in the affected leg or arm) [see Warnings and Precautions (5.5) ] . Hypersensitivity Advise patients to stop taking tofacitinib and to call their healthcare provider right away if they experience any symptoms of allergic reactions while taking tofacitinib [see Warnings and Precautions (5.7) ] .
Hypoglycemia in Patients with Diabetes Consider advising patients with diabetes to increase monitoring of blood glucose since hypoglycemia, including severe hypoglycemia, has been reported after starting tofacitinib. Advise patients with diabetes to notify their healthcare provider if they develop signs or symptoms of hypoglycemia [see Warnings and Precautions (5.8)] . Important Information on Laboratory Abnormalities Inform patients that tofacitinib may affect certain lab test results, and that blood tests are required before and during tofacitinib treatment [see Warnings and Precautions (5.9) ] .
Pregnancy Advise pregnant females and females of reproductive potential of the potential risk to a fetus. Advise females to inform their prescriber of a known or suspected pregnancy [see Use in Specific Populations (8.1) ]. Lactation Advise women not to breastfeed during treatment with tofacitinib and for at least 18 hours after the last dose of tofacitinib [see Use in Specific Populations (8.2) ].
Infertility Advise females of reproductive potential that tofacitinib may impair fertility [see Use in Specific Populations (8.3) , Nonclinical Toxicology (13.1) ] . It is not known if this effect is reversible. Manufactured by: Ohm Laboratories Inc.
New Brunswick, NJ 08901 Distributed by: Sun Pharmaceutical Industries, Inc. Cranbury, NJ 08512 All trademarks are the property of their respective owners. XELJANZ/XELJANZ XR is a registered trademark of Pfizer Inc.
Revised: 07/2026
💬 Medication Guide ▾
Medication Guide MEDICATION GUIDE Tofacitinib (toe-fa-sye-ti-nib) Oral Solution What is the most important information I should know about tofacitinib oral solution? Tofacitinib oral solution may cause serious side effects including: 1. Serious infections.
Tofacitinib oral solution is a medicine that affect your immune system. Tofacitinib oral solution can lower the ability of your immune system to fight infections. Some people can have serious infections while taking tofacitinib oral solution, including tuberculosis (TB), and infections caused by bacteria, fungi, or viruses that can spread throughout the body.
Some people have died from these infections. Your healthcare provider should test you for TB before starting tofacitinib oral solution and during treatment. Your healthcare provider should monitor you closely for signs and symptoms of TB infection during treatment with tofacitinib oral solution.
You should not start taking tofacitinib oral solution if you have any kind of infection unless your healthcare provider tells you it is okay. You may be at a higher risk of developing shingles (herpes zoster). Before starting tofacitinib oral solution, tell your healthcare provider if you: think you have an infection or have symptoms of an infection such as: fever, sweating, or chills muscle aches cough shortness of breath blood in phlegm weight loss warm, red, or painful skin or sores on your body diarrhea or stomach pain burning when you urinate or urinating feeling very tired more often than normal are being treated for an infection. get a lot of infections or have infections that keep coming back. have diabetes, chronic lung disease, HIV, or a weak immune system.
People with these conditions have a higher chance for infections. have TB, or have been in close contact with someone with TB. live or have lived, or have traveled to certain parts of the country (such as the Ohio and Mississippi River valleys and the Southwest) where there is an increased chance for getting certain kinds of fungal infections (histoplasmosis, coccidioidomycosis, or blastomycosis). These infections may happen or become more severe if you take tofacitinib oral solution. Ask your healthcare provider if you do not know if you have lived in an area where these infections are common. have or have had hepatitis B or C.
After starting tofacitinib oral solution, call your healthcare provider right away if you have any symptoms of an infection. Tofacitinib oral solution can make you more likely to get infections or make worse any infection that you have. 2.
Increased risk of death in people 50 years of age and older who have at least 1 heart disease (cardiovascular) risk factor and are taking XELJANZ 5 mg or 10 mg twice daily. 3. Cancer and immune system problems.
Tofacitinib oral solution may increase your risk of certain cancers by changing the way your immune system works. Lymphoma and other cancers including skin cancers can happen in people taking tofacitinib oral solution. People taking XELJANZ 5 mg twice daily or XELJANZ 10 mg twice daily have a higher risk of certain cancers including lymphoma and lung cancer, especially if you are a current or past smoker.
Tell your healthcare provider if you have ever had any type of cancer. 4. Increased risk of major cardiovascular events such as heart attack, stroke or death in people 50 years of age and older who have at least 1 heart disease (cardiovascular) risk factor and are taking XELJANZ 5 mg or 10 mg twice daily, especially if you are a current or past smoker .
Get emergency help right away if you have any symptoms of a heart attack or stroke while taking tofacitinib oral solution, including: discomfort in the center of your chest that lasts for more than a few minutes, or that goes away and comes back severe tightness, pain, pressure, or heaviness in your chest, throat, neck, or jaw pain or discomfort in your arms, back, neck, jaw, or stomach shortness of breath with or without chest discomfort breaking o…