Tofacitinib

Serious warning

The strongest warning the FDA requires. It is printed in a box at the top of the label.

Quoted from the official label, section “Boxed Warning”.

Do not take it if

Quoted from the official label, section “Contraindications”.

How to take it

These directions are for this exact strength and form. Another one is different.

• Recommended Evaluations and Immunization Prior to Treatment Initiation' Prior to initiating tofacitinib tablets, consider performing an active and latent TB evaluation, viral hepatitis screening, a complete blood count, and updating immunizations.
• Avoid tofacitinib tablets initiation if absolute lymphocyte count <500 cells/mm 3 , an absolute neutrophil count (ANC) <1000 cells/mm 3 or hemoglobin <9 g/dL.
• (2.1) Important Administration Instructions XELJANZ XR (extended-release tablets) is not substitutable with tofacitinib tablets.
• (2.2) Switching between tofacitinib tablets and XELJANZ XR should be made by the healthcare provider.
• (2.2) Recommended Dosage Adult Patients with RA, PsA or AS Tofacitinib tablets 5 mg twice daily.
• (2.3) Pediatric Patients 2 Years of Age and Older with PsA or pcJIA Who Weigh At Least 10 kg Tofacitinib tablets 5 mg twice daily for those ≥40 kg or weight-based equivalent twice daily for those <40 kg.
• (2.4) Adult Patients with UC Induction:
• Tofacitinib tablets 10 mg twice daily for 8 weeks; evaluate patients and transition to maintenance therapy depending on therapeutic response.
• If needed, continue tofacitinib tablets 10 mg twice daily for a maximum of 16 weeks.
• Discontinue tofacitinib tablets 10 mg twice daily after 16 weeks if adequate therapeutic response is not achieved.
• (2.5) Maintenance: Tofacitinib tablets 5 mg twice daily.
• For patients with loss of response during maintenance treatment, tofacitinib tablets 10 mg twice daily may be considered and limited to the shortest duration, with careful consideration of the benefits and risks for the individual patient.
• Use the lowest effective dose needed to maintain response.
• (2.5) Dosage in Patients with Renal Impairment or Hepatic Impairment Use of tofacitinib tablets in patients with severe HI is not recommended.
• (2.3, 2.4, 2.5, 8.7) See full prescribing information (FPI) for recommended dosage in patients with moderate or severe RI or moderate HI.
• (2.3, 2.4, 2.5, 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.
• (2.3, 2.4, 2.5, 7)
• 2.1 Recommended Evaluations and Immunization Prior to Treatment Initiation Prior to initiating tofacitinib tablets, consider performing the following:
• Active and latent tuberculosis (TB) infection evaluation:
• If the patient has latent TB, treat for TB prior to tofacitinib tablets 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 tablets treatment in patients with a lymphocyte count less than 500 cells/mm 3 , absolute neutrophil count less than 1000 cells/mm 3 , or hemoglobin level less than 9 g/dL [see Warnings and Precautions (5.8)].
• Baseline hepatic function evaluation:
• Tofacitinib tablets are 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 tablets should be in accordance with current vaccination guidelines regarding immunosuppressive agents [see Warnings and Precautions (5.9)].
• 2.2 Important Administration Instructions XELJANZ XR (extended-release tablets) is not substitutable with tofacitinib tablets.
• Switching between tofacitinib tablets 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 (5.8) and Adverse Reactions (6.1)] .
• Interrupt use of tofacitinib tablets if a patient develops a serious infection until the infection is controlled [see Warnings and Precautions (5.1)] .
• Take tofacitinib tablets with or without food [see Clinical Pharmacology (12.3)] .
• Recommended Dosage in
• Adults with Rheumatoid Arthritis, Psoriatic Arthritis, and Ankylosing Spondylitis Table 1 displays the recommended dosage of tofacitinib tablets for
• adults with RA, PsA, and AS [see Indication and Usage (1.1, 1.2, 1.3)] 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 displays the recommended dosage modifications for patients concomitantly using CYP2C19 and/or CYP3A4 inhibitors [see Drug Interactions (7) and Clinical Pharmacology (12.3)], and patients with lymphopenia, neutropenia, or anemia.
• Table 1:
• Recommended Dosage of Tofacitinib Tablets in
• Adults with Rheumatoid Arthritis, Psoriatic Arthritis, or Ankylosing Spondylitis
• Adults Tofacitinib Tablets Patients with Normal Renal and Hepatic Function a 5 mg twice daily Recommended Dosage in Patients with Renal Impairment (RI) b Mild RI (CLcr >50 and ≤80 mL/min) 5 mg twice daily Moderate RI (CLcr ≥30 and ≤50 mL/min) 5 mg once daily Severe RI (CLcr <30 mL/min) 5 mg once daily For patients undergoing hemodialysis, administer the dose after the dialysis session on dialysis days.
• If a dose was taken before the dialysis procedure, supplemental doses are not recommended after dialysis.
• Recommended Dosage in Patients with Hepatic Impairment (HI) Mild HI (Child-Pugh A) 5 mg twice daily Moderate HI (Child-Pugh B) 5 mg once daily Severe HI (Child-Pugh C) Use of tofacitinib tablets is not recommended.
• Dosage Modifications with Concomitant Use of CYP3A4 and/or CYP2C19 Inhibitor(s) Strong CYP2C19 inhibitor(s) 5 mg twice daily Moderate CYP2C19 inhibitor(s) Moderate CYP3A4 inhibitor(s) Moderate CYP3A4 inhibitor(s) with strong CYP2C19 inhibitor(s) (e.g., fluconazole) 5 mg once daily Strong CYP3A4 inhibitor(s) Dosage Modifications for Lymphopenia, Neutropenia, or Anemia Patients with lymphocyte count less than 500 cells/mm 3 , confirmed by repeat testing Discontinue dosing.
• Patients with ANC less than 500 cells/mm 3 Discontinue dosing.
• Patients with ANC 500 to 1000 cells/mm 3 Interrupt dosing.
• When ANC is greater than 1000, resume 5 mg twice daily.
• Patients with hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL Interrupt dosing until hemoglobin values have normalized. a Excludes patients who concomitantly use tofacitinib tablets with strong CYP3A4 inhibitor(s) or moderate CYP3A4 inhibitor(s) and strong CYP2C19 inhibitor(s), as well as patients with lymphocyte count less than 500 cells/mm 3 , ANC <1000 cells/mm 3 , or hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL. b Tofacitinib PK was evaluated in subjects with varying degrees of renal impairment, where the severity of renal impairment was defined based on creatinine clearance (CLcr) estimated using the Cockcroft-Gault equation:
• CLcr >80 mL/min (normal renal function); >50 and ≤80 mL/min (mild renal impairment); ≥30 and ≤50 mL/min (moderate renal impairment); <30 mL/min (severe renal impairment).
• Switching from Tofacitinib Tablets to XELJANZ XR Extended-Release Tablets Patients treated with tofacitinib tablets 5 mg twice daily may be switched to XELJANZ XR extended-release tablets 11 mg once daily the day following the last dose of tofacitinib tablets 5 mg.
• 2.4 Recommended 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 tofacitinib tablets 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, neutropenia, or anemia.
• Table 2:
• Recommended Dosage of Tofacitinib Tablets in Pediatric Patients 2 Years of Age and Older with PsA or pcJIA Pediatric Patients 2 Years of Age and Older Tofacitinib tablets Patients with Normal Renal and Hepatic Function a Body weight ≥40 kg:
• 5 mg (one 5 mg tablet or 5 mL oral solution) twice daily b Recommended Dosage in Patients with Renal Impairment (RI) Mild RI Same as patients with normal renal function.
• Moderate RI Body weight ≥40 kg:
• 5 mg once daily b Severe RI Body weight ≥40 kg:
• 5 mg once daily b For patients undergoing hemodialysis, administer the dose after the dialysis session on dialysis days.
• If a dose was taken before the dialysis procedure, supplemental doses are not recommended after dialysis.
• Recommended Dosage in Patients with Hepatic Impairment (HI) Mild HI Same as patients with normal hepatic function.
• Moderate HI Body weight ≥40 kg:
• 5 mg once daily b Severe HI Use of tofacitinib tablets is not recommended.
• Dosage Modifications with Concomitant Use of CYP3A4 and/or CYP2C19 Inhibitor(s) Strong CYP2C19 inhibitor(s) No dosage modification is recommended.
• Moderate CYP2C19 inhibitor(s) Moderate CYP3A4 inhibitor(s) Moderate CYP3A4 inhibitor(s) with strong CYP2C19 inhibitor(s) (e.g., fluconazole) Body weight ≥40 kg:
• 5 mg once daily b Strong CYP3A4 inhibitor(s) Dosage Modifications for Lymphopenia, Neutropenia, or Anemia Patients with lymphocyte count less than 500 cells/mm 3 , confirmed by repeat testing Discontinue dosing.
• Patients with ANC less than 500 cells/mm 3 Discontinue dosing.
• Patients with ANC 500 to 1000 cells/mm 3 Interrupt dosing until ANC is greater than 1000 cells/mm 3 .
• Patients with hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL Interrupt dosing until hemoglobin values have normalized. a Excludes patients who concomitantly use tofacitinib tablets with strong CYP3A4 inhibitor(s) or moderate CYP3A4 inhibitor(s) and strong CYP2C19 inhibitor(s), as well as patients with lymphocyte count less than 500 cells/mm 3 , ANC <1000 cells/mm 3 , or hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL. b Patients treated with XELJANZ oral solution 5 mL may be switched to tofacitinib tablets 5 mg.
• Recommended Dosage in
• Adults with Ulcerative Colitis Table 3 displays the recommended dosage of tofacitinib tablets in adult patients with ulcerative colitis (UC) [see Indications and Usage (1.5)] with and without renal impairment (including those who are undergoing hemodialysis) or hepatic impairment [see Use in Specific Populations (8.6, 8.7)].
• Table 4 displays the recommended dosage modification for patients concomitantly using CYP2C19 and/or CYP3A4 inhibitors [see Drug Interactions (7) and Clinical Pharmacology (12.3)] , and patients with lymphopenia, neutropenia, or anemia.
• Table 3:
• Recommended Dosage of Tofacitinib Tablets in
• Adults with Ulcerative Colitis With and Without Renal Impairment or Hepatic Impairment
• Adults Tofacitinib Tablets Patients with Normal Renal and Hepatic Function a Induction:
• 10 mg twice daily for at least 8 weeks [see Clinical Studies (14.5)] ; evaluate patients and transition to maintenance therapy depending on therapeutic response.
• If needed continue 10 mg twice daily for a maximum of 16 weeks.
• Discontinue 10 mg twice daily after 16 weeks if adequate therapeutic response is not achieved.
• Maintenance: 5 mg twice daily.
• For patients with loss of response during maintenance treatment, may consider a dosage of 10 mg twice daily (limited to the shortest duration), with careful consideration of the benefits and risks for the individual patient.
• Use the lowest effective dosage needed to maintain response .
• Recommended Dosage in Patients with Renal Impairment (RI) b Mild RI (CLcr >50 and ≤80 mL/min) Same as patients with normal renal function.
• Moderate RI (CLcr ≥30 and ≤50 mL/min) Induction:
• 5 mg twice daily for at least 8 weeks [see Clinical Studies (14.5)] ; evaluate patients and transition to maintenance therapy depending on therapeutic response.
• If needed continue 5 mg twice daily for a maximum of 16 weeks.
• Discontinue 5 mg twice daily after 16 weeks if adequate therapeutic response is not achieved.
• Maintenance: 5 mg once daily.
• For patients with loss of response during maintenance treatment, may consider a dosage of 5 mg twice daily (limited to the shortest duration), with careful consideration of the benefits and risks for the individual patient.
• Use the lowest effective dosage needed to maintain response .
• For patients undergoing hemodialysis, administer the dose after the dialysis session on dialysis days.
• If a dose was taken before the dialysis procedure, supplemental doses are not recommended after dialysis.
• Severe RI (CLcr <30 mL/min) Recommended Dosage in Patients with Hepatic Impairment (HI) Mild HI (Child-Pugh A) Same as patients with normal hepatic function.
• Moderate HI (Child-Pugh B) Induction:
• 5 mg twice daily for at least 8 weeks [see Clinical Studies (14.5)] ; evaluate patients and transition to maintenance therapy depending on therapeutic response.
• If needed continue 5 mg twice daily for a maximum of 16 weeks.
• Discontinue 5 mg twice daily after 16 weeks if adequate therapeutic response is not achieved.
• Maintenance: 5 mg once daily.
• For patients with loss of response during maintenance treatment, may consider a dosage of 5 mg twice daily (limited to the shortest duration), with careful consideration of the benefits and risks for the individual patient.
• Use the lowest effective dosage needed to maintain response .
• Severe HI (Child-Pugh C) Use of tofacitinib tablets is not recommended. a Excludes patients who concomitantly use tofacitinib tablets with strong CYP3A4 inhibitor(s) or moderate CYP3A4 inhibitor(s) and strong CYP2C19 inhibitor(s), as well as patients with lymphocyte count less than 500 cells/mm 3 , ANC <1000 cells/mm 3 , or hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL. b Tofacitinib PK was evaluated in subjects with varying degrees of renal impairment, where the severity of renal impairment was defined based on creatinine clearance (CLcr) estimated using the Cockcroft-Gault equation:
• CLcr >80 mL/min (normal renal function);
• CLcr >50 and ≤80 mL/min (mild renal impairment); ≥30 and ≤50 mL/min (moderate renal impairment); <30 mL/min (severe renal impairment).
• Table 4:
• Dosage Modifications of Tofacitinib Tablets Due to Drug Interactions and for Lymphopenia, Neutropenia or Anemia in
• Adults with Ulcerative Colitis
• Adults Tofacitinib Tablets Dosage Modifications with Concomitant Use of CYP3A4 and/or CYP2C19 Inhibitor(s) Strong CYP2C19 inhibitor(s) Moderate CYP2C19 inhibitor(s) No dosage modification is recommended.
• Moderate CYP3A4 inhibitor(s) Moderate CYP3A4 inhibitor(s) with strong CYP2C19 inhibitor(s) (e.g., fluconazole) Induction:
• 5 mg twice daily for at least 8 weeks [see Clinical Studies (14.5)] ; evaluate patients and transition to maintenance therapy depending on therapeutic response.
• If needed continue 5 mg twice daily for a maximum of 16 weeks.
• Discontinue 5 mg twice daily after 16 weeks if adequate therapeutic response is not achieved.
• Strong CYP3A4 inhibitor(s) Maintenance: 5 mg once daily.
• For patients with loss of response during maintenance treatment, may consider a dosage of 5 mg twice daily (limited to the shortest duration), with careful consideration of the benefits and risks for the individual patient.
• Use the lowest effective dosage needed to maintain response .
• Dosage Modifications for Lymphopenia, Neutropenia, or Anemia Lymphocyte count less than 500 cells/mm 3 , confirmed by repeat testing Discontinue dosing.
• ANC less than 500 cells/mm 3 Discontinue dosing.
• ANC 500 to 1000 cells/mm 3 If taking: 10 mg twice daily, reduce to 5 mg twice daily.
• When ANC is greater than 1000, increase to 10 mg twice daily based on clinical response. 5 mg twice daily, interrupt dosing.
• When ANC is greater than 1000, resume 5 mg twice daily.
• Hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL Interrupt dosing until hemoglobin values have normalized.
• Switching from Tofacitinib Tablets to XELJANZ XR Extended-Release Tablets Patients treated with tofacitinib tablets:
• 5 mg twice daily may be switched to XELJANZ XR extended-release tablets 11 mg once daily the day following the last dose of tofacitinib tablets 5 mg. 10 mg twice daily may be switched to XELJANZ XR extended-release tablets 22 mg once daily the day following the last dose of tofacitinib tablets 10 mg.

Quoted from the official label, section “Dosage & Administration”.

Other warnings

Quoted from the official label, section “Warnings”.

Pregnancy and breastfeeding

Quoted from the official label, section “OTC — Pregnancy or Breast Feeding”.

Other medicines

Quoted from the official label, section “Drug Interactions”.

If you take too much

In an emergency, call your local emergency number or a poison control centre.

Quoted from the official label, section “Overdosage”.

Use in children

• The safety and effectiveness of tofacitinib tablets in pediatric patients for indications, other than in patients with active pcJIA and PsA, have not been established.
• The safety and effectiveness of tofacitinib tablets 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 tablets 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 tablets for this indication is supported by evidence from adequate and well-controlled studies of tofacitinib 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 tablets 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 (14.1, 14.4)] .
• Adverse reactions observed in pediatric patients with pcJIA who received tofacitinib tablets were consistent with those reported in
• adults with RA [see Adverse Reactions (6.1)] .
• Psoriatic Arthritis The safety and effectiveness of tofacitinib tablets 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 tablets 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 tablets 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 tablets 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 tablets for the treatment of pediatric patients with systemic juvenile idiopathic arthritis (sJIA) have not been established.
• The results from a two-part study (an open-label, run-in phase, followed by a double-blind, placebo-controlled, randomized event-driven withdrawal phase) in 100 patients 2 years to 17 years of age with sJIA with active systemic features did not demonstrate that tofacitinib tablets (dosed at 5 mg twice daily or body weight-based equivalent twice daily) was efficacious in the treatment of sJIA with active systemic features.
• Of the 100 patients enrolled in the open-label run-in phase, 59 (59%) patients achieved a clinical response and were eligible for the double-blind withdrawal phase.
• There were 28 patients randomized to tofacitinib tablets and 31 patients to placebo.
• The study data were insufficient to demonstrate efficacy and, therefore, tofacitinib tablets are not recommended for the treatment of sJIA.
• Adverse reactions observed in pediatric patients with sJIA receiving tofacitinib tablets were consistent with those reported in pcJIA and RA patients [see Adverse Reactions (6.1)] .

Quoted from the official label, section “Pediatric Use”.

Use in older people

• Of the 3315
• adults who were enrolled in clinical trials with RA (Studies RA-I to V), 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 tofacitinib tablets-treated patients 65 years of age and older was higher than among those
• adults under the age of 65.
• Of the 1156 tofacitinib tablets-treated patients in clinical trials of patients with UC, a total of 77 patients (7%) were 65 years of age or older.
• Clinical studies of tofacitinib tablets in patients with UC did not include sufficient numbers of patients aged 65 years and older to determine whether they respond differently from younger adult patients.
• Of the 783 tofacitinib 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.
• Of the 420 tofacitinib tablet-treated patients in clinical trials of patients with AS, a total of 12 (2.9%) patients were 65 years of age and older, including 1 (0.2%) patient 75 years and older.
• These clinical studies did not include sufficient numbers of patients aged 65 years and older with AS to determine if they respond differently from younger adult patients.

Quoted from the official label, section “Geriatric Use”.

Side effects

• 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)] Laboratory Abnormalities [see Warnings and Precautions (5.8)] Most common adverse reactions are:
• RA, PsA, and AS :
• Reported in ≥2% of adult patients treated with tofacitinib 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) UC :
• Reported in ≥5% of adult patients treated with tofacitinib tablets and ≥1% greater than reported in patients treated with placebo:
• nasopharyngitis, elevated cholesterol levels, headache, URI, increased blood creatine phosphokinase, rash, diarrhea, and herpes zoster.
• (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Somerset Therapeutics, LLC at 1-800-417-9175 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.
• The clinical studies described in this subsection were conducted using tofacitinib tablets and/or XELJANZ oral solution.
• Adverse Reactions in
• Adults with Rheumatoid Arthritis In RA Safety Study 1, 1,455
• adults were treated with tofacitinib 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)] .
• A dosage of tofacitinib tablets 10 mg twice daily is not recommended for the treatment of RA because of increased risks [see Dosage and Administration (2.3) and Warnings and Precautions (5)].
• For the treatment of
• adults with moderately to severely active RA [see Indications and Usage (1.1)] , the recommended dosage of tofacitinib tablets is 5 mg twice daily.
• The safety of tofacitinib 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:
• Tofacitinib tablets (monotherapy) 5 mg twice daily (292 patients) or 10 mg twice daily (306 patients), In combination with DMARDs (including methotrexate), tofacitinib tablets 5 mg twice daily (1044 patients) or 10 mg twice daily (1043 patients) and Placebo (809 patients).
• All seven trials included provisions for patients taking placebo to receive treatment with tofacitinib 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 tofacitinib tablets in both the placebo and tofacitinib tablets group of a given interval.
• Comparisons between placebo and tofacitinib tablets groups were based on the first 3 months of exposure, and comparisons between tofacitinib tablets 5 mg twice daily and tofacitinib 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 tofacitinib 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 tofacitinib tablets-treated patients and 3% for placebo-treated patients.
• Overall Infections In the seven placebo-controlled trials in patients with RA, during the 0 to 3 months exposure, the overall frequency of infections was 20% and 22% in the tofacitinib tablets 5 mg twice daily and tofacitinib tablets 10 mg twice daily groups, respectively, and 18% in the placebo group.
• The most commonly reported infections with tofacitinib tablets were upper respiratory tract infections, nasopharyngitis, and urinary tract infections (4%, 3%, and 2% of patients, respectively).
• Serious Infections:
• In the seven placebo-controlled trials in patients with RA, during the 0 to 3 months exposure, serious infections were reported in 1 patient (0.5 events per 100 patient-years) who received placebo and 11 patients (1.7 events per 100 patient-years) who received tofacitinib tablets 5 mg or 10 mg twice daily.
• The rate difference between treatment groups (and the corresponding 95% confidence interval) was 1.1 (-0.4, 2.5) events per 100 patient-years for the combined tofacitinib tablets 5 mg twice daily and 10 mg twice daily group minus placebo.
• In the seven placebo-controlled trials, during the 0 to 12 months exposure, serious infections were reported in 34 patients (2.7 events per 100 patient-years) who received tofacitinib tablets 5 mg twice daily and 33 patients (2.7 events per 100 patient-years) who received tofacitinib tablets 10 mg twice daily.
• The rate difference between tofacitinib tablets doses (and the corresponding 95% confidence interval) was -0.1 (-1.3, 1.2) events per 100 patient-years for tofacitinib tablets 10 mg twice daily minus tofacitinib tablets 5 mg twice daily.
• The most common serious infections included pneumonia, cellulitis, herpes zoster, and urinary tract infection [see Warnings and Precautions (5.1)] .
• Tuberculosis:
• In the seven placebo-controlled trials in patients with RA, during the 0 to 3 months exposure, tuberculosis (TB) was not reported in patients who received placebo, tofacitinib tablets 5 mg twice daily, or tofacitinib tablets 10 mg twice daily.
• In the seven placebo-controlled trials, during the 0 to 12 months exposure, TB was reported in 0 patients who received tofacitinib tablets 5 mg twice daily and 6 patients (0.5 events per 100 patient-years) who received tofacitinib tablets 10 mg twice daily.
• The rate difference between tofacitinib tablets doses (and the corresponding 95% confidence interval) was 0.5 (0.1, 0.9) events per 100 patient-years for tofacitinib tablets 10 mg twice daily minus tofacitinib tablets 5 mg twice daily.
• Cases of disseminated TB were also reported.
• The median tofacitinib tablets exposure prior to diagnosis of TB was 10 months (range from 152 to 960 days) [see Warnings and Precautions (5.1)].
• Opportunistic Infections (excluding tuberculosis):
• In the seven placebo-controlled trials in patients with RA, during the 0 to 3 months exposure, opportunistic infections were not reported in patients who received placebo, tofacitinib tablets 5 mg twice daily, or tofacitinib tablets 10 mg twice daily.
• In the seven placebo-controlled trials, during the 0 to 12 months exposure, opportunistic infections were reported in 4 patients (0.3 events per 100 patient-years) who received tofacitinib tablets 5 mg twice daily and 4 patients (0.3 events per 100 patient-years) who received tofacitinib tablets 10 mg twice daily.
• The rate difference between tofacitinib tablets doses (and the corresponding 95% confidence interval) was 0 (-0.5, 0.5) events per 100 patient-years for tofacitinib tablets 10 mg twice daily minus tofacitinib tablets 5 mg twice daily.
• The median tofacitinib tablets exposure prior to diagnosis of an opportunistic infection was 8 months (range from 41 to 698 days) [see Warnings and Precautions (5.1)].
• Malignancies In the seven placebo-controlled trials in patients with RA, during the 0 to 3 months exposure, malignancies excluding NMSC were reported in 0 patients who received placebo and 2 patients (0.3 events per 100 patient-years) who received either tofacitinib tablets 5 mg or 10 mg twice daily.
• The rate difference between treatment groups (and the corresponding 95% confidence interval) was 0.3 (-0.1, 0.7) events per 100 patient-years for the combined tofacitinib tablets 5 mg and 10 mg twice daily group minus placebo.
• In the seven placebo-controlled trials, during the 0 to 12 months exposure, malignancies excluding NMSC were reported in 5 patients (0.4 events per 100 patient-years) who received tofacitinib tablets 5 mg twice daily and 7 patients (0.6 events per 100 patient-years) who received tofacitinib tablets 10 mg twice daily.
• The rate difference between tofacitinib tablets doses (and the corresponding 95% confidence interval) was 0.2 (-0.4, 0.7) events per 100 patient-years for tofacitinib tablets 10 mg twice daily minus tofacitinib tablets 5 mg twice daily.
• One of these malignancies was a case of lymphoma that occurred during the 0-to-12-month period in a patient treated with tofacitinib tablets 10 mg twice daily.
• The most common types of malignancy, including malignancies observed during the long-term extension in tofacitinib tablets-treated patients, were lung and breast cancer, followed by gastric, colorectal, renal cell, prostate cancer, lymphoma, and malignant melanoma [see Warnings and Precautions (5.3)].
• Laboratory Abnormalities Lymphopenia:
• In the placebo-controlled clinical trials in patients with RA, confirmed decreases in absolute lymphocyte counts below 500 cells/mm 3 occurred in 0.04% of patients for the tofacitinib tablets 5 mg twice daily and 10 mg twice daily groups combined during the first 3 months of exposure.
• Confirmed lymphocyte counts less than 500 cells/mm 3 were associated with an increased incidence of treated and serious infections [see Warnings and Precautions (5.8)].
• Neutropenia:
• In the placebo-controlled clinical trials in patients with RA, confirmed decreases in ANC below 1,000 cells/mm 3 occurred in 0.07% of patients for the tofacitinib tablets 5 mg twice daily and 10 mg twice daily groups combined during the first 3 months of exposure.
• There were no confirmed decreases in ANC below 500 cells/mm 3 observed in any treatment group.
• There was no clear relationship between neutropenia and the occurrence of serious infections.
• In the long-term safety population, the pattern and incidence of confirmed decreases in ANC remained consistent with what was seen in the placebo-controlled clinical trials [see Warnings and Precautions (5.8)].
• Liver Enzyme Elevations:
• Confirmed increases in liver enzymes greater than 3 times the upper limit of normal (3x ULN) were observed in patients with RA treated with tofacitinib tablets.
• In patients experiencing liver enzyme elevation, modification of treatment regimen, such as reduction in the dose of concomitant DMARD, interruption of tofacitinib tablets, or reduction in tofacitinib tablets dosage, resulted in decrease or normalization of liver enzymes.
• In the placebo-controlled monotherapy trials (0-3 months), no differences in the incidence of ALT or AST elevations were observed between the placebo, and tofacitinib tablets 5 mg, and 10 mg twice daily groups.
• In the placebo-controlled background DMARD trials (0-3 months), ALT elevations greater than 3x ULN were observed in 1.0%, 1.3% and 1.2% of patients who received placebo, tofacitinib tablets 5 mg, and 10 mg twice daily, respectively.
• In these trials, AST elevations greater than 3x ULN were observed in 0.6%, 0.5% and 0.4% of patients who received placebo, tofacitinib tablets 5 mg, and 10 mg twice daily, respectively.
• One case of drug-induced liver injury was reported in a patient treated with tofacitinib tablets 10 mg twice daily for approximately 2.5 months.
• The patient developed symptomatic elevations of AST and ALT greater than 3x ULN and bilirubin elevations greater than 2x ULN, which required hospitalizations and a liver biopsy.
• Lipid Elevations:
• In the placebo-controlled clinical trials in patients with RA, dose-related elevations in lipid parameters (total cholesterol, LDL cholesterol, HDL cholesterol, triglycerides) were observed at one month of exposure and remained stable thereafter.
• Changes in lipid parameters during the first 3 months of exposure in the placebo-controlled clinical trials are summarized below:
• Mean LDL cholesterol increased by 15% in the tofacitinib tablets 5 mg twice daily arm and 19% in the tofacitinib tablets 10 mg twice daily arm.
• Mean HDL cholesterol increased by 10% in the tofacitinib tablets 5 mg twice daily arm and 12% in the tofacitinib tablets 10 mg twice daily arm.
• Mean LDL/HDL ratios were essentially unchanged in tofacitinib tablets-treated patients.
• In a placebo-controlled clinical trial, elevations in LDL cholesterol and ApoB decreased to pretreatment levels in response to statin therapy.
• In the long-term safety population, elevations in lipid parameters remained consistent with what was seen in the placebo-controlled clinical trials.
• Serum Creatinine Elevations:
• In the placebo-controlled clinical trials in patients with RA, dose-related elevations in serum creatinine were observed with tofacitinib tablets treatment.
• The mean increase in serum creatinine was <0.1 mg/dL in the 12-month pooled safety analysis; however, with increasing duration of exposure in the long-term extensions, up to 2% of patients were discontinued from tofacitinib tablets treatment due to the protocol-specified discontinuation criterion of an increase in creatinine by more than 50% of baseline.
• The clinical significance of the observed serum creatinine elevations is unknown.
• Common Adverse Reactions Table 5 displays adverse reactions that occurred in 2% or more of patients on tofacitinib tablets 5 mg or 10 mg twice daily and at least 1% greater than in tofacitinib tablets-treated patients that observed in placebo-treated patients with or without DMARD in the RA trials.
• Table 5:
• Common Adverse Reactions* in Clinical Trials of Tofacitinib Tablets for the Treatment of Rheumatoid Arthritis in
• Adults With or Without Concomitant DMARDs (0-3 Months) Preferred Term Placebo Tofacitinib Tablets 5 mg Twice Daily Tofacitinib Tablets 10 mg Twice Daily** N = 809 (%) N = 1336 (%) N = 1349 (%) Upper respiratory tract infection 3 4 4 Nasopharyngitis 3 4 3 Diarrhea 2 4 3 Headache 2 4 3 Hypertension 1 2 2 N reflects randomized and treated patients from the seven placebo-controlled clinical trials. * reported in ≥2% of patients treated with either dose of tofacitinib tablets and ≥1% greater than that reported for placebo. ** The recommended dose of tofacitinib tablets for the treatment of RA is 5 mg twice daily [see Dosage and Administration (2)] .
• Other adverse reactions that occurred in placebo-controlled and open-label extension studies in patients with RA included:
• Blood and lymphatic system disorders:
• Anemia Infections and infestations:
• Diverticulitis Metabolism and nutrition disorders:
• Dehydration Psychiatric disorders:
• Insomnia Nervous system disorders:
• Paresthesia Respiratory, thoracic and mediastinal disorders:
• Dyspnea, cough, sinus congestion, interstitial lung disease (cases were limited to patients with RA and some were fatal) Gastrointestinal disorders:
• Abdominal pain, dyspepsia, vomiting, gastritis, nausea Hepatobiliary disorders:
• Hepatic steatosis Skin and subcutaneous tissue disorders:
• Rash, erythema, pruritus Musculoskeletal, connective tissue and bone disorders:
• Musculoskeletal pain, arthralgia, tendonitis, joint swelling Neoplasms benign, malignant and unspecified (including cysts and polyps):
• Non-melanoma skin cancers General disorders and administration site conditions:
• Pyrexia, fatigue, peripheral edema Clinical Experience in Methotrexate-Naïve Patients Study RA-VI was an active-controlled clinical trial in methotrexate-naïve patients [see Clinical Studies (14)] .
• The safety experience in these patients was consistent with Studies RA-I through V.
• Adverse Reactions in
• Adults with Psoriatic Arthritis The safety of tofacitinib tablets was evaluated in 2 double-blind Phase 3 clinical trials in
• adults with active psoriatic arthritis (PsA):
• Study PsA-I (NCT01877668) had a duration of 12 months and enrolled
• adults who had an inadequate response to a nonbiologic DMARD and who were naïve to treatment with a TNF blocker.
• Study PsA-I included a 3-month placebo-controlled period and also included adalimumab 40 mg subcutaneously once every 2 weeks for 12 months.
• Study PsA-II (NCT01882439) had a duration of 6 months and enrolled
• adults who had an inadequate response to at least one approved TNF blocker.
• This clinical trial included a 3-month placebo-controlled period.
• In these combined Phase 3 clinical trials, 238 patients were randomized and treated with tofacitinib tablets 5 mg twice daily and 236 patients were randomized and treated with tofacitinib tablets 10 mg twice daily.
• A dosage of tofacitinib tablets 10 mg twice daily is not recommended for the treatment of PsA.
• For the treatment of
• adults with active PsA [see Indications and Usage (1.2)] , the recommended dosage of tofacitinib tablets is 5 mg twice daily [see Dosage and Administration (2.3)].
• All patients in the clinical trials in patients with PsA were required to receive treatment with a stable dose of a nonbiologic DMARD [the majority (79%) received methotrexate].
• The study population randomized and treated with tofacitinib tablets (474 patients) included 45 (10%) patients aged 65 years or older and 66 (14%) patients with diabetes at baseline.
• During the 2 PsA controlled clinical trials, there were:
• 3 malignancies (excluding NMSC) in 474 patients who received tofacitinib tablets plus non-biologic DMARD (6 to 12 months exposure) 0 malignancies in 236 patients who received placebo plus non-biologic DMARD group (3 months exposure) and 0 malignancies in 106 patients in patients who received adalimumab plus non-biologic DMARD group (12 months exposure).
• No lymphomas were reported.
• Malignancies have also been observed in the long-term extension study in patients with PsA treated with tofacitinib tablets.
• The safety profile observed in
• adults with active PsA treated with tofacitinib tablets was consistent with the safety profile observed in
• adults with RA.
• Adverse Reactions in
• Adults with Ankylosing Spondylitis The safety of tofacitinib tablets was evaluated in
• adults with active ankylosing spondylitis (AS) in a double-blind placebo-controlled Phase 3 clinical trial (Study AS-I) and in a dose-ranging Phase 2 clinical trial (Study AS-II).
• Study AS-I (NCT03502616) had a duration of 48 weeks and enrolled
• adults who had an inadequate response to at least 2 NSAIDs.
• Study AS-I included a 16-week double-blind period in which patients received tofacitinib tablets 5 mg or placebo twice daily and a 32-week open-label treatment period in which all patients received tofacitinib tablets 5 mg twice daily.
• Study AS-II (NCT01786668) had a duration of 16 weeks and enrolled
• adults who had an inadequate response to at least 2 NSAIDs.
• This clinical trial included a 12-week treatment period in which patients received either tofacitinib tablets 2 mg (40% of the recommended dose), 5 mg, 10 mg, or placebo twice daily.
• A dosage of tofacitinib tablets 10 mg twice daily is not recommended for the treatment of AS .
• For the treatment of
• adults with active AS [see Indications and Usage (1.3)], the recommended dosage of tofacitinib tablets is 5 mg twice daily [see Dosage and Administration (2.3)].
• In the combined Phase 2 and Phase 3 clinical trials, a total of 420 patients were treated with either tofacitinib tablets 2 mg, 5 mg, or 10 mg twice daily.
• Of these, 316 patients were treated with tofacitinib tablets 5 mg twice daily for up to 48 weeks.
• In the combined double-blind period, 185 patients were randomized to and treated with tofacitinib tablets 5 mg twice daily and 187 to placebo for up to 16 weeks.
• Concomitant treatment with stable doses of nonbiologic DMARDs, NSAIDs, or corticosteroids (≤10 mg/day) was permitted.
• The study population randomized and treated with tofacitinib tablets included 13 (3%) patients aged 65 years or older and 18 (4%) patients with diabetes at baseline.
• The safety profile observed in
• adults with AS treated with tofacitinib tablets was consistent with the safety profile observed in
• adults with RA and PsA.
• Adverse Reactions in Pediatric Patients 2 Years of Age and Older with Polyarticular Course Juvenile Idiopathic Arthritis Tofacitinib tablets and XELJANZ oral solution 5 mg twice daily or weight-based equivalent twice daily was studied in 225 pediatric patients from 2 years to 17 years of age in Study pcJIA-I [see Clinical Studies (14.4)] and one open-label extension study (Study A3921145).
• The total patient exposure (defined as patients who received at least one dose of tofacitinib tablets or XELJANZ oral solution) was 105.6 patient-years in Study pcJIA-I and 777.5 patient-years in Study A3921145.
• In general, the types of adverse reactions in pediatric patients 2 years of age and older with pcJIA, were consistent with those seen in
• adults with RA and PsA (see Adverse Reactions in
• Adults with Rheumatoid Arthritis and Adverse Reactions in
• Adults with Psoriatic Arthritis) .
• Adverse Reactions in
• Adults with Ulcerative Colitis The safety of tofacitinib tablets has been evaluated in
• adults with moderately to severely active UC in 4 randomized, double-blind, placebo-controlled trials (UC-I, UC-II, UC-III, and dose-ranging UC-V) and an open-label long-term extension study (UC-IV) [see Clinical Studies (14.5)] .
• Adverse reactions reported in ≥5% of patients treated with either tofacitinib tablets 5 mg or 10 mg twice daily and ≥1% greater than reported in patients receiving placebo in either the induction or maintenance clinical trials of patients with UC were:
• nasopharyngitis, elevated cholesterol levels, headache, upper respiratory tract infection, increased blood creatine phosphokinase, rash, diarrhea, and herpes zoster.
• Induction Trials in
• Adults with UC Common adverse reactions reported in ≥2% of patients treated with tofacitinib tablets 10 mg twice daily and ≥1% greater in tofacitinib tablets-treated patients than placebo-treated patients in the 3 induction trials of patients with UC (Studies UC-I, UC-II, and UC-V) were:
• headache, nasopharyngitis, elevated cholesterol levels, acne, increased blood creatine phosphokinase, and pyrexia.
• Maintenance Trial in
• Adults with UC Common adverse reactions reported in ≥4% of patients treated with either dosage of tofacitinib tablets and ≥1% greater than reported in patients treated with placebo in the maintenance trial of patients with UC (Study UC-III) are shown in Table 6.
• Table 6:
• Common Adverse Reactions* in
• Adults with UC During the 52-Week Maintenance Trial (Study UC-III) Preferred Term Placebo Tofacitinib Tablets 5 mg Twice Daily Tofacitinib Tablets 10 mg Twice Daily N = 198 (%) N = 198 (%) N = 196 (%) Nasopharyngitis 6 10 14 Elevated cholesterol levels** 1 5 9 Headache 6 9 3 Upper respiratory tract infection 4 7 6 Increased blood creatine phosphokinase 2 3 7 Rash 4 3 6 Diarrhea 3 2 5 Herpes zoster 1 1 5 Gastroenteritis 3 3 4 Anemia 2 4 2 Nausea 3 1 4 * Reported in ≥4% of patients treated with either tofacitinib tablets dosage and ≥1% greater in tofacitinib tablets-treated patients than placebo-treated patients. ** Includes hypercholesterolemia, hyperlipidemia, blood cholesterol increased, dyslipidemia, blood triglycerides increased, low-density lipoprotein increased, low-density lipoprotein abnormal, or lipids increased.
• Dose-dependent adverse reactions seen in patients treated with tofacitinib tablets 10 mg twice daily, in comparison to 5 mg twice daily, include the following:
• herpes zoster infections, serious infections, and NMSC [see Warnings and Precautions (5.1, 5.3)].
• During the UC controlled clinical studies (8-week induction and 52-week maintenance studies), which included 1,220 patients, 0 cases of solid cancer or lymphoma were observed in tofacitinib tablets-treated patients.
• In the long-term extension study, malignancies (including solid cancers, lymphomas and NMSC) were observed in patients treated with tofacitinib tablets 5 mg and 10 mg twice daily [see Warnings and Precautions (5.3)] .
• Five cases of pulmonary embolism were reported in patients taking tofacitinib tablets 10 mg twice daily, including one fatality in a patient with advanced cancer [see Warnings and Precautions (5.5)] .
• 6.2 Postmarketing Experience The following adverse reactions have been identified during post-approval use of tofacitinib 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

Quoted from the official label, section “Adverse Reactions”.

What to discuss with your doctor

• Advise patients to read the FDA-approved patient labeling (Medication Guide).
• Serious Infections Inform patients that tofacitinib tablets may lower the ability of their immune system to fight infections.
• Advise patients not to start taking tofacitinib tablets 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 tablets [see Warnings and Precautions (5.1)] .
• Malignancies and Lymphoproliferative Disorders Inform patients that tofacitinib tablets may increase their risk of certain cancers, and that lymphoma and other cancers have been observed in patients taking tofacitinib tablets.
• 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 tablets 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 tablets 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 tablets and to call their healthcare provider right away if they experience any symptoms of allergic reactions while taking tofacitinib tablets [see Warnings and Precautions (5.7)] .
• Important Information on Laboratory Abnormalities Inform patients that tofacitinib tablets may affect certain lab test results, and that blood tests are required before and during tofacitinib tablets treatment [see Warnings and Precautions (5.8)] .
• 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 tablets and for at least 18 hours after the last dose of tofacitinib tablets [see Use in Specific Populations (8.2)].
• Infertility Advise females of reproductive potential that tofacitinib tablets may impair fertility [see Use in Specific Populations (8.3), Nonclinical Toxicology (13.1)] .
• It is not known if this effect is reversible.

Quoted from the official label, section “Patient Counseling Information”.

Strengths and forms

• FORMS AND STRENGTHS Tofacitinib tablets:
• 5 mg:
• White, round, immediate-release biconvex film-coated tablets, debossed with "T5" on one side, and no debossing on the other side. 10 mg:
• Blue, round, immediate-release biconvex film-coated tablets, debossed with "T10" on one side, and no debossing on the other side.
• Tofacitinib tablets: 5 mg, 10 mg (3)

Quoted from the official label, section “Dosage Forms & Strengths”.

What it looks like and how it is packed

• How Supplied Information for Tofacitinib Tablets How supplied information for tofacitinib tablets is shown in Table 23.
• Table 23:
• How Supplied Information for Tofacitinib Tablets Dosage Form, Strength, and Description Bottle Size (number of tablets) NDC Number Tofacitinib tablets, 5 mg White, round, immediate-release, biconvex film-coated tablets, debossed with "T5" on one side, and no debossing on the other side 60 NDC 70069- 841 -01 Tofacitinib tablets, 10 mg Blue, round, immediate-release, biconvex film-coated tablets, debossed with "T10" on one side, and no debossing on the other side 60 NDC 70069- 842 -01 Storage and Handling for tofacitinib tablets Store tofacitinib tablets at 20°C to 25°C (68°F to 77°F). [See USP Controlled Room Temperature].
• Do not repackage.

Quoted from the official label, section “How Supplied”.

What is in it

• Tofacitinib tablets 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 C16H20N6O
• C6H8O7. The chemical structure of tofacitinib citrate is:
• Tofacitinib tablets are supplied for oral administration as a:
• 5 mg white round, biconvex, debossed with "T5" on one side and no debossing on the other side, immediate-release film-coated tablet. Each tofacitinib tablet contains 5 mg of tofacitinib (equivalent to 8.08 mg of tofacitinib citrate) and the following inactive ingredients:
• croscarmellose sodium, hypromellose 2910, lactose monohydrate, macrogol/PEG400, magnesium stearate, microcrystalline cellulose, and titanium dioxide. 10 mg blue round, biconvex, debossed with "T10" on one side and no debossing on the other side, immediate-release film-coated tablet. Each tofacitinib tablet contains 10 mg of tofacitinib (equivalent to 16.16 mg of tofacitinib citrate) and the following inactive ingredients:
• croscarmellose sodium, FD&C Blue #2/Indigo Carmine Aluminum Lake, hypromellose 2910, lactose monohydrate, macrogol/PEG4000, magnesium stearate, microcrystalline cellulose, and titanium dioxide. Image

Quoted from the official label, section “Description”.

Ingredients people check for

Lactose, gluten, dyes, sugars and other ingredients that matter with an allergy, intolerance or diet — as this product’s FDA label lists them.

Same active substance, strength and form in other countries

Matched on active substance, strength and kind of form only. This is not a statement that the products are equivalent or interchangeable: other ingredients, release and approved uses can differ — ask a pharmacist before swapping.

Medicine passport: one printable page to show a pharmacist abroad

Details

Source: NDC Directory · 2026-09-13 · not reviewed by a clinician

Source: US Food and Drug Administration, NDC Directory. Reuse terms: US government work (FDA).

Report wrong or outdated information on this page

Other strengths and forms

36 products are sold under this name. Grouped by form; a number on a strength means several companies make it.

Same active substance

These contain the same substance. That does not mean one can replace another — ask a pharmacist.

See every product with Tofacitinib