XELJANZ / XELJANZ XR Dosage and Administration

(tofacitinib)

2 DOSAGE AND ADMINISTRATION

2.1 Important Administration Instructions

•
XELJANZ XR (tofacitinib extended-release tablets) is not interchangeable or substitutable with XELJANZ Oral Solution.
•
Changes between XELJANZ and XELJANZ XR should be made by the healthcare provider [see Dosage and Administration (2.2)].
•
Do not initiate XELJANZ/XELJANZ XR/XELJANZ Oral Solution in patients with an absolute lymphocyte count less than 500 cells/mm3, an absolute neutrophil count (ANC) less than 1000 cells/mm3 or who have hemoglobin levels less than 9 g/dL.
•
Dose interruption is recommended for management of lymphopenia, neutropenia, and anemia [see Warnings and Precautions (5.8), Adverse Reactions (6.1)].
•
Interrupt use of XELJANZ/XELJANZ XR/XELJANZ Oral Solution if a patient develops a serious infection until the infection is controlled [see Warnings and Precautions (5.1)].
•
Take XELJANZ/XELJANZ XR/XELJANZ Oral Solution with or without food [see Clinical Pharmacology (12.3)].
•
Swallow XELJANZ XR tablets whole and intact. Do not crush, split, or chew.

2.2 Recommended Dosage in Rheumatoid Arthritis, Psoriatic Arthritis, and Ankylosing Spondylitis

Table 1 displays the recommended adult daily dosage of XELJANZ and XELJANZ XR and dosage adjustments for patients receiving CYP2C19 and/or CYP3A4 inhibitors, in patients with moderate or severe renal impairment (including but not limited to those with severe insufficiency who are undergoing hemodialysis) or moderate hepatic impairment, with lymphopenia, neutropenia, or anemia.

Table 1: Recommended Dosage of XELJANZ and XELJANZ XR in Patients with Rheumatoid Arthritis, Psoriatic Arthritis*, and Ankylosing Spondylitis
XELJANZ
tablet		XELJANZ XR
extended-release tablet
*
XELJANZ/XELJANZ XR is used in combination with nonbiologic disease-modifying antirheumatic drugs (DMARDs) in psoriatic arthritis. The efficacy of XELJANZ/XELJANZ XR as a monotherapy has not been studied in psoriatic arthritis.
†
Use of XELJANZ/XELJANZ XR in patients with severe hepatic impairment is not recommended.

Adult patients

5 mg twice daily

11 mg once daily

Patients receiving:

•
Strong CYP3A4 inhibitors (e.g., ketoconazole), or
•
a moderate CYP3A4 inhibitor(s) with a strong CYP2C19 inhibitor(s) (e.g., fluconazole)

[see Drug Interactions (7)]

5 mg once daily

Reduce to XELJANZ 5 mg once daily

Patients with:

•
moderate or severe renal impairment [see Use in Specific Populations (8.7)]
•
moderate hepatic impairment [see Use in Specific Populations (8.8)]†

5 mg once daily

Reduce to XELJANZ 5 mg once daily

For patients undergoing hemodialysis, dose should be administered after the dialysis session on dialysis days. If a dose was taken before the dialysis procedure, supplemental doses are not recommended in patients after dialysis.

Patients with lymphocyte count less than 500 cells/mm3, confirmed by repeat testing

Discontinue dosing.

Patients with ANC 500 to 1000 cells/mm3

Interrupt dosing.
When ANC is greater than 1000, resume 5 mg twice daily.

Interrupt dosing.
When ANC is greater than 1000, resume 11 mg once daily.

Patients with ANC less than 500 cells/mm3

Discontinue dosing.

Patients with hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL

Interrupt dosing until hemoglobin values have normalized.

Switching from XELJANZ Tablets to XELJANZ XR Extended-Release Tablets

Patients treated with XELJANZ 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 XELJANZ 5 mg.

2.3 Recommended Dosage in Ulcerative Colitis

Table 2 displays the recommended adult daily dosage of XELJANZ/XELJANZ XR and dosage adjustments for patients receiving CYP2C19 and/or CYP3A4 inhibitors, with moderate or severe renal impairment (including but not limited to those with severe insufficiency who are undergoing hemodialysis) or moderate hepatic impairment, with lymphopenia, neutropenia or anemia.

Table 2: Recommended Dosage of XELJANZ/XELJANZ XR in Patients with UC
XELJANZ
tablet		XELJANZ XR
extended-release tablet
*
Use of XELJANZ/XELJANZ XR in patients with severe hepatic impairment is not recommended.

Adult patients

Induction: 10 mg twice daily for at least 8 weeks [see Clinical Studies (14.4)]; 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, a dosage of 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.

Induction: 22 mg once daily for at least 8 weeks; evaluate patients and transition to maintenance therapy depending on therapeutic response. If needed continue 22 mg once daily for a maximum of 16 weeks. Discontinue 22 mg once daily after 16 weeks if adequate therapeutic response is not achieved.


Maintenance: 11 mg once daily.


For patients with loss of response during maintenance treatment, a dosage of 22 mg once 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.

Patients receiving:

•
Strong CYP3A4 inhibitors (e.g., ketoconazole), or
•
a moderate CYP3A4 inhibitor(s) with a strong CYP2C19 inhibitor(s) (e.g., fluconazole)

[see Drug Interactions (7)]

If taking 10 mg twice daily, reduce to 5 mg twice daily.


If taking 5 mg twice daily, reduce to 5 mg once daily.

If taking 22 mg once daily, reduce to 11 mg once daily.


If taking 11 mg once daily, reduce to XELJANZ 5 mg once daily

Patients with:

•
moderate or severe renal impairment [see Use in Specific Populations (8.7)]
•
moderate hepatic impairment [see Use in Specific Populations (8.8)]*

If taking 10 mg twice daily, reduce to 5 mg twice daily.


If taking 5 mg twice daily, reduce to 5 mg once daily.

If taking 22 mg once daily, reduce to 11 mg once daily.


If taking 11 mg once daily, reduce to XELJANZ 5 mg once daily.

For patients undergoing hemodialysis, dose should be administered after the dialysis session on dialysis days. If a dose was taken before the dialysis procedure, supplemental doses are not recommended in patients after dialysis.

Patients with lymphocyte count less than 500 cells/mm3, confirmed by repeat testing

Discontinue dosing.

Patients with ANC 500 to 1000 cells/mm3

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.


If taking 5 mg twice daily, interrupt dosing. When ANC is greater than 1000, resume 5 mg twice daily.

If taking 22 mg once daily, reduce to 11 mg once daily. When ANC is greater than 1000, increase to 22 mg once daily based on clinical response.


If taking 11 mg once daily, interrupt dosing. When ANC is greater than 1000, resume 11 mg once daily.

Patients with ANC less than 500 cells/mm3

Discontinue dosing.

Patients with hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL

Interrupt dosing until hemoglobin values have normalized.

Switching from XELJANZ Tablets to XELJANZ XR Extended-Release Tablets

Patients treated with XELJANZ 5 mg tablets twice daily may be switched to XELJANZ XR extended-release tablets 11 mg once daily the day following the last dose of XELJANZ tablets 5 mg. Patients treated with XELJANZ 10 mg tablets twice daily may be switched to XELJANZ XR extended-release tablets 22 mg once daily the day following the last dose of XELJANZ 10 mg.

2.4 Recommended Dosage in Polyarticular Course Juvenile Idiopathic Arthritis

Table 3 displays the recommended body weight-based dosages for XELJANZ tablets/XELJANZ Oral Solution and dosage adjustments for patients receiving CYP2C19 and/or CYP3A4 inhibitors [see Drug Interactions (7)], in patients with moderate or severe renal impairment, including but not limited to those undergoing hemodialysis [see Use in Specific Populations (8.7)], with moderate hepatic impairment [see Use in Specific Populations (8.8)], with lymphopenia, neutropenia, or anemia.

Table 3: Recommended Dosage of XELJANZ/XELJANZ Oral Solution in Patients with pcJIA
XELJANZ tablets/XELJANZ Oral Solution
*
Patients treated with 5 mL XELJANZ Oral Solution may be switched to a XELJANZ 5 mg tablet.
†
XELJANZ/XELJANZ Oral Solution is not recommended for patients with severe hepatic impairment.

pcJIA patients

•
10 kg ≤ body weight <20 kg:
3.2 mg (3.2 mL oral solution) twice daily
•
20 kg ≤ body weight <40 kg:
4 mg (4 mL oral solution) twice daily
•
Body weight ≥40 kg:
5 mg (one 5 mg tablet or 5 mL oral solution*) twice daily

Patients receiving:

•
strong CYP3A4 inhibitors (e.g., ketoconazole), or
•
a moderate CYP3A4 inhibitor(s) with a strong CYP2C19 inhibitor(s) (e.g., fluconazole)

[see Drug Interactions (7)]

If taking 3.2 mg twice daily, reduce to 3.2 mg once daily.


If taking 4 mg twice daily, reduce to 4 mg once daily.


If taking 5 mg twice daily, reduce to 5 mg once daily.

Patients with:

•
moderate or severe renal impairment [see Use in Specific Populations (8.7)]
•
moderate hepatic impairment [see Use in Specific Populations (8.8)]†

If taking 3.2 mg twice daily, reduce to 3.2 mg once daily.


If taking 4 mg twice daily, reduce to 4 mg once daily.


If taking 5 mg twice daily, reduce to 5 mg once daily.


For patients undergoing hemodialysis, dose should be administered after the dialysis session on dialysis days. If a dose was taken before the dialysis procedure, supplemental doses are not recommended in patients after dialysis.

Patients with lymphocyte count less than 500 cells/mm3, confirmed by repeat testing

Discontinue dosing.

Patients with ANC 500 to 1000 cells/mm3

Interrupt dosing until ANC is greater than 1000 cells/mm3.

Patients with ANC less than 500 cells/mm3

Discontinue dosing.

Patients with hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL

Interrupt dosing until hemoglobin values have normalized.

Administer XELJANZ Oral Solution using the included press-in bottle adapter and oral dosing syringe [see Instructions for Use].

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Dosage and Administration

2 DOSAGE AND ADMINISTRATION

2.1 Important Administration Instructions

•
XELJANZ XR (tofacitinib extended-release tablets) is not interchangeable or substitutable with XELJANZ Oral Solution.
•
Changes between XELJANZ and XELJANZ XR should be made by the healthcare provider [see Dosage and Administration (2.2)].
•
Do not initiate XELJANZ/XELJANZ XR/XELJANZ Oral Solution in patients with an absolute lymphocyte count less than 500 cells/mm3, an absolute neutrophil count (ANC) less than 1000 cells/mm3 or who have hemoglobin levels less than 9 g/dL.
•
Dose interruption is recommended for management of lymphopenia, neutropenia, and anemia [see Warnings and Precautions (5.8), Adverse Reactions (6.1)].
•
Interrupt use of XELJANZ/XELJANZ XR/XELJANZ Oral Solution if a patient develops a serious infection until the infection is controlled [see Warnings and Precautions (5.1)].
•
Take XELJANZ/XELJANZ XR/XELJANZ Oral Solution with or without food [see Clinical Pharmacology (12.3)].
•
Swallow XELJANZ XR tablets whole and intact. Do not crush, split, or chew.

2.2 Recommended Dosage in Rheumatoid Arthritis, Psoriatic Arthritis, and Ankylosing Spondylitis

Table 1 displays the recommended adult daily dosage of XELJANZ and XELJANZ XR and dosage adjustments for patients receiving CYP2C19 and/or CYP3A4 inhibitors, in patients with moderate or severe renal impairment (including but not limited to those with severe insufficiency who are undergoing hemodialysis) or moderate hepatic impairment, with lymphopenia, neutropenia, or anemia.

Table 1: Recommended Dosage of XELJANZ and XELJANZ XR in Patients with Rheumatoid Arthritis, Psoriatic Arthritis*, and Ankylosing Spondylitis
XELJANZ
tablet		XELJANZ XR
extended-release tablet
*
XELJANZ/XELJANZ XR is used in combination with nonbiologic disease-modifying antirheumatic drugs (DMARDs) in psoriatic arthritis. The efficacy of XELJANZ/XELJANZ XR as a monotherapy has not been studied in psoriatic arthritis.
†
Use of XELJANZ/XELJANZ XR in patients with severe hepatic impairment is not recommended.

Adult patients

5 mg twice daily

11 mg once daily

Patients receiving:

•
Strong CYP3A4 inhibitors (e.g., ketoconazole), or
•
a moderate CYP3A4 inhibitor(s) with a strong CYP2C19 inhibitor(s) (e.g., fluconazole)

[see Drug Interactions (7)]

5 mg once daily

Reduce to XELJANZ 5 mg once daily

Patients with:

•
moderate or severe renal impairment [see Use in Specific Populations (8.7)]
•
moderate hepatic impairment [see Use in Specific Populations (8.8)]†

5 mg once daily

Reduce to XELJANZ 5 mg once daily

For patients undergoing hemodialysis, dose should be administered after the dialysis session on dialysis days. If a dose was taken before the dialysis procedure, supplemental doses are not recommended in patients after dialysis.

Patients with lymphocyte count less than 500 cells/mm3, confirmed by repeat testing

Discontinue dosing.

Patients with ANC 500 to 1000 cells/mm3

Interrupt dosing.
When ANC is greater than 1000, resume 5 mg twice daily.

Interrupt dosing.
When ANC is greater than 1000, resume 11 mg once daily.

Patients with ANC less than 500 cells/mm3

Discontinue dosing.

Patients with hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL

Interrupt dosing until hemoglobin values have normalized.

Switching from XELJANZ Tablets to XELJANZ XR Extended-Release Tablets

Patients treated with XELJANZ 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 XELJANZ 5 mg.

2.3 Recommended Dosage in Ulcerative Colitis

Table 2 displays the recommended adult daily dosage of XELJANZ/XELJANZ XR and dosage adjustments for patients receiving CYP2C19 and/or CYP3A4 inhibitors, with moderate or severe renal impairment (including but not limited to those with severe insufficiency who are undergoing hemodialysis) or moderate hepatic impairment, with lymphopenia, neutropenia or anemia.

Table 2: Recommended Dosage of XELJANZ/XELJANZ XR in Patients with UC
XELJANZ
tablet		XELJANZ XR
extended-release tablet
*
Use of XELJANZ/XELJANZ XR in patients with severe hepatic impairment is not recommended.

Adult patients

Induction: 10 mg twice daily for at least 8 weeks [see Clinical Studies (14.4)]; 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, a dosage of 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.

Induction: 22 mg once daily for at least 8 weeks; evaluate patients and transition to maintenance therapy depending on therapeutic response. If needed continue 22 mg once daily for a maximum of 16 weeks. Discontinue 22 mg once daily after 16 weeks if adequate therapeutic response is not achieved.


Maintenance: 11 mg once daily.


For patients with loss of response during maintenance treatment, a dosage of 22 mg once 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.

Patients receiving:

•
Strong CYP3A4 inhibitors (e.g., ketoconazole), or
•
a moderate CYP3A4 inhibitor(s) with a strong CYP2C19 inhibitor(s) (e.g., fluconazole)

[see Drug Interactions (7)]

If taking 10 mg twice daily, reduce to 5 mg twice daily.


If taking 5 mg twice daily, reduce to 5 mg once daily.

If taking 22 mg once daily, reduce to 11 mg once daily.


If taking 11 mg once daily, reduce to XELJANZ 5 mg once daily

Patients with:

•
moderate or severe renal impairment [see Use in Specific Populations (8.7)]
•
moderate hepatic impairment [see Use in Specific Populations (8.8)]*

If taking 10 mg twice daily, reduce to 5 mg twice daily.


If taking 5 mg twice daily, reduce to 5 mg once daily.

If taking 22 mg once daily, reduce to 11 mg once daily.


If taking 11 mg once daily, reduce to XELJANZ 5 mg once daily.

For patients undergoing hemodialysis, dose should be administered after the dialysis session on dialysis days. If a dose was taken before the dialysis procedure, supplemental doses are not recommended in patients after dialysis.

Patients with lymphocyte count less than 500 cells/mm3, confirmed by repeat testing

Discontinue dosing.

Patients with ANC 500 to 1000 cells/mm3

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.


If taking 5 mg twice daily, interrupt dosing. When ANC is greater than 1000, resume 5 mg twice daily.

If taking 22 mg once daily, reduce to 11 mg once daily. When ANC is greater than 1000, increase to 22 mg once daily based on clinical response.


If taking 11 mg once daily, interrupt dosing. When ANC is greater than 1000, resume 11 mg once daily.

Patients with ANC less than 500 cells/mm3

Discontinue dosing.

Patients with hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL

Interrupt dosing until hemoglobin values have normalized.

Switching from XELJANZ Tablets to XELJANZ XR Extended-Release Tablets

Patients treated with XELJANZ 5 mg tablets twice daily may be switched to XELJANZ XR extended-release tablets 11 mg once daily the day following the last dose of XELJANZ tablets 5 mg. Patients treated with XELJANZ 10 mg tablets twice daily may be switched to XELJANZ XR extended-release tablets 22 mg once daily the day following the last dose of XELJANZ 10 mg.

2.4 Recommended Dosage in Polyarticular Course Juvenile Idiopathic Arthritis

Table 3 displays the recommended body weight-based dosages for XELJANZ tablets/XELJANZ Oral Solution and dosage adjustments for patients receiving CYP2C19 and/or CYP3A4 inhibitors [see Drug Interactions (7)], in patients with moderate or severe renal impairment, including but not limited to those undergoing hemodialysis [see Use in Specific Populations (8.7)], with moderate hepatic impairment [see Use in Specific Populations (8.8)], with lymphopenia, neutropenia, or anemia.

Table 3: Recommended Dosage of XELJANZ/XELJANZ Oral Solution in Patients with pcJIA
XELJANZ tablets/XELJANZ Oral Solution
*
Patients treated with 5 mL XELJANZ Oral Solution may be switched to a XELJANZ 5 mg tablet.
†
XELJANZ/XELJANZ Oral Solution is not recommended for patients with severe hepatic impairment.

pcJIA patients

•
10 kg ≤ body weight <20 kg:
3.2 mg (3.2 mL oral solution) twice daily
•
20 kg ≤ body weight <40 kg:
4 mg (4 mL oral solution) twice daily
•
Body weight ≥40 kg:
5 mg (one 5 mg tablet or 5 mL oral solution*) twice daily

Patients receiving:

•
strong CYP3A4 inhibitors (e.g., ketoconazole), or
•
a moderate CYP3A4 inhibitor(s) with a strong CYP2C19 inhibitor(s) (e.g., fluconazole)

[see Drug Interactions (7)]

If taking 3.2 mg twice daily, reduce to 3.2 mg once daily.


If taking 4 mg twice daily, reduce to 4 mg once daily.


If taking 5 mg twice daily, reduce to 5 mg once daily.

Patients with:

•
moderate or severe renal impairment [see Use in Specific Populations (8.7)]
•
moderate hepatic impairment [see Use in Specific Populations (8.8)]†

If taking 3.2 mg twice daily, reduce to 3.2 mg once daily.


If taking 4 mg twice daily, reduce to 4 mg once daily.


If taking 5 mg twice daily, reduce to 5 mg once daily.


For patients undergoing hemodialysis, dose should be administered after the dialysis session on dialysis days. If a dose was taken before the dialysis procedure, supplemental doses are not recommended in patients after dialysis.

Patients with lymphocyte count less than 500 cells/mm3, confirmed by repeat testing

Discontinue dosing.

Patients with ANC 500 to 1000 cells/mm3

Interrupt dosing until ANC is greater than 1000 cells/mm3.

Patients with ANC less than 500 cells/mm3

Discontinue dosing.

Patients with hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL

Interrupt dosing until hemoglobin values have normalized.

Administer XELJANZ Oral Solution using the included press-in bottle adapter and oral dosing syringe [see Instructions for Use].
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