(tofacitinib)

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Dosage and Administration

2 DOSAGE AND ADMINISTRATION

2.1 Recommended Evaluations and Immunization Prior to Treatment Initiation

Prior to initiating XELJANZ (tablets and oral solution) or XELJANZ XR (extended-release tablets), consider performing the following:

•
Active and latent tuberculosis (TB) infection evaluation: If the patient has latent TB, treat for TB prior to XELJANZ/XELJANZ XR 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 XELJANZ/XELJANZ XR treatment in patients with a lymphocyte count less than 500 cells/mm3, absolute neutrophil count less than 1000 cells/mm3, or hemoglobin level less than 9 g/dL [see Warnings and Precautions (5.8)].
•
Baseline hepatic function evaluation: XELJANZ/XELJANZ XR 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 XELJANZ/XELJANZ XR 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 XELJANZ (tablets and oral solution). Switching between XELJANZ 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 XELJANZ/XELJANZ XR if a patient develops a serious infection until the infection is controlled [see Warnings and Precautions (5.1)].
•
Take XELJANZ/XELJANZ XR with or without food [see Clinical Pharmacology (12.3)].
•
Swallow XELJANZ XR whole and intact. Do not crush, split, or chew the extended-release tablets [see Clinical Pharmacology (12.3)].

2.3 Recommended Dosage in Adults with Rheumatoid Arthritis, Psoriatic Arthritis, and Ankylosing Spondylitis

Table 1 displays the recommended dosage of XELJANZ tablets and XELJANZ XR (extended-release 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 XELJANZ Tablets and XELJANZ XR in Adults with Rheumatoid Arthritis, Psoriatic Arthritis, or Ankylosing Spondylitis
*
Excludes patients who concomitantly use XELJANZ tablets/XELJANZ XR 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/mm3, ANC <1000 cells/mm3, or hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL.
†
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).

Adults

XELJANZ Tablets

XELJANZ XR

(extended-release tablets)

Patients with Normal Renal and Hepatic Function*

5 mg twice daily

11 mg once daily

Recommended Dosage in Patients with Renal Impairment (RI)†

Mild RI

(CLcr >50 and ≤80 mL/min)

5 mg twice daily

11 mg once daily

Moderate RI

(CLcr ≥30 and ≤50 mL/min)

5 mg once daily

XELJANZ tablets 5 mg once daily

Severe RI

(CLcr <30 mL/min)

5 mg once daily

XELJANZ tablets 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

11 mg once daily

Moderate HI

(Child-Pugh B)

5 mg once daily

XELJANZ tablets 5 mg once daily

Severe HI

(Child-Pugh C)

Use of XELJANZ tablets/XELJANZ XR is not recommended.

Dosage Modifications with Concomitant Use of CYP3A4 and/or CYP2C19 Inhibitor(s)

Strong CYP2C19 inhibitor(s)

5 mg twice daily

11 mg once 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

XELJANZ tablets 5 mg once daily

Strong CYP3A4 inhibitor(s)

Dosage Modifications for Lymphopenia, Neutropenia, or Anemia

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

Discontinue dosing.

Patients with ANC less than 500 cells/mm3

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 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 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 XELJANZ tablets and XELJANZ 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, neutropenia, or anemia.

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

Table 2: Recommended Dosage of XELJANZ Tablets and XELJANZ Oral Solution in Pediatric Patients 2 Years of Age and Older with PsA or pcJIA
Pediatric Patients 2 Years of Age and OlderXELJANZ tablets and XELJANZ oral solution
*
Excludes patients who concomitantly use XELJANZ (tablets and oral solution) 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/mm3, ANC <1000 cells/mm3, or hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL.
†
Patients treated with XELJANZ oral solution 5 mL may be switched to XELJANZ tablets 5 mg.

Patients with Normal Renal and Hepatic Function*

•
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†

Recommended Dosage in Patients with Renal Impairment (RI)

Mild RI

Same as patients with normal renal function.

Moderate RI

•
10 kg ≤ body weight <20 kg: 3.2 mg once daily
•
20 kg ≤ body weight <40 kg: 4 mg once daily
•
Body weight ≥40 kg: 5 mg once daily†

Severe RI

•
10 kg ≤ body weight <20 kg: 3.2 mg once daily
•
20 kg ≤ body weight <40 kg: 4 mg once daily
•
Body weight ≥40 kg: 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

Same as patients with normal hepatic function.

Moderate HI

•
10 kg ≤ body weight <20 kg: 3.2 mg once daily
•
20 kg ≤ body weight <40 kg: 4 mg once daily
•
Body weight ≥40 kg: 5 mg once daily†

Severe HI

Use of XELJANZ tablets/XELJANZ oral solution 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)

•
10 kg ≤ body weight <20 kg: 3.2 mg once daily
•
20 kg ≤ body weight <40 kg: 4 mg once daily
•
Body weight ≥40 kg: 5 mg once daily†

Strong CYP3A4 inhibitor(s)

Dosage Modifications for Lymphopenia, Neutropenia, or Anemia

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

Discontinue dosing.

Patients with ANC less than 500 cells/mm3

Discontinue dosing.

Patients with ANC 500 to 1000 cells/mm3

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

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

Interrupt dosing until hemoglobin values have normalized.

2.5 Recommended Dosage in Adults with Ulcerative Colitis

Table 3 displays the recommended dosage of XELJANZ tablets and XELJANZ XR (extended-release 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 XELJANZ Tablets and XELJANZ XR in Adults with Ulcerative Colitis With and Without Renal Impairment or Hepatic Impairment
AdultsXELJANZ
tablets		XELJANZ XR
(extended-release tablets)
*
Excludes patients who concomitantly use XELJANZ tablets/XELJANZ XR 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/mm3, ANC <1000 cells/mm3, or hemoglobin less than 8 g/dL or a decrease of more than 2 g/dL.
†
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).

Patients with Normal Renal and Hepatic Function*

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.

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: 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.

Maintenance: 11 mg once daily.

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

Recommended Dosage in Patients with Renal Impairment (RI)†

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.

Induction: 11 mg once daily for at least 8 weeks; evaluate patients and transition to maintenance therapy depending on therapeutic response. If needed continue 11 mg once daily for a maximum of 16 weeks. Discontinue 11 mg once daily after 16 weeks if adequate therapeutic response is not achieved.

Severe RI
(CLcr <30 mL/min)

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.

Maintenance: XELJANZ XR is not recommended. See Maintenance Dosage for XELJANZ tablets for Moderate or Severe RI.


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)

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.

Induction: 11 mg once daily for at least 8 weeks; evaluate patients and transition to maintenance therapy depending on therapeutic response. If needed continue 11 mg once daily for a maximum of 16 weeks. Discontinue 11 mg once 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.

Maintenance: XELJANZ XR is not recommended. See Maintenance Dosage for XELJANZ tablets for Moderate HI.

Severe HI
(Child-Pugh C)

Use of XELJANZ tablets/XELJANZ XR is not recommended.

Table 4: Dosage Modifications of XELJANZ Tablets and XELJANZ XR Due to Drug Interactions and for Lymphopenia, Neutropenia or Anemia in Adults with Ulcerative Colitis
AdultsXELJANZ
Tablets		XELJANZ XR
(extended-release tablets)

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)

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.

Induction: 11 mg once daily for at least 8 weeks; evaluate patients and transition to maintenance therapy depending on therapeutic response. If needed continue 11 mg once daily for a maximum of 16 weeks. Discontinue 11 mg once 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.

Maintenance: XELJANZ XR is not recommended. see Maintenance Dosage for XELJANZ tablets for Strong CYP3A4 inhibitors.

Dosage Modifications for Lymphopenia, Neutropenia, or Anemia

Lymphocyte count less than 500 cells/mm3, confirmed by repeat testing

Discontinue dosing.

ANC less than 500 cells/mm3

Discontinue dosing.

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.
•
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.
•
11 mg once daily, interrupt dosing. When ANC is greater than 1000, resume 11 mg once 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 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 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 XELJANZ tablets 10 mg.
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