Dosing & Uses
Dosage Forms & Strengths
tablet (Xeljanz)
- 5mg
- 10mg
tablet, extended-release (Xeljanz XR)
- 11mg
- 22mg
Rheumatoid Arthritis
Indicated for moderate-to-severe active rheumatoid arthritis (RA) in adults with an inadequate response or intolerance to ≥1 tumor necrosis factor (TNF) blockers
Xeljanz: 5 mg PO BID
Xeljanz XR: 11 mg PO qDay
Psoriatic Arthritis
Indicated for active psoriatic arthritis in adults who have had an inadequate response or intolerance to ≥1 TNF blockers
Recommended dose in combination with nonbiologic DMARDs
- Xeljanz: 5 mg PO BID
- Xeljanz XR: 11 mg PO qDay
Ulcerative Colitis
Indicated for adults with moderately to severely active ulcerative colitis (UC), who have had an inadequate response or intolerance to ≥1 TNF blockers
Xeljanz
-
Induction
- 10 mg PO BID for at least 8 weeks; evaluate patients and transition to maintenance therapy depending on therapeutic response
- If needed, continue 10 mg BID for maximum of 16 weeks; discontinue after 16 weeks if adequate therapeutic benefit not achieved
-
Maintenance
- 5 mg PO BID; may consider 10 mg BID (limited to shorter duration) in patients with loss of response during maintenance treatment
- Use the lowest effective dose needed to maintain response
Xeljanz XR
-
Induction
- 22 mg PO qDay for at least 8 weeks; evaluate patients and transition to maintenance therapy depending on therapeutic response
- If needed, continue 22 mg qDay for maximum of 16 weeks; discontinue after 16 weeks if adequate therapeutic benefit not achieved
-
Maintenance
- 11 mg PO qDay; may consider 22 mg qDay (limited to shorter duration) in patients with loss of response during maintenance treatment
- Use the lowest effective dose needed to maintain response
Ankylosing Spondylitis
Indicated for active ankylosing spondylitis (AS) in adults who have an inadequate response or are intolerant to ≥1 TNF blockers
Xeljanz: 5 mg PO BID
Xeljanz XR: 11 mg PO qDay
Dosage Modifications
Strong CYP3A4 inhibitors OR moderate CYP3A4 inhibitors with strong CYP2C19 inhibitors
-
RA, PsA, or AS
- Xeljanz: Not to exceed 5 mg qDay
- Xeljanz XR: Switch to Xeljanz 5 mg qDay
-
UC
- Xeljanz: If taking 10 mg BID, reduce to 5 mg BID; if taking 5 mg BID, reduce to 5 mg qDay
- Xeljanz XR: If taking 22 mg qDay, reduce to 11 mg qDay; if taking 11 mg qDay, switch to Xeljanz 5 mg qDay
Lymphopenia
-
RA, PsA, AS, or UC
- Lymphocytes <500 cells/mm3: Confirmed by repeat testing; discontinue until infection controlled
ANC 500-1000 cells/mm³
-
RA, PsA, or AS
- Interrupt dosing for persistent decreases; when ANC >1000/mm3, resume dose at Xeljanz 5 mg BID or Xeljanz XR 11 mg qDay
- ANC <500 cells/mm3: Confirmed by repeat testing; discontinue
-
UC
- Xeljanz: If taking 10 mg BID, reduce to 5 mg BID; when ANC >1000, increase to 10 mg BID based on clinical response; if taking 5 mg BID, interrupt dosing; when ANC >1000, resume 5 mg BID
- Xeljanz XR: If taking 22 mg qDay, reduce to 11 mg qDay when ANC >1000, increase to 22 mg qDay based on clinical response; if taking 11 mg qDay, interrupt dosing; when ANC >1000, resume 11 mg qDay
Anemia
-
RA, PsA, AS, or UC
- Hgb >2 g/dL decrease or level <8.0 g/dL: Confirmed by repeat testing; interrupt treatment until Hgb levels have normalized
Renal impairment
-
RA, PsA, or AS
- Mild: No dosage adjustment required
- Moderate-to-severe (Xeljanz): Not to exceed 5 mg qDay
- Moderate-to-severe (Xeljanz XR): Switch to Xeljanz 5 mg qDay
- Patients undergoing hemodialysis: Administer dose after dialysis session on dialysis days; if dose administered before dialysis session, supplemental doses are not recommended
-
UC
- Mild (Xeljanz and Xeljanz XR): No dosage adjustment required
- Moderate-to-severe (Xeljanz): If taking 10 mg BID, reduce to 5 mg BID; if taking 5 mg BID, reduce to 5 mg qDay
- Moderate-to-severe (Xeljanz XR): If taking 22 mg qDay, reduce to 11 mg qDay; if taking 11 mg qDay, switch to Xeljanz 5 mg qDay
- Patients undergoing hemodialysis: Administer dose after dialysis session on dialysis days; if dose administered before dialysis session, supplemental doses are not recommended
Hepatic impairment
- Safety and efficacy have not been studied in patients with positive hepatitis B virus or hepatitis C virus serology (Add to adult)
-
RA, PsA, or AS
- Mild (Xeljanz and Xeljanz XR): No dosage adjustment required
- Moderate (Xeljanz): Not to exceed 5 mg qDay
- Moderate (Xeljanz XR): Switch to Xeljanz 5 mg qDay
- Severe (Xeljanz and Xeljanz XR): Not recommended
-
UC
- Mild (Xeljanz and Xeljanz XR): No dosage adjustment required
- Moderate (Xeljanz): If taking 10 mg BID, reduce to 5 mg BID; if taking 5 mg BID, reduce to 5 mg qDay
- Moderate (Xeljanz XR): If taking 22 mg qDay, reduce to 11 mg qDay; if taking 11 mg qDay, switch to Xeljanz 5 mg qDay
- Severe (Xeljanz and Xeljanz XR): Not recommended
Dosing Considerations
Higher incidence of infections in geriatric patients; use with caution
Do not initiate if
- Absolute lymphocyte count <500 cells/mm3 OR
- ANC <1000 cells/mm3 OR
- Hgb <9 g/dL
Limitations of use
- RA, PsA, AS: Use in combination with biologic disease-modifying antirheumatic drugs (DMARDS) or potent immunosuppressants (eg, azathioprine, cyclosporine) is not recommended
- UC: Use in combination with biologic therapies or potent immunosuppressants (eg, azathioprine, cyclosporine) is not recommended
Dosage Forms & Strengths
oral solution (Xeljanz)
- 1mg/mL
tablet (Xeljanz)
- 5mg
- 10mg
Polyarticular Course Juvenile Idiopathic Arthritis
Indicated for active polyarticular course juvenile idiopathic arthritis (pcJIA) in patients aged ≥2 years
≥2 years
-
Oral solution
- 10 to <20 kg: 3.2 mg PO BID
- 20 to <40 kg: 4 mg PO BID
-
Oral solution or tablet
- ≥40 kg: 5 mg PO BID
Dosage Modifications
Coadministration with strong CYP3A4 inhibitors, OR a moderate CYP3A4 inhibitor(s) with a strong CYP2C19 inhibitor(s)
-
pcJIA
- If taking 3.2 mg BID, reduce to 3.2 mg qDay
- If taking 4 mg BID, reduce to 4 mg qDay
- If taking 5 mg BID, reduce to 5 mg qDay
Hematologic abnormalities
- Do not initiate in patients with an absolute lymphocyte count <500 cells/mm3, ANC <1000 cells/mm3 or Hgb <9 g/dL
- Lymphocyte count <500 cells/mm3: Confirmed by repeat testing; discontinue dosing
- ANC 500-1000 cells/mm3: Interrupt dosing until ANC >1000 cells/mm3
- ANC <500 cells/mm3: Discontinue dosing
- Hgb <8 g/dL or a decrease of >2 g/dL: Interrupt dosing until Hgb normalized
Renal impairment
-
pcJIA
- Mild: No dosage adjustment required
- Moderate-to-severe: Reduce dosing frequency to qDay (eg, 3.2 mg BID to 3.2 mg qDay)
- Hemodialysis: Administer after dialysis session on dialysis days; if dose taken before dialysis, supplemental doses are not recommended after dialysis
Hepatic impairment
-
pcJIA
- Mild: No dosage adjustment required
- Moderate: Reduce dosing frequency to qDay (eg, 3.2 mg BID to 3.2 mg qDay)
- Severe: Not studied; not recommended
- Safety and efficacy have not been studied in patients with positive hepatitis B virus or hepatitis C virus serology (Add to adult)
Dosing Considerations
Limitation of use: Use in combination with biologic DMARDs or potent immunosuppressants (eg, azathioprine, cyclosporine) is not recommended
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (118)
- abatacept
abatacept, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- antithymocyte globulin equine
antithymocyte globulin equine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- antithymocyte globulin rabbit
antithymocyte globulin rabbit, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- apalutamide
apalutamide will decrease the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP2C19 inducer, with drugs that are CYP2C19 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered.
apalutamide will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed. - atazanavir
atazanavir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- auranofin
auranofin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- axicabtagene ciloleucel
tofacitinib, axicabtagene ciloleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- azathioprine
azathioprine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- baricitinib
baricitinib, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Baricitinib is not recommended in combination with other JAK inhibitors, biologic DMARDs, or potent immunosuppressives.
- basiliximab
basiliximab, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- belatacept
belatacept, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- bendamustine
bendamustine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- betamethasone
betamethasone, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- brexucabtagene autoleucel
tofacitinib, brexucabtagene autoleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- busulfan
busulfan, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- capecitabine
capecitabine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- carboplatin
carboplatin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- carmustine
carmustine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- ceritinib
ceritinib will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- certolizumab pegol
certolizumab pegol, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- chlorambucil
chlorambucil, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- chloramphenicol
chloramphenicol will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ciltacabtagene autoleucel
tofacitinib, ciltacabtagene autoleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- cimetidine
cimetidine increases levels of tofacitinib by decreasing metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with 1 or more concomitant medications that result in both moderate CYP3A4 inhibition and potent CYP2C19 inhibition.
- cisplatin
cisplatin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- cladribine
cladribine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- clarithromycin
clarithromycin increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- clofarabine
clofarabine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- cobicistat
cobicistat increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- conivaptan
conivaptan increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- corticotropin
corticotropin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- cortisone
cortisone, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- cyclophosphamide
cyclophosphamide, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- cyclosporine
cyclosporine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- cytarabine
cytarabine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- dacarbazine
dacarbazine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- darunavir
darunavir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- daunorubicin
daunorubicin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- deferiprone
deferiprone, tofacitinib. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid use of deferiprone with other drugs known to be associated with neutropenia or agranulocytosis; if an alternative is not possible, monitor absolute neutrophil count more frequently.
- dexamethasone
dexamethasone, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- doxorubicin
doxorubicin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- doxorubicin liposomal
doxorubicin liposomal, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- epirubicin
epirubicin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- etanercept
etanercept, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- everolimus
everolimus, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- fexinidazole
fexinidazole will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.
- floxuridine
floxuridine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- fluconazole
fluconazole increases levels of tofacitinib by decreasing metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with 1 or more concomitant medications that result in both moderate CYP3A4 inhibition and potent CYP2C19 inhibition.
- fludarabine
fludarabine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- fludrocortisone
fludrocortisone, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- fluorouracil
fluorouracil, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- fosamprenavir
fosamprenavir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- gemcitabine
gemcitabine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- gold sodium thiomalate
gold sodium thiomalate, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- hydrocortisone
hydrocortisone, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- hydroxychloroquine sulfate
hydroxychloroquine sulfate, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- hydroxyurea
hydroxyurea, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- idecabtagene vicleucel
tofacitinib, idecabtagene vicleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- idelalisib
idelalisib will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrates
- ifosfamide
ifosfamide, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid use in combination with potent immunosuppressants; concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted. Agents considered as potent immunosuppressants are not specified, but lower corticosteroid doses (ie, equivalent to prednisone 10 mg/day or less), leflunomide, and antirheumatic doses of methotrexate were permitted in clinical studies.
ifosfamide will increase the level or effect of tofacitinib by Other (see comment). Avoid or Use Alternate Drug. Avoid use in combination with potent immunosuppressants; concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted. Agents considered as potent immunosuppressants are not specified, but lower corticosteroid doses (ie, equivalent to prednisone 10 mg/day or less), leflunomide, and antirheumatic doses of methotrexate were permitted in clinical studies. - imatinib
imatinib increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- indinavir
indinavir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- infliximab
infliximab, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- isoniazid
isoniazid increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- itraconazole
itraconazole increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- ivosidenib
ivosidenib will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternative therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.
- ketoconazole
ketoconazole increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay (psoriatic arthritis and rheumatoid arthritis) when coadministered with potent CYP3A4 inhibitors. Refer to prescribing information for other indications. .
- leflunomide
leflunomide, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- levoketoconazole
levoketoconazole increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay (psoriatic arthritis and rheumatoid arthritis) when coadministered with potent CYP3A4 inhibitors. Refer to prescribing information for other indications. .
- lisocabtagene maraleucel
tofacitinib, lisocabtagene maraleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- lomustine
lomustine will increase the level or effect of tofacitinib by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid use in combination with potent immunosuppressants; concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted. Agents considered as potent immunosuppressants are not specified, but lower corticosteroid doses (ie, equivalent to prednisone 10 mg/day or less), leflunomide, and antirheumatic doses of methotrexate were permitted in clinical studies.
- lonafarnib
lonafarnib will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration with sensitive CYP3A substrates. If coadministration unavoidable, monitor for adverse reactions and reduce CYP3A substrate dose in accordance with product labeling.
lonafarnib will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Lonafarnib may increase the AUC and peak concentration of CYP2C19 substrates. If coadministration unavoidable, monitor for adverse reactions and reduce the CYP2C19 substrate dose in accordance with its approved product labeling. - lopinavir
lopinavir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- mechlorethamine
mechlorethamine will increase the level or effect of tofacitinib by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid use in combination with potent immunosuppressants; concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted. Agents considered as potent immunosuppressants are not specified, but lower corticosteroid doses (ie, equivalent to prednisone 10 mg/day or less), leflunomide, and antirheumatic doses of methotrexate were permitted in clinical studies.
- mechlorethamine topical
mechlorethamine topical, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- melphalan
melphalan will increase the level or effect of tofacitinib by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Avoid use in combination with potent immunosuppressants; concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted. Agents considered as potent immunosuppressants are not specified, but lower corticosteroid doses (ie, equivalent to prednisone 10 mg/day or less), leflunomide, and antirheumatic doses of methotrexate were permitted in clinical studies.
- mercaptopurine
mercaptopurine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- methotrexate
methotrexate, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- methylprednisolone
methylprednisolone, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- mitoxantrone
mitoxantrone, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- muromonab CD3
muromonab CD3, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- mycophenolate
mycophenolate, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- nefazodone
nefazodone increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- nelarabine
nelarabine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- nelfinavir
nelfinavir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- nicardipine
nicardipine increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- oxaliplatin
oxaliplatin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- pemetrexed
pemetrexed, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- pentostatin
pentostatin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- posaconazole
posaconazole increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- pralatrexate
pralatrexate, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- prednisolone
prednisolone, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- prednisone
prednisone, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- procarbazine
procarbazine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted. Agents considered as potent immunosuppressants are not specified, but lower corticosteroid doses (ie, equivalent to prednisone 10 mg/day or less), leflunomide, and antirheumatic doses of methotrexate were permitted in clinical studies.
- quinidine
quinidine increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- ribociclib
ribociclib will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ritonavir
ritonavir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- ropeginterferon alfa 2b
ropeginterferon alfa 2b, tofacitinib. Either increases toxicity of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Myelosuppressive agents can produce additive myelosuppression. Avoid use and monitor patients receiving the combination for effects of excessive myelosuppression.
- saquinavir
saquinavir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- sirolimus
sirolimus, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- streptozocin
streptozocin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- tacrolimus
tacrolimus, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- temozolomide
temozolomide, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- temsirolimus
temsirolimus, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- thioguanine
thioguanine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- thiotepa
thiotepa, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- tipranavir
tipranavir increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- tisagenlecleucel
tofacitinib, tisagenlecleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- triamcinolone acetonide injectable suspension
triamcinolone acetonide injectable suspension, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- tucatinib
tucatinib will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.
- upadacitinib
tofacitinib, upadacitinib. Either increases effects of the other by immunosuppressive effects; risk of infection. Contraindicated.
- valrubicin
valrubicin, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- vinblastine
vinblastine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- vincristine
vincristine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- vincristine liposomal
vincristine liposomal, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- vinorelbine
vinorelbine, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- voriconazole
voriconazole increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Reduce tofacitinib dose to 5 mg qDay when coadministered with potent CYP3A4 inhibitors.
- voxelotor
voxelotor will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.
Monitor Closely (77)
- amiodarone
amiodarone increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- aprepitant
aprepitant increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- bicalutamide
bicalutamide increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- bosentan
bosentan will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
- cannabidiol
cannabidiol will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider reducing the dose of sensitive CYP2C19 substrates, as clinically appropriate, when coadministered with cannabidiol.
- carbamazepine
carbamazepine will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
- cenobamate
cenobamate will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider a dose reduction of CYP2C19 substrates, as clinically appropriate, when used concomitantly with cenobamate.
- cimetidine
cimetidine increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
cimetidine increases levels of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with potent CYP2C19 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors . - crizotinib
crizotinib increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- cyclosporine
cyclosporine increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- dabrafenib
dabrafenib will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
- desipramine
desipramine increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- dexamethasone
dexamethasone will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
- diltiazem
diltiazem increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- doxycycline
doxycycline increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- dronedarone
dronedarone increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- duvelisib
duvelisib will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration with duvelisib increases AUC of a sensitive CYP3A4 substrate which may increase the risk of toxicities of these drugs. Consider reducing the dose of the sensitive CYP3A4 substrate and monitor for signs of toxicities of the coadministered sensitive CYP3A substrate.
- efavirenz
efavirenz increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers.
- elagolix
elagolix will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak CYP2C19 inhibitor. Caution with sensitive CYP2C19 substrates.
elagolix decreases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed. - encorafenib
encorafenib, tofacitinib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.
- enzalutamide
enzalutamide will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
- erythromycin base
erythromycin base increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- erythromycin ethylsuccinate
erythromycin ethylsuccinate increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- erythromycin lactobionate
erythromycin lactobionate increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- erythromycin stearate
erythromycin stearate increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
eslicarbazepine acetate will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. - etravirine
etravirine will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
- fedratinib
fedratinib will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.
fedratinib will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP2C19 substrates as necessary. - fexinidazole
fexinidazole will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.
- fluconazole
fluconazole increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
fluconazole increases levels of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with potent CYP2C19 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors . - fluvoxamine
fluvoxamine increases levels of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Decrease tofacitinib dose is coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- fosaprepitant
fosaprepitant increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- fosphenytoin
fosphenytoin will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
- gemfibrozil
gemfibrozil increases levels of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with potent CYP2C19 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .
- grapefruit
grapefruit increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- haloperidol
haloperidol increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- iloperidone
iloperidone increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- isoniazid
isoniazid increases levels of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with potent CYP2C19 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .
- istradefylline
istradefylline will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.
- lapatinib
lapatinib increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- lenacapavir
lenacapavir will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lencapavir may increase CYP3A4 substrates initiated within 9 months after last SC dose of lenacapavir, which may increase potential risk of adverse reactions of CYP3A4 substrates.
- lidocaine
lidocaine increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- lorlatinib
lorlatinib will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lumacaftor/ivacaftor
lumacaftor/ivacaftor, tofacitinib. affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. In vitro studies suggest that lumacaftor may induce and ivacaftor may inhibit CYP2C19 substrates. .
- metronidazole
metronidazole increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- mifepristone
mifepristone will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If coadministration necessary, reduce dose of tofacitinib if chronic mifepristone therapy used; reduce to 5 mg twice daily in patients receiving 10 mg twice daily; reduce to 5 mg once daily in patients receiving 5 mg twice daily; change to 11 mg XR once daily in patients receiving 22 mg once daily of XR formulation; change to immediate-release formulation at dose of 5 mg once daily in patients receiving 11 mg XR once daily
- mitotane
mitotane decreases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Mitotane is a strong inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4 substrates for possible dosage adjustments.
- modafinil
modafinil increases levels of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with potent CYP2C19 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .
- nafcillin
nafcillin will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
- nevirapine
nevirapine will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
- ocrelizumab
tofacitinib and ocrelizumab both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Coadministration of ocrelizumab with immunosuppressants may increase the risk of immunosuppression.
- ofatumumab SC
ofatumumab SC, tofacitinib. Either increases effects of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Consider the risk of additive immune system effects when coadministering immunosuppressive therapies with coadministration. When switching from therapies with immune effects, take into account the duration and mechanism of action of these therapies when initiating ofatumumab SC.
- omeprazole
omeprazole increases levels of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with potent CYP2C19 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .
- oxcarbazepine
oxcarbazepine will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
- pentobarbital
pentobarbital will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
- phenobarbital
phenobarbital will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
- phenytoin
phenytoin will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
- primidone
primidone will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
- rifabutin
rifabutin will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
- rifampin
rifampin will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
- rifapentine
rifapentine will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
- rucaparib
rucaparib will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP2C19 substrates, if clinically indicated.
- sertraline
sertraline increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors.
- siponimod
siponimod and tofacitinib both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.
- sparsentan
sparsentan will decrease the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Sparsentan (a CYP2C19 inducer) decreases exposure of CYP2C19 substrates and reduces efficacy related to these substrates.
- St John's Wort
St John's Wort will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Loss of, or decreased response to tofacitinib may occur when coadministered with potent CYP3A4 inducers
- stiripentol
stiripentol, tofacitinib. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.
stiripentol will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider reducing the dose of CYP2C19 substrates, if adverse reactions are experienced when administered concomitantly with stiripentol. - tecovirimat
tecovirimat will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Tecovirimat is a weak inhibitor of CYP2C8 and CYP2C19. Monitor for adverse effects if coadministered with sensitive substrates of these enzymes.
tecovirimat will decrease the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered. - tetracycline
tetracycline increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .
- ticagrelor
ticagrelor increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .
- ticlopidine
ticlopidine increases levels of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with potent CYP2C19 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .
- trastuzumab
trastuzumab, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .
- trastuzumab deruxtecan
trastuzumab deruxtecan, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .
- triclabendazole
triclabendazole will increase the level or effect of tofacitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. If plasma concentrations of the CYP2C19 substrates are elevated during triclabendazole, recheck plasma concentration of the CYP2C19 substrates after discontinuation of triclabendazole.
- ublituximab
ublituximab and tofacitinib both increase immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Owing to potential additive immunosuppressive effects, consider duration of effect and mechanism of action of these therapies if coadministered
- verapamil
verapamil increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .
- zileuton
zileuton increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .
Minor (4)
- acetazolamide
acetazolamide will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- anastrozole
anastrozole will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- cyclophosphamide
cyclophosphamide will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- larotrectinib
larotrectinib will increase the level or effect of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
Adverse Effects
>10%
UC
- Nasopharyngitis (10-14%)
1-10%
RA
- Upper respiratory tract infection (4%)
- Nasopharyngitis (3-4%)
- Diarrhea (3-4%)
- Headache (3-4%)
- Hypertension (2%)
UC
- Elevated cholesterol levels (5-9%)
- Headache (3-9%)
- Upper respiratory tract infection (6-7%)
- Increased blood creatine phosphokinase (3-7%)
- Rash (3-6%)
- Diarrhea (2-5%)
- Herpes zoster (1-5%)
- Gastroenteritis (3-4%)
- Anemia (2-4%)
- Nausea (1-4%)
Frequency Not Defined
RA
- 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 rheumatoid arthritis 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
Postmarketing Reports
Immune system disorders: Drug hypersensitivity
Warnings
Black Box Warnings
Serious infections
- Increased risk for developing serious infections that may lead to hospitalization or death; most patients who developed these infections were taking concomitant immunosuppressants (eg, methotrexate, corticosteroid)
- If serious infection develops, interrupt until infection controlled
- Reported infections include active tuberculosis (TB), invasive fungal infections, and bacterial, viral, or other opportunistic pathogens
- Test for latent TB before and during tofacitinib treatment; treatment for latent TB infection should be initiated prior to tofacitinib treatment
Malignancies
- Malignancies, including lymphoma and solid tumors, reported
- Lymphomas and lung cancers observed at a higher rate in patients with RA treated with 5-10 mg BID compared with those treated with TNF blockers; patients who are current or past smokers are at additional increased risk
- Epstein Barr virus-associated post-transplant lymphoproliferative disorder has been observed at an increased rate in renal transplant patients treated with tofacitinib and concomitant immunosuppressive medications
Mortality
- A higher rate of all-cause mortality, including sudden cardiovascular death, reported in RA patients ≥50 years with at least 1 cardiovascular risk factor treated with 5 or 10 mg BID compared to those treated with TNF blockers
- Xeljanz 5 or 10 mg BID or Xeljanz XR 22 mg qDay NOT recommended for treatment of RA or PsA
Major adverse cardiovascular events
- Patients with RA aged ≥50 years with at least 1 CV risk factor treated with 5 or 10 mg BID had a higher rate of major adverse cardiovascular events (eg, cardiovascular death, myocardial infarction, stroke)
- Patients who are current or past smokers are at additional increased risk
- Discontinue treatment in patients that have experienced a myocardial infarction or stroke
Increased risk of blood clots
- Thrombosis, including pulmonary embolism, deep venous thrombosis, and arterial thrombosis have occurred in patients treated with Janus kinase inhibitors used to treat inflammatory conditions
- Patients with RA aged ≥50 years with at least 1 CV risk factor treated with 5 or 10 mg BID showed an increased incidence of thrombosis compared with TNF blockers
- Avoid in patients at risk
- Discontinue therapy and promptly evaluate patients with thrombosis symptoms
- For UC patients, use lowest effective dose and for shortest duration needed to achieve/maintain therapeutic response
Contraindications
None
Cautions
Malignancy and lymphoproliferative disorders reported (see Black Box Warnings); malignancies were observed in clinical studies and the postmarketing setting, including, but not limited to, lung cancer, breast cancer, melanoma, prostate cancer, and pancreatic cancer
GI perforation reported, although role of JAK inhibition in these events is unknown; caution in patients at increased risk for gastrointestinal perforation (eg, diverticulitis)
Associated with gradual decrease in lymphocyte and neutrophils counts, and hemoglobin levels that may require treatment interruption
Associated with increased LFTs
Associated with increase lipid parameters including total cholesterol, LDL, and HDL
Viral reactivation, including cases of herpes virus reactivation (eg, herpes zoster), reported; hepatitis B reactivation reported; impact on chronic viral hepatitis reactivation unknown; perform screening for viral hepatitis in accordance with clinical guidelines before starting therapy
Non-melanoma skin cancers (NMSCs) reported; periodic skin examination recommended for patients at increased risk for skin cancer
Use caution when treating patients with diabetes; higher incidence of infection in diabetic population in general reported
Diverticulitis reported
Twice daily dosing of tofacitinib 10 mg or 11 mg tofacitinib XR not recommended in patients with rheumatoid arthritis or psoriatic arthritis
Rheumatoid arthritis patients ≥50 years of age with at least 1 cardiovascular (CV) risk factor treated with tofacitinib 10 mg BID had a higher rate of all-cause mortality
Thrombosis, including pulmonary embolism, deep venous thrombosis, and arterial thrombosis, have occurred
Higher rate of major adverse cardiovascular events (MACE; defined as cardiovascular death, myocardial infarction, and stroke) reported with another JAK inhibitor Vs TNF blockers in RA patients
Structural joint damage progression
- Radiographic response data from the ORAL Scan and ORAL Start studies evaluated the efficacy of tofacitinib on structural joint damage progression as measured by mean change from baseline in van der Heijde modified Total Sharp Score (mTSS) and its components, erosion score, and joint space narrowing (JSN) score
Serious infections
- Serious and sometimes fatal infections reported due to bacterial, mycobacterial, invasive fungal, viral, or other opportunistic pathogens; the most common serious infections reported have included pneumonia, cellulitis, herpes zoster, urinary tract infection, diverticulitis, and appendicitis
- In the UC population, treatment with 10 mg BID was associated with greater risk of serious infections compared with 5 mg BID; additionally, opportunistic herpes zoster infections (including meningoencephalitis, ophthalmologic, and disseminated cutaneous) were seen in patients who were treated with 10 mg twice daily
- Use caution in patients with a history of chronic lung disease, or in those who develop interstitial lung disease, as they may be more prone to infections
- Risk of infection may be higher with increasing degrees of lymphopenia; consideration should be given to lymphocyte counts when assessing individual patient risk of infection
- Avoid use in patients with an active, serious infection, including localized infections
-
Consider the risks and benefits of tofacitinib prior to initiating treatment
- Patients with chronic or recurrent infection
- Patients who have been exposed to tuberculosis
- Patients with a history of a serious or an opportunistic infection
- Patients who have resided or traveled in areas of endemic tuberculosis or endemic mycoses
- Patients with underlying conditions that may predispose them to infection
Extended-release tablet
- Patients may notice an inert tablet shell passing in the stool or via colostomy
- Caution when administering the extended-release tablet to patients with pre-existing severe gastrointestinal narrowing (pathologic or iatrogenic); rare reports of obstructive symptoms with strictures in association with the ingestion of other drugs utilizing a non-deformable extended release formulation
Increased risk of serious heart-related problems and cancer
- On September 1st, 2021, FDA is requiring revisions to the Boxed Warning for tofacitinib to include information about the risks of serious heart-related events, cancer, blood clots, and death
- Revisions are based on results from completed trial show a higher occurrence of serious heart-related events and cancer in tofacitinib-treated group (both doses) compared to TNF inhibitor-treated group; results also showed an increased risk of blood clots and death with lower doses of tofacitinib
- Consider the benefits and risks for the individual patient before initiating or continuing treatment, especially the following patients:
- Who are current or past smokers
- Who have other cardiovascular risk factors
- Who have developed a malignancy
- Who have a known malignancy other than a successfully treated nonmelanoma skin cancer
- Reserve JAK inhibitors (eg, tofacitinib) if patients have an inadequate response or intolerance to ≥1 TNF blockers
- Counsel patients about the benefits and risks of these medicines and advise them to seek emergency medical attention if they experience signs and symptoms of a heart attack, stroke, or blood clot
Drug interactions overview
- Tofacitinib is a CYP3A4 substrate and a minor CYP2C19 substrate
- Strong CYP3A4 inducers may decrease clinical response
- Decreased dose required if coadministered with strong CYP3A4 inhibitors, or moderate CYP3A4 inhibitors plus CYP2C19 inhibitors (see Dosage Modifications)
- Avoid coadministration with live virus vaccines
- Risk of added immunosuppression when tofacitinib is concomitantly used with potent immunosuppressive drugs (eg, azathioprine, tacrolimus, cyclosporine); combined use of multiple dose tofacitinib with potent immunosuppressants has not been studied in rheumatoid arthritis and psoriatic arthritis
Pregnancy & Lactation
Pregnancy
There is a pregnancy exposure registry that monitors pregnancy outcomes in women during pregnancy; patients can call the toll free number 1-877-311-8972
There are no adequate and well-controlled studies therapy in pregnant women
In the tofacitinib clinical development programs, birth defects and miscarriages were reported
Animal data
- Based on animal studies, tofacitinib has the potential to affect a developing fetus
- Feticidal and teratogenic effects were noted when pregnant rats and rabbits received tofacitinib during the period of organogenesis at exposures multiples of 146 times and 13 times the human dose of 5 mg BID, respectively
- In a peri and post-natal study in rats, tofacitinib resulted in reductions in live litter size, postnatal survival, and pup body weights at exposure multiples of approximately 73 times the human dose of 5 mg BID
- Based on findings in rats, females of reproductive potential taking tofacitinib may result in reduced fertility
Contraception
- Advise females of reproductive potential to use effective contraception during treatment and for >4 weeks after the last dose
- Advise females to inform their healthcare provider if they become pregnant, or if pregnancy is suspected, during treatment
Lactation
It is not known whether the drug is excreted in human milk
There are no data to assess effects of drug on breastfed child; drug is excreted in rat milk at concentrations higher than in maternal serum
Women should not breastfeed while treated; a decision should be made whether to discontinue breastfeeding or to discontinue therapy
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Janus kinases (JAKs) pathways inhibitor; JAK consists of a group of intracellular tyrosine kinases that transmit signals from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoieses and immune cell function
Within the signaling pathway, JAKs phosphorylate and activate signal transducers and activators of transcription (STATs) which modulate intracellular activity including gene expression; tofacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs
These signals are essential in maintaining the inflammatory condition in rheumatoid arthritis (RA); inhibition of JAKs reduces production of and modulates proinflammatory cytokines central to RA
Absorption
Bioavailability
- Xeljanz: 74%
Minimum plasma concentration
- Xeljanz: 1.41-3.1 ng/mL
- Xeljanz XR: 1.07-3.11 ng/mL
Peak plasma concentration
- Xeljanz: 42.7-84.7 ng/mL
- Xeljanz XR: 38.2-83.8 ng/mL
Peak plasma time
- Xeljanz or oral solution: 0.5-1 hr
- Xeljanz XR: 4 hr
AUC
- Xeljanz: 263.4-539.6 ng⋅hr/mL
- Xeljanz XR: 269-596.6 ng⋅hr/mL
Steady-state reached
- Xeljanz or oral solution: 24-48 hr
- Xeljanz XR: 48 hr
Distribution
Protein Bound: ~40% (predominately to albumin)
Vd: 87 L (following IV administration)
Distributes equally between RBCs and plasma
Metabolism
Clearance mechanisms: ~70% hepatic metabolism and 30% renal excretion
Primarily metabolized by CYP3A4 (accounting for ~53% of total clearance) and by CYP2C19 (accounting for ~17% of total clearance)
Metabolites: Potency <10% of parent compound
Elimination
Renal clearance: 30%
Excretion: 30% urine
Half-life
- Xeljanz or oral solution: 0.8-1 hr
- Xeljanz XR: 4 hr
Administration
Oral Administration
May take with or without food
Extended-release tablets: Swallow whole; do not crush, split, or chew
Switching from regular tablets to extended-release tablets
Patients treated with tofacitinib 5 mg BID may switch to tofacitinib ER 11 mg qDay the day following the last dose of tofacitinib 5 mg
Patients treated with tofacitinib 10 mg BID may switch to tofacitinib 22 mg qDay the day following the last dose of tofacitinib 10 mg
Storage
Xeljanz or Xeljanz ER: Store at 20-25ºC (68-77ºF)
Oral solution
- Store at room temperature 20-25ºC (68-77ºF) in the original bottle and carton to protect from light
- Safely throw away solution that is out of date or no longer needed
- Use within 60 days of opening bottle; discard remaining oral solution after 60 days
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Xeljanz XR oral - | 11 mg tablet |  | |
| Xeljanz oral - | 10 mg tablet |  | |
| Xeljanz oral - | 5 mg tablet |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
tofacitinib oral
TOFACITINIB EXTENDED-RELEASE - ORAL
(TOE-fa-SYE-ti-nib)
COMMON BRAND NAME(S): Xeljanz XR
WARNING: Tofacitinib may lower your ability to fight infections. This may make you more likely to get a serious (rarely fatal) infection or make any infection you have worse. The most common serious infections include pneumonia, skin infections, shingles, a certain bowel disease (diverticulitis), swelling of the appendix (appendicitis), and urinary tract infections. The risk for infections may be higher if you also take other drugs that suppress the immune system (such as cyclosporine, tacrolimus). Tell your doctor right away if you have any signs of infection (such as a sore throat that doesn't go away, fever, chills, cough, trouble breathing, painful/frequent urination, non-healing skin sores).You should have a tuberculosis (TB) skin test before and during treatment with this medication. Tell your doctor if you have been near someone with tuberculosis or have lived or traveled in areas where certain fungal infections (such as coccidioidomycosis, histoplasmosis) are common. These areas include the Ohio and Mississippi River valleys and the southwestern United States.Though it is very unlikely to occur, there may be a risk of developing cancer (such as lymphoma, skin cancer, lung cancer) with this medication. Your risk may be higher if you are a current or past smoker. Tell your doctor right away if you develop symptoms such as fever or cough that doesn't go away, wheezing, unusual lumps/growths, unexplained weight loss, night sweats, change in appearance or size of moles, or unusual skin changes.Tofacitinib may cause serious (possibly fatal) blood clots in the lungs or legs, or clots that cause a stroke or heart attack. You may be at an increased risk for blood clots if you are a current or past smoker, or are 50 years of age or older and have at least one risk factor for heart disease. Discuss the risks and benefits of treatment with your doctor. Get medical help right away if you have symptoms of blood clots, such as shortness of breath/rapid breathing, chest/jaw/left arm pain, unusual sweating, confusion, sudden dizziness/fainting, pain/swelling/warmth in the groin/calf, sudden/severe headaches, trouble speaking, weakness on one side of the body, or sudden vision changes.People with a kidney transplant who are also taking other drugs that suppress the immune system may be at greater risk for developing a certain white blood cell disorder (Epstein Barr Virus-associated post-transplant lymphoproliferative disorder) with this medication. Discuss the risks and benefits of treatment with your doctor.
USES: Tofacitinib is used to treat certain types of arthritis (such as psoriatic arthritis, rheumatoid arthritis, ankylosing spondylitis). It helps to decrease pain/tenderness/swelling in the joints. Tofacitinib is also used to treat a certain bowel disease (ulcerative colitis). It helps to reduce symptoms of ulcerative colitis such as diarrhea, rectal bleeding, and stomach pain.
HOW TO USE: Read the Medication Guide provided by your pharmacist before you start taking tofacitinib and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with or without food as directed by your doctor, usually once daily. Swallow the tablets whole. Do not crush, split, or chew the tablets. Doing so can release all of the drug at once, increasing the risk of side effects.The dosage is based on your medical condition, response to treatment, lab tests, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products). Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of serious side effects will increase.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.Tell your doctor if your condition does not get better or if it gets worse.
SIDE EFFECTS: See also Warning section.Headache or diarrhea may occur. If either of these effects lasts or gets worse, tell your doctor or pharmacist promptly.An empty tablet shell may appear in your stool. This effect is harmless because your body has already absorbed the medication.People using this medication may have serious side effects. However, you have been prescribed this drug because your doctor has judged that the benefit to you is greater than the risk of side effects. Careful monitoring by your doctor may decrease your risk.Tell your doctor right away if you have any serious side effects, such as: unusual tiredness, fast heartbeat, signs of liver disease (such as nausea/vomiting that doesn't stop, loss of appetite, stomach/abdominal pain, yellowing eyes/skin, dark urine).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, such as: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: See also Warning section.Before taking tofacitinib, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: blood clots (such as in the lungs, legs), blood/bone marrow disorders (such as anemia, low lymphocyte/neutrophil count), cancer, heart problems (such as previous heart attack), kidney disease, liver disease (such as hepatitis B or C), lung disease, past/recent/current infections (such as tuberculosis, herpes zoster, HIV infection), current or past smoking, other stomach/intestinal disorders (such as ulcers, diverticulitis), stroke.Tofacitinib can make you more likely to get infections or may make current infections worse. Stay away from anyone who has an infection that may easily spread (such as chickenpox, COVID-19, measles, flu). Talk to your doctor if you have been exposed to an infection or for more details.Tell your health care professional that you are using tofacitinib before having any immunizations/vaccinations. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Older adults may be at greater risk for infections while using this drug.During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor. Tell your doctor if you are planning pregnancy or become pregnant.It is unknown if this medication passes into breast milk. However, because of the possible risk to the infant, breast-feeding while using this drug and for at least 36 hours after the last dose is not recommended. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: See also Warning section.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Other medications can affect the removal of tofacitinib from your body, which may affect how tofacitinib works. Examples include rifampin, among others.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: Do not share this medication with others.Lab and/or medical tests (such as liver/kidney function, complete blood count, cholesterol levels, skin exams) should be done while you are taking this medication. Keep all medical and lab appointments.
MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).
Information last revised March 2023. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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- View the formulary and any restrictions for each plan.
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