Adult Dosing

Moderate-to-severe active rheumatoid arthritis

• 5mg PO bid

Note:

• Used as monotherapy or in combination with methotrexate or disease modifying antirheumatic drugs (DMARDs)
• Refer package insert for dose modification information

Pediatric Dosing

• Safety and effectiveness in pediatric patients has not been established

[Outline]

• Adult Dosing
• Pediatric Dosing

• Treatment of moderate-to-severe active rheumatoid arthritis in patients with refractory response to methotrexate. It may be used as monotherapy or in combination with methotrexate or other nonbiologic DMARDs

Note:

• Should not be used in combination with biologic DMARDs or potent immunosuppressive agents (eg, azathioprine, cyclosporine)

• Hypersensitivity to any of the ingredients of the product
• Concurrent live vaccination
• Severe hepatic impairment
• Hgb baseline <9
• Lymphocytes Baseline <500
• Baseline ANC <1000
• Active infection

• Increased risk of developing serious infections such as pulmonary and extrapulmonary tuberculosis, invasive fungal infections, and other opportunistic infections leading to hospitalization or death have been reported in patients treated with tofacitinib. Infection was more common in patients who were on concomitant immunosuppressants such as methotrexate or corticosteroids. Discontinue the treatment if serious infection develops and resume once the infection is controlled
• Closely monitor all the patients for signs and symptoms of infection during and after treatment, including those with possible development of tuberculosis, who were tested negative for latent tuberculosis infection before starting treatment
• Invasive fungal infections, including cryptococcosis and pneumocystosis and other bacterial, viral, and other infections due to opportunistic pathogens may occur with tofacitinib
• Consider risk and benefits prior to therapy with chronic or recurrent infection
• Lymphoma and other malignancies are reported in patients receiving tofacitinib. Increased rate of Epstein-Barr virus-associated post transplant lymphoproliferative disorder has been observed in renal transplant patients treated with concomitant immunosuppressive medications

Renal Dose Adjustment

• Moderate-severe impairment: 5 mg PO qd

Hepatic Dose Adjustment

• Moderate impairment: 5 mg PO qd
• Severe impairment: Avoid use

• Serious and fatal infections due to bacterial, mycobacterial, invasive fungal, viral, or other opportunistic pathogens have been reported with therapy. Pneumonia, cellulitis, herpes zoster and urinary tract infection were most common serious infections
• Opportunistic infections such as tuberculosis cryptococcus, esophageal candidiasis, pneumocystosis, multidermatomal herpes zoster, cytomegalovirus, and BK virus were reported with tofacitinib
• Closely monitor all the patients for signs and symptoms of infection during and after treatment, including those with possible development of tuberculosis, who were tested negative for latent tuberculosis infection before starting treatment
• Consider risk and benefits prior to therapy with chronic or recurrent infection
• Lymphoma and other malignancies are reported in patients receiving tofacitinib. Increased rate of Epstein-Barr virus-associated post transplant lymphoproliferative disorder has been observed in renal transplant patients treated with concomitant immunosuppressive medications
• Gastrointestinal perforation has been reported with tofacitinib. Use cautiously in patients who are at increased risk for gastrointestinal perforation. Evaluate patients who have abdominal symptoms for early identification of gastrointestinal perforation
• Therapy is not recommended in patients with a low lymphocyte count (<500 cells/mm³, neutrophil count, and hemoglobin level. Monitor CBC at baseline and every 3 months thereafter
• Consider routine monitoring of liver tests in patients receiving tofacitinib. Lipid parameters should be monitored 4-8 weeks following initiation of therapy
• Avoid live vaccines concurrently with tofacitinib

Cautions: Use cautiously in:

• Elderly patients
• Risk for gastrointestinal perforation
• Malignancy
• HBV or HCV carrier
• History of herpes zoster
• Risk to TB
• Chronic or recurrent infection
• Opportunistic infection
• Renal impairment
• Hepatic impairment

Pregnancy Category:C

Breastfeeding: It is unknown whether tofacitinib is excreted in human milk. Because many drugs are excreted in human milk and potential for serious adverse reactions in nursing infants from tofacitinib, a decision should be made whether to discontinue nursing or drug, taking into account the importance of the drug for the mother

• CNS: Headache
• RESP: Pneumonia, tuberculosis, upper respiratory tract infections
• GI: Diarrhea, GI perforation
• DERM: Cellulitis, herpes zoster
• GU: Urinary tract infection
• EENT: Nasopharyngitis
• LABTEST: Neutropenia, lymphopenia

• Janus kinase (JAK) pathways inhibitor; which transmit signals arising from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoiesis and immune cell function
• Metabolized by liver: CYP450: 3A4 and 2C19
• Excretion in urine (30%)
• Half-life: approximately 3 hrs

US Trade Name(s)

• Xeljanz

US Availability

Xeljanz (tofacitinib)

• TABS: 5 mg

Canadian Trade Name(s)

• N/A

Canadian Availability

• N/A

UK Trade Name(s)

• N/A

UK Availability

• N/A

Australian Trade Name(s)

• N/A

Australian Availability

• N/A

[Outline]