Rheumatoid Arthritis: Tofacitinib is indicated for adult patients with moderate to severe rheumatoid arthritis who have shown inadequate response or intolerance to methotrexate. It can be used alone or in combination with methotrexate or other non-biologic DMARDs.

Psoriatic Arthritis: Tofacitinib is indicated for adult patients with active psoriatic arthritis who have had an inadequate response or intolerance to methotrexate or other DMARDs.

Ulcerative Colitis: Tofacitinib is indicated for the treatment of adult patients with moderately to severely active ulcerative colitis.

Rheumatoid arthritis is an autoimmune condition characterized by dysregulation of pro-inflammatory cytokines such as IL-7, IL-15, IL-21, IL-6, IFN-α, and IFN-β. These cytokines promote inflammation and joint damage by activating immune cells through the Janus kinase (JAK) signaling pathway.

Tofacitinib is a selective and reversible inhibitor of Janus kinase (JAK). It interferes with cytokine signaling by blocking JAK activity, thereby preventing phosphorylation and activation of STAT proteins. The JAK-STAT pathway plays a critical role in immune cell function and hematopoiesis. By inhibiting this pathway, tofacitinib reduces inflammatory responses and helps control disease activity. Additional mechanisms of action may also contribute to its therapeutic effects.

Rheumatoid Arthritis: Tofacitinib 5 mg twice daily or Tofacitinib 11 mg once daily. Recommended dosage in patients with moderate and severe renal impairment or moderate hepatic impairment is Tofacitinib 5 mg once daily.

Psoriatic Arthritis (in combination with nonbiologic DMARDs): Tofacitinib 5 mg twice daily or Tofacitinib 11 mg once daily. Recommended dosage in patients with moderate and severe renal impairment or moderate hepatic impairment is Tofacitinib 5 mg once daily.

Ulcerative Colitis: Tofacitinib 10 mg twice daily for at least 8 weeks; then 5 or 10 mg twice daily. Discontinue after 16 weeks of 10 mg twice daily, if adequate therapeutic benefit is not achieved. Use the lowest effective dose to maintain response.

• Potent CYP3A4 inhibitors (e.g., ketoconazole): The recommended dose is tofacitinib 5 mg once daily.
• Concomitant use of moderate CYP3A4 inhibitors with potent CYP2C19 inhibitors (e.g., fluconazole): The recommended dose is tofacitinib 5 mg once daily.
• Potent CYP inducers (e.g., rifampin): May reduce the effectiveness of tofacitinib and lead to diminished clinical response.

The most commonly reported adverse reactions during the first 3 months of controlled clinical trials (≥2%) include upper respiratory tract infections, headache, diarrhea, and nasopharyngitis.

Pregnancy: Category C. Adequate and well-controlled studies in pregnant women are not available. Tofacitinib should be used during pregnancy only if the potential benefit outweighs the potential risk to the fetus.

Lactation: It is not known whether tofacitinib is excreted in human milk. Due to the possibility of serious adverse reactions in nursing infants, a decision should be made to either discontinue breastfeeding or discontinue the drug, considering the importance of therapy to the mother.

• Serious infections: Avoid use in patients with active serious infections, including localized infections.
• Gastrointestinal perforations: Use with caution in patients at increased risk.
• Laboratory monitoring: Regular monitoring is recommended due to possible changes in lymphocytes, neutrophils, hemoglobin, liver enzymes, and lipid levels.
• Immunizations: Avoid administration of live vaccines during treatment.
• Do not initiate tofacitinib if absolute lymphocyte count is <500 cells/mm³, absolute neutrophil count (ANC) is <1000 cells/mm³, or hemoglobin is <9 g/dL.

Pediatric use: Safety and effectiveness have not been established in pediatric patients.

Geriatric use: Patients aged ≥65 years have a higher risk of serious infections compared to younger patients; therefore, caution is advised.

Renal and hepatic impairment: In patients with moderate to severe renal impairment or moderate hepatic impairment, the dose should be reduced to half of the usual daily dose.

Immunosuppressant

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