What is the starting dose of Xeljanz (tofacitinib) for rheumatoid arthritis?

Xeljanz Starting Dose for Rheumatoid Arthritis

For rheumatoid arthritis, start Xeljanz (tofacitinib) at 5 mg orally twice daily. 1

Dosing Recommendations

The FDA-approved starting dose for rheumatoid arthritis is 5 mg twice daily, taken orally. 1 This dose has been extensively studied across multiple Phase 3 trials and demonstrates significant efficacy in reducing signs and symptoms of RA while maintaining an acceptable safety profile 2.

Key Dosing Points:

• Standard dose: 5 mg twice daily (BID) for all RA patients 1
• Extended-release formulation: 11 mg once daily is an alternative option 2
• Higher dose NOT recommended: The 10 mg twice daily dose is specifically not recommended for RA treatment due to increased thromboembolic risk 2, 1

Clinical Context

The 5 mg twice daily dose has demonstrated:

• ACR20 response rates of 51.5-73.1% across multiple trials 2
• Significant improvements in HAQ-DI scores (mean changes of -0.40 to -0.44) 2
• Remission rates (DAS28-ESR <2.6) of 5-10% at 3 months and 7.2-8.5% at 6 months 2, 3

Administration Guidelines:

• Can be used as monotherapy or in combination with methotrexate or other conventional DMARDs 2, 1
• Should not be combined with potent immunosuppressants (azathioprine, cyclosporine) or biologics 2
• No food restrictions for administration 1

Dose Adjustments Required

Reduce to 5 mg once daily in the following situations 2:

• Moderate to severe renal impairment (CrCl 30-60 mL/min: use 5 mg once daily; CrCl <30 mL/min: use 5 mg once daily) 2
• Moderate to severe hepatic impairment (Child-Pugh B or C) 2
• Concomitant strong CYP3A4 inhibitors (e.g., ketoconazole) 2
• Concomitant moderate CYP3A4 inhibitors plus potent CYP2C19 inhibitors (e.g., fluconazole) 2

Critical Safety Considerations

Important contraindications and warnings that affect starting decisions 2:

• Screen for latent tuberculosis before initiating therapy 2
• Consider herpes zoster vaccination before starting, especially in patients >50-70 years 2
• Avoid in patients with active serious infections 2
• Use caution in elderly patients (≥65 years) with cardiovascular risk factors due to increased infection and thromboembolic risk 2

Common Pitfalls to Avoid:

• Do not start at 10 mg twice daily - this dose carries significantly increased risk of venous thromboembolism and pulmonary embolism without proportional benefit in RA 2
• Do not forget baseline monitoring: Complete blood count, liver function tests, lipid panel, and creatinine should be checked before starting 1
• Do not overlook drug interactions: Rifampicin increases metabolism requiring dose adjustment; strong CYP3A4 inhibitors require dose reduction 2

Efficacy Timeline

Patients can expect 2, 4:

• Initial response typically seen within 2-4 weeks
• Maximal benefit usually achieved by 3-6 months
• Sustained efficacy demonstrated up to 96 months in long-term studies 4, 5