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Tofacitinib

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Tofacitinib, Xeljanz

  • See Also
  1. Janus Kinase Inhibitor
  • Indications
  1. Rheumatoid Arthritis (moderate to severe, refractory to non-biologic DMARD)
  2. Psoriatic Arthritis (moderate to severe, refractory to non-biologic DMARD)
  3. Ulcerative Colitis (moderate to severe, refractory to TNF agents)
  • Contraindications
  1. Severe hepatic Impairment
  2. Live Vaccines (including Herpes Zoster Vaccine)
  3. Concurrent Immunosuppressants
    1. Biologic DMARDs
    2. Cyclosporine, azathoprine and other potent Immunosuppressants
    3. Probenacid (OAT3 transport inhibitor)
  • Precautions
  1. Multiple FDA black box warnings
    1. Serious infections
    2. Thrombosis (e.g. Venous Thromboembolism)
    3. Cardiovascular events (e.g. Myocardial Infarction)
    4. Lung Cancer
    5. Increased mortality
  2. References
    1. (2021) Presc Lett 28(4): 22
  • Mechanism
  1. See Janus Kinase Inhibitor
  • Medications
  1. Tofacitinib (Xeljanz): 5 mg tablets
  2. Tofacitinib Extended Release (Xeljanz XR): 11 mg
    1. Do not cut, split or chew extended release tablets
  • Dosing
  • Adults
  1. Rheumatoid Arthritis or Psoriatic Arthritis
    1. Tofacitinib 5 mg orally twice daily
    2. Tofacitinib XR 11 mg orally once daily
    3. May be given with non-biologic DMARD
  2. Ulcerative Colitis
    1. Start induction: 10 mg orally twice daily for 8 weeks (up to 16 weeks)
    2. Maintenance: 5 mg orally twice daily (up to 10 mg orally twice daily in lower dose ineffective)
  3. Lower dose indications (decreasing frequency to once daily or decreasing dose to 50%)
    1. Strong CYP3A4 Inhibitor (e.g. Fluconazole, Carbamazepine, Phenobarbital, Phenytoin, Rifampin, St. Johns Wort)
    2. Moderate CYP3A4 Inhibitor AND Strong CYP2C19 Inhibitor
    3. Myelosuppression (lymphopenia, Neutropenia, Anemia)
    4. Moderate to severe renal Impairment (and dose after Hemodialysis)
    5. Moderate hepatic Impairment (avoid in severe hepatic Impairment)
  • Adverse Effects
  1. See Janus Kinase Inhibitor
  2. See precautions above
  3. Serious infections
  4. Opportunistic infections
  5. Major cardiovascular events
  6. Malignancy including Lymphoma
  7. Venous Thromboembolism
  8. Infection Reactivation (e.g. Tb reactivation, Hepatitis BVirus, Shingles reactivation)
    1. Screen for Latent Tuberculosis, Viral Hepatitis before starting
  9. Gastrointestinal perforation (esp. if history of Diverticulitis)
  10. Hepatotoxicity
  11. Hyperlipidemia
  12. Myelosuppression
    1. Lymphopenia
      1. Avoid starting if Absolute Lymphocyte Count (ALC) <500
      2. Stop if ALC <500
    2. Anemia
      1. Avoid starting if Hemoglobin <9 mg/dl
    3. Neutropenia
      1. Avoid starting if Absolute Neutrophil Count (ANC) <1000
      2. Stop if ANC <500
  • Safety
  1. Avoid in pregnancy (Unknown safety)
    1. Use reliable Contraception during and for at least 4 weeks after stopping Tofacitinib
  2. Avoid in Lactation
    1. Wait at least 4 days after last dose to begin Breast Feeding
  3. Monitoring (obtain baseline and recheck periodically every 3 months)
    1. Complete Blood Count
    2. Liver Function Tests
    3. Lipid panel (after 1-2 months of use)
  • Drug Interactions
  1. See Contraindications above
  2. Strong CYP3A4 Inhibitors
  3. Strong CYP2C19 Inhibitors
  • Resources
  1. Tofacitinib (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=68e3d6b2-7838-4d2d-a417-09d919b43e13