Baricitinib

Baricitinib Brand Name– OLUMIANT

What is Baricitinib

Baricitinib is an oral Janus kinase (JAK) inhibitor and is considered a targeted synthetic disease-modifying antirheumatic drug (tsDMARD).

Janus kinases are intracellular enzymes that transmit signals arising from cytokine interactions on the cellular membrane to influence cellular processes of immune cell function. JAK inhibitors have been shown useful for a variety of inflammatory conditions.

Baricitinib is indicated for adults with moderately to severely active rheumatoid arthritis (RA) who have had an inadequate response or intolerance to 1 or more tumor necrosis factor (TNF) inhibitors.

For patients with rheumatoid arthritis (RA), baricitinib is used as monotherapy or in combination with methotrexate or other non-biologic disease-modifying antirheumatic drugs (DMARDs).

Baricitinib improves RA symptoms and inhibits the radiographic progression of structural joint damage.

Guidelines for RA were published before the availability of baricitinib, but the drug, like other tsDMARDs, is usually reserved for patients with contraindications, intolerance, or inadequate response to biologic agents such as the TNF inhibitors.

The ideal combination of therapy for individual patients with inflammatory arthritis conditions such as RA is determined by treat to target strategies and severity of the disease.

The use of baricitinib does present some safety concerns. Serious infections and malignancy may be precipitated by JAK inhibitors; the drug is not to be used in combination with other JAK inhibitors, biologic DMARDs, or with potent immunosuppressants such as azathioprine and cyclosporine.

Also, JAK inhibitors have been associated with an increased risk of thrombosis.

How is baricitinib different from tofacitinib?

Baricitinib blocks both JAK1 and JAK2 with expected inhibition of cytokines and growth factors which depend on JAK1 and JAK2 (see Question 19). It is eliminated primarily by the kidney (75%) and thus dose adjustments should be made in patients with significant renal insufficiency (2 mg/day max if CrCl <60 mL/minute or patient on probenecid). Do not use in patients with CrCl <30 mL/minute. Half-life is 12.5 hours.

  • • FDA-approved indication: RA after failure of MTX and TNF inhibitor. Ex-US it is approved for RA without need to fail an anti-TNF.
  • • Available formulations: 2-mg tablet. Ex-US there is also a 4-mg tablet.
  • • Dosage: 2 mg QD. Ex-US can also use 4 mg QD. Not affected by food. Can be used alone or in combination with MTX.
  • • Cost (2 mg QD): $2150/month.
  • • Follow-up: same as tofacitinib.
  • • Adverse reactions, laboratory abnormalities, and precautions similar to tofacitinib. Notable differences were:
    • venous thromboembolism was numerically more common in patients receiving the 4-mg/day dose. Therefore, the FDA approved only the 2-mg/day dose for use in the United States. It should be noted that patients with RA have an increased risk of deep vein thrombosis (DVT)/pulmonary embolism (PE) (3–7/1000 ptyrs) regardless of therapy. However, baricitinib should be used with caution in patients with a prior history of DVT/PE or multiple risk factors.
    • Creatine kinase (CK) elevations: CK elevations >5× upper limit of normal (1.5% of patients on 4 mg/day; 0.8% of patients on 2 mg/day). No evidence of muscle weakness or rhabdomyolysis. Etiology unclear. CK usually improves without interruption of therapy.
    • Creatinine elevations not observed but need to monitor since baricitinib is excreted renally.

Indications

  • coronavirus disease 2019 (COVID-19)
  • rheumatoid arthritis
  • severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection

For the treatment of moderately to severely active rheumatoid arthritis in patients who have had an inadequate response to 1 or more tumor necrosis factor (TNF) antagonists

Side Effects

  1. abdominal pain
  2. acne vulgaris
  3. anemia
  4. candidiasis
  5. elevated hepatic enzymes
  6. GI perforation
  7. hepatotoxicity
  8. hypercholesterolemia
  9. hypertriglyceridemia
  10. infection
  11. laryngitis
  12. lymphoma
  13. lymphopenia
  14. nausea
  15. neutropenia
  16. new primary malignancy
  17. pharyngitis
  18. pulmonary embolism
  19. rhinitis
  20. sinusitis
  21. skin cancer
  22. thrombocytosis
  23. thromboembolism
  24. thrombosis
  25. tracheitis

Monitoring Parameters

  • CBC with differential
  • hemoglobin/hematocrit
  • LFTs
  • serum cholesterol profile
  • serum creatinine/BUN
  • skin cancer screening exam
  • tuberculin skin test

Contraindications

  • anemia
  • breast-feeding
  • children
  • corticosteroid therapy
  • diabetes mellitus
  • diverticulitis
  • fungal infection
  • geriatric
  • GI perforation
  • hepatic disease
  • hepatitis
  • hepatitis C infection
  • herpes infection
  • human immunodeficiency virus (HIV) infection
  • hypercholesterolemia
  • hyperlipidemia
  • immunosuppression
  • infants
  • infection
  • lymphoma
  • neutropenia
  • new primary malignancy
  • pregnancy
  • pulmonary disease
  • renal failure
  • renal impairment
  • skin cancer
  • thrombocytosis
  • thromboembolic disease
  • thromboembolism
  • thrombosis
  • tuberculosis
  • vaccination
  • viral infection

Interactions

  • Abatacept
  • Adalimumab
  • Anakinra
  • Azathioprine
  • Bacillus Calmette-Guerin Vaccine, BCG
  • Brodalumab
  • Canakinumab
  • Certolizumab pegol
  • Colchicine; Probenecid
  • Cyclosporine
  • Daclizumab
  • Etanercept
  • Golimumab
  • Guselkumab
  • Infliximab
  • Influenza Virus Vaccine
  • Intranasal Influenza Vaccine
  • Ixekizumab
  • Leflunomide
  • Live Vaccines
  • Measles Virus; Mumps Virus; Rubella Virus; Varicella Virus Vaccine, Live
  • Measles/Mumps/Rubella Vaccines, MMR
  • Probenecid
  • Rituximab
  • Rituximab; Hyaluronidase
  • Rotavirus Vaccine
  • Rubella Virus Vaccine Live
  • Sarilumab
  • Secukinumab
  • Smallpox and Monkeypox Vaccine, Live, Nonreplicating
  • Smallpox Vaccine, Vaccinia Vaccine
  • Teriflunomide
  • Tocilizumab
  • Tofacitinib
  • Tumor Necrosis Factor modifiers
  • Typhoid Vaccine
  • Upadacitinib
  • Ustekinumab
  • Varicella-Zoster Virus Vaccine, Live
  • Yellow Fever Vaccine, Live
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