Baricitinib

Baricitinib is a selective and reversible JAK1 and JAK2 inhibitor used for the treatment of moderate to severely active rheumatoid arthritis in adult patients who have had an inadequate response to one or more TNF antagonist therapies. It may be used as monotherapy or in combination with methotrexate or other non-biologic DMARDs.

Baricitinib modulates signaling pathways by partially inhibiting JAK1 and JAK2 enzymatic activity, thereby reducing the phosphorylation and activation of STATs, which decreases inflammation and joint damage.

Common side effects include upper respiratory tract infections, nausea, and increased LDL cholesterol. Serious risks include infections, thrombosis, and gastrointestinal perforation.

• Moderate to severely active rheumatoid arthritis in adult patients who have had an inadequate response to one or more TNF antagonist therapies

Baricitinib is a selective and reversible inhibitor of Janus kinase JAK1 and JAK2. Janus kinases (JAKs) are enzymes that transduce intracellular signals from cell surface receptors for a number of cytokines and growth factors involved in haematopoiesis, inflammation and immune function. Within the intracellular signalling pathway, JAKs phosphorylate and activate signal transducers and activators of transcription (STATs), which activate gene expression within the cell. Baricitinib modulates these signaling pathways by partially inhibiting JAK1 and JAK2 enzymatic activity, thereby reducing the phosphorylation and activation of STATs.

Baricitinib inhibits JAK1 and JAK2 enzyme activity, regulating cytokine-mediated signaling pathways. JAK enzymes phosphorylate STAT proteins, which enter the nucleus and regulate gene expression. Baricitinib inhibits this process, reducing pro-inflammatory cytokine production and inflammation, thereby decreasing symptoms of rheumatoid arthritis.

Recommended dose: 2 mg once daily, orally.

Administration: May be taken with or without food. Can be used alone or in combination with methotrexate or other DMARDs.

Renal impairment: Not recommended if eGFR <60 mL/min/1.73 m².

Hepatic impairment: No dose adjustment needed in mild to moderate hepatic impairment.

Elderly: Caution in dose selection due to increased likelihood of decreased renal function.

Take this medicine in the dose and duration as advised by your doctor. Swallow the tablet whole; do not chew, crush, or break. May be taken with or without food, but take at a fixed time.

If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and continue with your regular schedule. Do not double the dose.

• Upper respiratory tract infections (14.7%)
• Nausea (2.8%)
• Increased LDL cholesterol (33.6%)
• Viral infections
• Cold sores

Serious (rare): Serious infections, tuberculosis (TB), thrombosis, gastrointestinal perforation, malignancy

• Avoid use in active serious infections
• Perform TB skin test and chest X-ray before starting
• Inform doctor if symptoms of infection (fever, chills, cough, muscle aches) occur
• Caution in patients at risk of thrombosis
• Caution in patients at risk of gastrointestinal perforation
• Do not initiate/interrupt if hemoglobin <8 g/dL
• Do not initiate/interrupt if Absolute Lymphocyte Count <500 cells/mm³
• Do not initiate/interrupt if Absolute Neutrophil Count <1000 cells/mm³

• Hemoglobin <8 g/dL
• Absolute Lymphocyte Count <500 cells/mm³
• Absolute Neutrophil Count <1000 cells/mm³
• Active serious infection
• Active tuberculosis (TB)
• Pregnancy

• Strong OAT3 inhibitors (e.g., probenecid): Increase baricitinib systemic exposure
• Other JAK inhibitors or biologic DMARDs: Not studied in combination
• Live vaccines: Avoid use; update immunizations before initiating therapy

[SAFE] Consuming alcohol with Baricitinib does not cause any harmful side effects. However, caution is advised.

[CONSULT YOUR DOCTOR] Baricitinib is unsafe during pregnancy (Category D). There is definite evidence of risk to the developing baby. Animal studies have shown harmful effects on the fetus.

[CONSULT YOUR DOCTOR] No information is available on the presence of baricitinib in human milk. Limited human data suggests that the drug may pass into breastmilk and harm the baby. Avoid use in nursing mothers.

Safety and effectiveness in pediatric patients (under 18 years) have not been established.

Elderly patients are more likely to have decreased renal function, so care should be taken in dose selection.

[UNSAFE] Not recommended for use in patients with eGFR <60 mL/min/1.73 m².

[SAFE IF PRESCRIBED] Safe in liver disease. No dose adjustment needed in mild to moderate hepatic impairment. Caution in severe liver disease due to limited information.

In case of overdose, monitor the patient for signs and symptoms of adverse reactions. Patients who develop adverse reactions should receive appropriate treatment.

Store at or below 30°C. Keep away from light and moisture. Keep out of reach of children.

Baricitinib