Products
Baricitinib was approved in many countries and in the EU in 2017 and in the United States in 2018 in film-coated tablet form (Olumiant).
Structure and properties
Baricitinib (C16H17N7O2S, Mr = 371.4 g/mol) is structurally related to adenosine triphosphate and interacts with the ATP-binding site of kinases. It is sparingly soluble in water.
Effects
Baricitinib (ATC L04AA37) has anti-inflammatory, immunomodulatory, and antiproliferative properties. The effects are due to selective and reversible inhibition of Janus kinases 1 and 2 (JAK). These are intracellular enzymes involved in the signal transduction of cytokines and growth factors into the nucleus. The half-life is approximately 13 hours.
Indications
For combination therapy of moderate-to-severe active rheumatoid arthritis as a 2nd-line agent.
Dosage
According to the SmPC. Tablets are taken once daily, independent of meals.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Baricitinib is a substrate of CYP3A4, but this does not appear to be clinically relevant. The drug is also a substrate of OAT3, P-glycoprotein, BCRP, and MATE2-K.
Adverse effects
The most common potential adverse effects include an increase in LDL cholesterol, upper respiratory tract infections, and nausea.
