Products
Tofacitinib was approved in the United States in November 2012, in many countries in 2013, and in the EU in 2017 in film-coated tablet form (Xeljanz). The European Medicines Agency initially rejected the approval in April 2013. However, baricitinib was approved. In the United States, additional sustained-release film-coated tablets are available that are taken once daily (Xeljanz XR).
Structure and properties
Tofacitinib (C16H20N6O, Mr = 312.4 g/mol) is a pyrrolopyrimidine and is present in drugs as tofacitinib citrate, a white powder that is highly soluble in water.
Effects
Tofacitinib (ATC L04AA29) has immunomodulatory, anti-inflammatory, and antiproliferative properties. The effects are due to inhibition of the Janus kinases JAK1, JAK2, and JAK3. These are intracellular enzymes involved in the signal transduction of cytokines and growth factors into the nucleus.
Indications
- Rheumatoid arthritis
- Psoriatic arthritis
- Ulcerative colitis
Dosage
According to the professional information. Tablets are taken twice daily, regardless of meals (XR: once daily).
Contraindications
- Hypersensitivity
- Active, severe infections
- Severe hepatic insufficiency
Full precautions can be found in the drug label.
Interactions
Tofacitinib is metabolized primarily by CYP3A4 and to a lesser extent by CYP2C19. Corresponding interactions with CYP inhibitors and CYP inducers are possible and must be considered during treatment. Side effects may be increased with concomitant administration of immunosuppressants.
Adverse effects
The most common potential adverse effects include headache, upper respiratory tract infection, nasopharyngitis, hypertension, nausea, and vomiting. Tofacitinib is immunosuppressive and therefore may promote the development of infectious diseases and cancers.
