Products
Upadacitinib was approved in the US and EU in 2019 and in many countries in 2020 in extended-release tablet form (Rinvoq sustained-release tablets).
Structure and properties
Upadacitinib (C17H19F3N6O, Mr = 380.4 g/mol) exists in the drug as a hemihydrate.
Effects
Upadacitinib has selective immunosuppressive and anti-inflammatory properties. The effects are due to selective and reversible inhibition of Janus kinases (JAK) and JAK1 in particular. Janus kinases are intracellular enzymes involved in cytokine and growth factor signal transduction. The half-life is in the range of 9 to 14 hours.
Indications
For the treatment of rheumatoid arthritis.
Dosage
According to the SmPC. Tablets are taken once daily, regardless of meals.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Upadacitinib is metabolized predominantly by CYP3A4 and to a lesser extent by CYP2D6. Drug-drug interactions have been described with potent inhibitors and inducers of CYP344.
Adverse effects
The most common potential adverse effects include upper respiratory tract infections, nausea, cough, and elevation of creatine phosphokinase (CPK) in the blood. Because of its immunosuppressive properties, upadacitinib may promote the development of infectious diseases.
