Products
Ruxolitinib was approved in tablet form in the United States in 2011 and in the EU and Switzerland in 2012 (Jakavi).
Structure and properties
Ruxolitinib (C17H21N6O4P, Mr = 404.4 g/mol) is present in drugs as ruxolitinib phosphate, a white to light pink powder that is soluble in water. It is a pyrrolopyrimidine pyrazole derivative and an ATP mimetic.
Effects
Ruxolitinib (ATC L01XE18) has antiproliferative properties. The effects are due to inhibition of mutant Janus kinases (JAK), which are involved in disease development. Ruxolitinib is selective for JAK1 and JAK2.
Indications
- Myelofibrosis
- Polycythaemia vera
Off-label use:
- In 2020, ruxolitinib was investigated for the treatment of the new coronavirus disease Covid-19.
Dosage
According to the drug label. The tablets are administered twice daily, regardless of meals.
Contraindications
- Hypersensitivity
- In particular, it must be taken into account that ruxolitinib can induce changes in blood counts and promote infections.
Full precautions can be found in the drug label.
Interactions
Ruxolitinib is metabolized by CYP3A4 and corresponding drug-drug interactions are possible. When strong CYP inhibitors are administered concomitantly, the dose must be reduced as directed.
Adverse effects
The most common possible adverse effects include thrombocytopenia, anemia, neutropenia, bruising, dizziness, and headache.
