Products
Fedratinib was approved in the United States in 2019 in capsule form (Inrebic).
Structure and properties
Fedratinib is present in the drug as dihydrochloride and monohydrate (fedratinib dihydrochloride monohydrate).
Effects
Fedratinib has antiproliferative properties. The effects are due to selective inhibition of Janus kinases 2 (JAK2). These are intracellular enzymes that belong to the tyrosine kinase group and transfer phosphate groups. They are involved in signal transduction from the cell membrane to the nucleus and have an influence on gene expression. The excessive activity of mutant JAK2 kinases (e.g. JAK2V617F) is involved in the development of myelofibrosis and polycythaemia vera. Fedratinib additionally inhibits FLT3 (FMS-like tyrosine kinase 3). It has a long terminal half-life of approximately 114 hours.
Indications
For the treatment of primary or secondary myelofibrosis.
Dosage
According to the SmPC. Capsules are taken once daily, independent of meals.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Fedratinib is metabolized by CYP3A4 and CYP2C19, and corresponding drug-drug interactions are possible.
Adverse effects
The most common potential adverse effects include diarrhea, nausea, anemia, and vomiting
