-5%
Rulicent is approved for the treatment of several hematologic and immune-mediated conditions in adults and selected pediatric populations:
- Myelofibrosis (MF): Rulicent is used in adults diagnosed with intermediate to high-risk MF, including primary myelofibrosis, post-polycythemia vera MF, and post-essential thrombocythemia MF, to manage disease progression and related symptoms.
- Polycythemia Vera (PV): Indicated for adult patients with PV who either do not respond adequately to hydroxyurea or are intolerant to its side effects.
- Steroid-Refractory Acute Graft-versus-Host Disease (GVHD): Approved for adults and pediatric patients aged 12 years and older with acute GVHD that does not respond to corticosteroid treatment.
Pregnancy: There is no conclusive evidence from human studies. Rulicent should be used during pregnancy only if the potential benefit justifies the risk to the fetus.
Breastfeeding: Unknown if excreted in human milk. Discontinue breastfeeding during treatment and for at least two weeks after the last dose due to potential infant exposure.
Ruxolitinib is an oral selective inhibitor of Janus-associated kinases (JAK1 and JAK2)—enzymes critical for signal transduction from cytokine and growth factor receptors involved in blood cell production and immune regulation.
In myelofibrosis, a condition marked by uncontrolled JAK signaling, Ruxolitinib corrects dysregulation by:
- Suppressing splenomegaly (enlarged spleen)
- Reducing mutant JAK2V617F allele burden
- Lowering circulating inflammatory cytokines (e.g., TNF-α, IL-6)
Pharmacokinetics Overview:
- Absorption: Rapidly absorbed after oral administration; peak levels (Cmax) achieved within 1–2 hours.
- Bioavailability: Oral absorption is at least 95%.
- Distribution: Steady-state volume of distribution ~72 L.
- Plasma Protein Binding: ~97%, primarily to albumin.
- Metabolism: Predominantly via CYP3A4, with minor involvement of CYP2C9.
- Elimination Half-Life: ~3 hours (drug); ~5.8 hours (with metabolites).
- Excretion: Primarily through metabolism—74% in urine, 22% in feces; <1% excreted as unchanged drug.