Generic
Ruxolitinib
11 brands available in the market
At a glance
Ruxolitinib is a JAK1/JAK2 inhibitor used for the treatment of myelofibrosis, polycythemia vera, and steroid-refractory acute graft-versus-host disease (GVHD). It modulates hematopoiesis and immune function by inhibiting JAK-STAT signaling pathways.
Description
Ruxolitinib is a kinase inhibitor that inhibits JAK1 and JAK2, which mediate signaling of cytokines and growth factors important for hematopoiesis and immune function. It prevents STAT phosphorylation and nuclear localization, modulating gene expression. In myelofibrosis, it reduces splenomegaly, decreases JAK2V617F mutant cells, and reduces inflammatory cytokines.
Indications
- Intermediate or high-risk myelofibrosis (primary MF, post-polycythemia vera MF, post-essential thrombocythemia MF)
- Polycythemia vera (inadequate response or intolerance to hydroxyurea)
- Steroid-refractory acute graft-versus-host disease (GVHD) – adults and pediatric patients ≥12 years
Therapeutic class
Pyrrolopyrimidines
Pharmacological class
JAK1/JAK2 Inhibitor
Pharmacology
Ruxolitinib inhibits JAK1 and JAK2 kinases, blocking JAK-STAT signaling pathways. It prevents STAT phosphorylation and nuclear translocation, modulating gene expression. In myelofibrosis, it reduces splenomegaly, decreases JAK2V617F mutant cells, and reduces inflammatory cytokines (TNF-α, IL-6).
Mechanism of action
Inhibits JAK1/JAK2 kinases to regulate JAK-STAT signaling.
Dosage
Adult Dose (Oral):
Myelofibrosis (based on platelet count):
- >200 × 10⁹/L: 20 mg twice daily
- 100-200 × 10⁹/L: 15 mg twice daily
- 50-100 × 10⁹/L: 5 mg twice daily
Polycythemia Vera:
- Starting: 10 mg twice daily
Acute GVHD:
- Starting: 5 mg twice daily; increase to 10 mg twice daily after 3 days if ANC/platelets not decreased by ≥50%
Administration
- Take orally with or without food
- Take at the same time each day
Missed dose
If a dose is missed, do not take an additional dose; take the next usual prescribed dose.
Side effects
Common Side Effects:
- Thrombocytopenia
- Anemia
- Neutropenia
- Risk of infection
- Bruising
- Dizziness and headache
- Non-melanoma skin cancer
- Lipid elevations
Precautions & warnings
- Thrombocytopenia, anemia, neutropenia: Reduce dose or interrupt; monitor CBC every 2-4 weeks
- Risk of serious bacterial, mycobacterial, fungal, and viral infections
- Tuberculosis: Evaluate risk before starting; delay if active TB
- PML: Suspect, discontinue and evaluate
- Herpes zoster: Early signs and symptoms, seek treatment
- Hepatitis B: Monitor HBV-DNA titers
- Do not stop abruptly (withdrawal syndrome); taper gradually
- Non-melanoma skin cancer: Periodic skin examinations
- Lipids: Assess at 8-12 weeks
Contraindications
- Hypersensitivity to ruxolitinib or any component
Drug interactions
- Fluconazole (>200 mg/day): CYP3A4/CYP2C9 inhibition increases ruxolitinib exposure; avoid (except GVHD)
- Strong CYP3A4 inhibitors: Increase exposure; consider dose reduction
- Strong CYP3A4 inducers: Decrease exposure; dose adjustment may be needed
Food interactions
Caution is advised when consuming alcohol with Ruxolitinib; consult your doctor.
Use in pregnancy
Use in Pregnancy: No adequate controlled studies; use only if clearly needed; consult your doctor.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Unknown if excreted in human milk; discontinue breastfeeding during treatment and for 2 weeks after the last dose; consult your doctor.
Pediatric use
Safety and efficacy not established in pediatric patients (except GVHD ≥12 years)
Geriatric use
Caution required in elderly patients; dose adjustment may be needed.
Renal / hepatic impairment
Renal Impairment: Indicated for CKD patients; adjust dose based on Hb levels; consult your doctor.
Hepatic Impairment: Not recommended in severe hepatic impairment; consult your doctor.
Overdose effects
No specific antidote for overdose; single doses up to 200 mg are tolerable; higher doses cause myelosuppression; hemodialysis is not effective.
Storage conditions
Store below 30°C in a dry place, away from sunlight; keep out of reach of children.
Chemical structure
Ruxolitinib