Ruxolitinib (Oral)
Generic Details
Generic Name
Ruxolitinib Oral
Other Names
- Jakafi
Drug Class
- Janus kinase (JAK) inhibitor
Chemical Formula
C17H18N6
Molecular Weight
306.37 g/mol
Mechanism of Action
- Inhibits JAK1 and JAK2 which are involved in cytokine signaling pathways
Indications
- Myelofibrosis
- Polycythemia Vera
- Acute Graft-Versus-Host Disease (GVHD)
Common Dosage Forms
- Tablet
Typical Dosage
- 5 mg twice daily to 25 mg twice daily depending on the condition being treated
Pediatric Dosage
- Not established
Geriatric Dosage
- Dose adjustments may be needed
Side Effects
- Anemia
- Thrombocytopenia
- Neutropenia
- Headache
- Dizziness
- Nausea
- Vomiting
- Diarrhea
Contraindications
- Severe infections
Pregnancy Category
- C - Risk cannot be ruled out
Lactation Safety
- Use caution or avoid
Drug Interactions
- Strong CYP3A4 inhibitors can increase ruxolitinib levels
Overdose Symptoms
- Increased risk of infections
- Thrombocytopenia
- Liver toxicity
Antidote for Overdose
- There is no specific antidote; manage symptoms and provide supportive care
Storage Conditions
- Store at room temperature between 68°F to 77°F (20°C to 25°C)
Pharmacokinetics
- Absorption: Well absorbed orally
- Distribution: Highly bound to plasma proteins
- Metabolism: Primarily metabolized by CYP3A4 enzymes
- Excretion: Mainly excreted in feces
Precautions
- Monitor blood counts regularly
- Risk of infections
- Risk of developing skin cancers
Warnings
- Serious and fatal infections have occurred; monitor closely
Others
- Ruxolitinib is also available in oral suspension form for ease of administration