1. Definition & Mechanism
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Generic Name:Ā Eltrombopag
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Brand Name:Ā Revolade (also marketed asĀ PromactaĀ in some regions)
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Class:Ā Thrombopoietin receptor agonist (TPO-RA)Ā (oral small-molecule)
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Mechanism:Ā Binds to the TPO receptor on megakaryocytes ā stimulates platelet production
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Half-life:Ā ~21ā32 hours (allows once-daily dosing)
2. Indications & Importance
ā Ā FDA/EMA-Approved Uses:
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Chronic Immune Thrombocytopenia (ITP)Ā (adults & children ā„1 year) āĀ 2nd-line therapy
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Severe Aplastic Anemia (SAA)Ā (in combination with immunosuppressants)
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Hepatitis C-associated ThrombocytopeniaĀ (to permit antiviral therapy)
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Chemotherapy-Induced ThrombocytopeniaĀ (under investigation)
ā ļøĀ Not for use in:
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Myelodysplastic syndromes (MDS) (ā risk of leukemic progression)
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Patients with normal platelet counts
3. Dosage & Administration
Standard Dosing Guidelines
Indication | Starting Dose | Dose Adjustment | Max Dose |
---|---|---|---|
ITP (Adults) | 50 mg once daily | Adjust by 25 mg every 2 weeks | 75 mg/day |
ITP (Children 1-5 yrs) | 25 mg once daily | Adjust by 12.5ā25 mg | 75 mg/day |
SAA | 150 mg once daily | Reduce if platelets >200,000/μL | 150 mg/day |
HCV Thrombocytopenia | 25 mg once daily | Titrate weekly | 100 mg/day |
Key Administration Points:
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Take on an empty stomachĀ (1 hr before or 2 hrs after food)
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Avoid calcium-rich foods/drugsĀ (dairy, antacids ā separate by ā„4 hrs)
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Do not crush tabletsĀ (film-coated)
4. Side Effects & Toxicity
Common (ā„10%)
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HeadacheĀ (20%)
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Nausea, diarrheaĀ (15%)
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FatigueĀ (12%)
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Mild liver enzyme elevationĀ (ALT/AST ā)
Serious (Monitor Closely)
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HepatotoxicityĀ (rare but severe)
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ThrombosisĀ (arterial/venous ā especially if platelets >400,000/μL)
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Bone Marrow FibrosisĀ (long-term use)
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CataractsĀ (ophthalmic exams recommended)
5. Storage & Handling
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Store at 20ā25°CĀ (room temperature)
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Keep in original blister packĀ (protects from moisture)
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Do not freeze
6. Contraindications & Warnings
āĀ Absolute Contraindications:
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Hypersensitivity to eltrombopag
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Severe hepatic impairment (Child-Pugh C)
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Active thrombosis
ā ļøĀ Black Box Warnings (FDA):
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Risk of hepatotoxicityĀ (monitor LFTs every 2 weeks initially)
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Risk of bone marrow fibrosisĀ (check reticulin staining if long-term use)
7. Drug Interactions
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Polyvalent cations (Ca²āŗ, Mg²āŗ, Fe²āŗ):Ā ā Absorption (separate doses by 4 hrs)
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CYP1A2/CYP2C8 inhibitors (fluvoxamine, gemfibrozil):Ā ā Eltrombopag levels
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Statins:Ā May ā risk of myopathy
8. Monitoring Requirements
Parameter | Frequency | Action Threshold |
---|---|---|
Platelet count | Weekly until stable, then monthly | >150,000/μL ā reduce dose |
Liver enzymes | Every 2 weeks Ć3 months, then monthly | ALT >3Ć ULN ā interrupt |
Bone marrow biopsy | Annually (if long-term use) | Reticulin fibrosis ā reconsider therapy |
9. Cost & Alternatives
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Price:Ā ~$5,000ā$7,000/month (brand)
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Alternatives:
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Romiplostim (Nplate)Ā (subcutaneous TPO-RA)
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Avatrombopag (Doptelet)Ā (alternative oral TPO-RA)
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10. Conclusion
REVOLADE 50 mgĀ is aĀ potent oral thrombopoietin agonistĀ for ITP, SAA, and HCV-related thrombocytopenia.
Key Takeaways:
āĀ Effective in refractory ITPĀ (60ā80% response rate)
āĀ Convenient oral dosingĀ (vs. injectable alternatives)
āĀ Requires strict monitoringĀ (liver, platelets, bone marrow)
Clinical Pearls:
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Start low, go slowĀ (especially in elderly)
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Discontinue if no response after 4 weeks
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Consider thromboprophylaxis if platelets >400,000/μL
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