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BLOOD AND BLOOD FORMING ORGANS › ANTIHEMORRHAGICS › VITAMIN K AND OTHER HEMOSTATICS › Other systemic hemostatics
eltrombopag
B02BX05
Forms & Strengths
- Oral tablets: 12.5 mg, 25 mg, 50 mg, 75 mg
- Oral suspension for reconstitution: 25 mg/packet, 50 mg/packet
Adult Dosing
- Chronic immune thrombocytopenia (ITP): Initial 50 mg once daily; adjust to maintain platelet count >= 50 x 10^3/mcL (max 75 mg/day)
- Chronic hepatitis C-associated thrombocytopenia: Initial 25 mg once daily; adjust by 25 mg every 2 weeks to target platelet count (max 100 mg/day)
- Severe aplastic anemia (first-line with immunosuppression): Initial 150 mg once daily for 6 months in combination with ATG and cyclosporine
- Severe aplastic anemia (refractory): Initial 50 mg once daily; titrate up to 150 mg daily as needed
Pediatric Dosing
- Chronic ITP (>= 6 years): Initial 50 mg once daily for children >= 6 years; 25 mg once daily for children aged 1-5 years
- Chronic ITP (under 1 year): Safety and efficacy not established
- Severe aplastic anemia (>= 2 years): Initial 75 mg once daily (age 2-11 years) or 150 mg once daily (>= 12 years) in combination with immunosuppressive therapy
Indications
- Treatment of chronic immune thrombocytopenia (ITP) in patients with insufficient response to corticosteroids, immunoglobulins, or splenectomy
- Treatment of thrombocytopenia in patients with chronic hepatitis C to allow initiation and maintenance of pegylated interferon-based therapy
- First-line treatment of severe aplastic anemia in combination with standard immunosuppressive therapy
- Treatment of severe aplastic anemia in patients refractory to immunosuppressive therapy
Mechanism of Action
- TPO receptor agonist that interacts with the transmembrane domain of the human thrombopoietin (TPO) receptor
- Initiates signaling cascades that induce proliferation and differentiation of megakaryocytes from bone marrow progenitor cells, increasing platelet production
Contraindications
- Hypersensitivity to eltrombopag or any component of the formulation
- Pre-existing myelodysplastic syndrome (MDS) transformation risk (use with caution, though specifically contraindicated in specific product labeling warnings regarding risk progression)
Adverse Reactions
- Hepatotoxicity (elevated ALT, AST, bilirubin)
- Thrombosis / thromboembolic events
- Bone marrow reticulin formation and marrow fibrosis
- Cataracts
- Nausea, diarrhea, vomiting
- Upper respiratory tract infection, nasopharyngitis
- Fatigue, headache
Drug Interactions
- Polyvalent cations (antacids, calcium, iron, magnesium, aluminum, selenium, zinc): Chelate eltrombopag; administer eltrombopag at least 2 hours before or 4 hours after these agents
- CYP1A2 and CYP2C8 substrates: Eltrombopag inhibits OATP1B1, CYP1A2, and CYP2C8
- HMG-CoA reductase inhibitors (statins): Potential for increased statin exposure and myopathy risk
- Bile acid sequestrants: May bind to eltrombopag; separate administration times significantly
Curated Content: Needs Vetting Before Put to Clinical Use