Revolade Eltrombopag Olamine Tablets

1. Indications and Usage
Chronic ITP: Indicated for the treatment of thrombocytopenia in adult and pediatric patients 1 year of age and older with chronic immune thrombocytopenia (ITP) who have had an inadequate response to corticosteroids, immunoglobulins, or splenectomy.
Hepatitis C-Associated Thrombocytopenia: Indicated for the treatment of thrombocytopenia in adult patients with chronic hepatitis C to enable initiation and maintenance of interferon-based therapy.
Severe Aplastic Anemia (SAA): Indicated in combination with standard immunosuppressive therapy (IST) for the first-line treatment of adult and pediatric patients 2 years of age and older with severe aplastic anemia.
2. Dosage and Administration
Initial Dosing: The starting dose varies by indication and patient population (e.g., 50 mg once daily for adult ITP patients, 25 mg once daily for East Asian patients or those with hepatic impairment).
Dose Titration: Dosage should be adjusted based on platelet count response. The goal is to maintain a safe platelet count and reduce bleeding risk without increasing the risk of thrombosis.
Administration Instructions: Take on an empty stomach. Do not take with food or multivalent cations (e.g., calcium, iron, magnesium, aluminum).
Timing Requirements: Administer at least 2 hours before or 4 hours after taking other medications, or consuming foods/drinks containing multivalent cations (e.g., dairy products, antacids, fortified juices).
3. Mechanism of Action
TPO Receptor Agonism: Eltrombopag is an oral small-molecule agonist of the thrombopoietin (TPO) receptor (c-Mpl) on hematopoietic progenitor cells.
Thrombopoiesis Stimulation: It activates the JAK-STAT signaling pathway, stimulating megakaryocyte proliferation and differentiation, leading to increased endogenous production of thrombopoietin and subsequent increases in platelet counts.
4. Safety and Warnings
Thrombotic/Thromboembolic Complications: Serious and fatal thrombotic events have occurred, particularly when platelet counts exceed 400,000/µL.
Hepatotoxicity: Severe liver injury has been reported. Liver function tests (ALT, AST, bilirubin) must be monitored regularly during therapy.
Bone Marrow Reticulin Fibrosis: Increased reticulin or collagen fiber formation in the bone marrow has been observed, which may be reversible upon discontinuation.
AML/MDS Risk: There is an increased risk of developing myelodysplastic syndrome (MDS) or acute myeloid leukemia (AML).
Cataracts: New or worsening cataracts have been reported; ophthalmologic evaluations are recommended during treatment.
5. Adverse Reactions and Clinical Research
Adverse Reactions: Common adverse reactions include nausea, diarrhea, upper respiratory tract infection, arthralgia, back pain, and headache.
Clinical Research: Clinical trials have demonstrated significant efficacy in increasing platelet counts and reducing bleeding risks in patients with chronic ITP and severe aplastic anemia.
6. Drug Interactions
Multivalent Cations: Concomitant use with antacids, iron supplements, calcium, or other multivalent cations significantly reduces absorption due to chelation.
OATP1B1 or BCRP Substrates: Eltrombopag inhibits OATP1B1 and BCRP transporters. Concomitant use with substrates of these transporters (e.g., statins, repaglinide) may increase systemic exposure to those drugs.
Hepatically Metabolized Drugs: Caution is advised with drugs metabolized by hepatic enzymes, as eltrombopag may alter their clearance.
7. Pharmaceutical Information
Composition: The active ingredient is eltrombopag olamine.
Appearance: The tablets are film-coated, typically appearing red to brown.
Storage: Store at controlled room temperature and protect from moisture.