Name | Eltrombopag Olamine |
CAS number | 496775-62-3 |
Description | Eltrombopag Olamine is the orally active ethanolamine salt form of eltrombopag, a small-molecule, nonpeptide thrombopoietin receptor agonist, with the CAS Registry Number 496775-62-3. |
Structural formula |  |
Molecular Formula | C27H29N5O5 |
Molecular Weight | 503.56 g/mol |
Appearance | White powder |
Quality Standard | 99% |
Storage Condition | Cool dry place( away from the light) |
Shelf Life | >2 years if stored properly |
Sample package | Aluminium foil bag |
Commercial package | Aluminium Tin, Fiber drum |
Origin | China |
Eltrombopag Olamine More Info
Eltrombopag Olamine is the orally active ethanolamine salt form of eltrombopag, a small-molecule, nonpeptide thrombopoietin receptor agonist, with the CAS Registry Number 496775-62-3. Its molecular structure consists of the eltrombopag free acid combined with two molecules of ethanolamine. This specific salt formulation enhances the compound's aqueous solubility and stability for oral pharmaceutical use, allowing it to be manufactured as film-coated tablets and powder for oral suspension. It is the active ingredient in branded products authorized in major markets since the late two thousands.
The mechanism of action of eltrombopag olamine is unique among hematologic agents as it represents the first-in-class oral, nonpeptide thrombopoietin receptor agonist. Unlike recombinant thrombopoietin, this small molecule interacts specifically with the transmembrane domain of the human thrombopoietin receptor on hematopoietic stem cells and megakaryocyte progenitors. This binding initiates intracellular signaling cascades analogous to those triggered by endogenous thrombopoietin, leading to the proliferation and differentiation of cells in the megakaryocytic lineage. The result is a dose-dependent increase in platelet production from bone marrow progenitor cells, effectively stimulating the body's own capacity to generate platelets rather than providing exogenous platelets through transfusion.
The clinical applications of eltrombopag olamine span several important hematologic conditions characterized by low platelet counts. It is primarily indicated for the treatment of primary immune thrombocytopenia in both adult and pediatric patients who are refractory to other treatments such as corticosteroids or immunoglobulins. It is also approved for the treatment of thrombocytopenia in adult patients with chronic hepatitis C virus infection, where low platelet counts may prevent the initiation or limit the ability to maintain optimal interferon-based therapy. Additionally, eltrombopag has demonstrated efficacy in acquired severe aplastic anemia, helping to restore multilineage hematopoiesis in patients with this life-threatening bone marrow failure syndrome.
This medication is administered orally once daily at approximately the same time each day, with dosing requirements that vary based on patient ancestry and concomitant food intake. Importantly, patients of Asian ancestry, including Chinese, Japanese, Taiwanese, or Korean individuals, typically require lower starting doses due to differences in drug metabolism. Eltrombopag tablets must be taken on an empty stomach, at least two hours before or four hours after consuming dairy products, minerals, supplements, or antacids containing calcium, magnesium, iron, or zinc, as these polyvalent cations chelate the drug and significantly reduce its absorption. Pharmacokinetic studies demonstrate that administration with a high-fat, low-calcium meal can reduce net systemic exposure substantially, underscoring the critical importance of proper timing relative to food intake. The powder for oral suspension formulation requires reconstitution with water immediately before administration using the provided measuring device, and should not be mixed with any other liquids or food.
The safety profile of eltrombopag olamine requires vigilant monitoring throughout treatment. Common adverse effects include headache, nausea, diarrhea, abdominal pain, fatigue, and joint or muscle discomfort. The most important serious risks are hepatotoxicity, manifested by elevated liver enzymes, and thrombotic or thromboembolic events, including portal vein thrombosis in patients with chronic liver disease. Regular monitoring of liver function through blood tests is mandatory during therapy. Patients must be instructed to seek immediate medical attention for symptoms of liver injury such as yellowing of the skin or eyes, dark urine, or right upper stomach pain, as well as for signs of blood clots including pain or swelling in the arms or legs, confusion, or difficulty speaking. Drug interactions are clinically significant; notably, eltrombopag may reduce the effectiveness of hormonal contraceptives, necessitating the use of additional barrier methods such as condoms during treatment. Despite these risks, when used under appropriate medical supervision with careful attention to dosing instructions and monitoring parameters, eltrombopag olamine provides a well-tolerated and effective oral option for managing thrombocytopenia across multiple clinical contexts.
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