Eltrombopag--an oral thrombopoietin agonist.
نویسندگان
چکیده
The therapy for immune thrombocytopenic purpura (ITP) has evolved in the recent past. In certain cases therapy for ITP remains inadequate. Thrombopoietin receptor agonists are the latest addition to the armamentarium to manage the thrombocytopenia. While romiplostim was the first second generation thrombopoietin agonist to become available, eltrombopag is particularly attractive as it is an orally bioavailable agent. This review focuses on the use, safety and efficacy of eltrombopag in various clinical conditions.
منابع مشابه
Preclinical Activity of Eltrombopag (SB-497115), an Oral, Nonpeptide Thrombopoietin Receptor Agonist
Eltrombopag is a first-in-class, orally bioavailable, small-molecule, nonpeptide agonist of the thrombopoietin receptor (TpoR), which is being developed as a treatment for thrombocytopenia of various etiologies. In vitro studies have demonstrated that the activity of eltrombopag is dependent on expression of TpoR, which activates the signaling transducers and activators of transcription (STAT) ...
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The metabolism and disposition of eltrombopag, the first-in-class small molecule human thrombopoietin receptor agonist, were studied in six healthy men after a single oral administration of a solution dose of [(14)C]eltrombopag (75 mg, 100 μCi). Eltrombopag was well tolerated. The drug was quickly absorbed and was the predominant circulating component in plasma (accounting for 63% of the total ...
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Thrombopoietin confers immediate protection against injury caused by ischemia/reperfusion in the rat heart. Eltrombopag is a small molecule agonist of the thrombopoietin receptor, the physiologic target of thrombopoietin. However, the ability of eltrombopag and thrombopoietin to protect human cardiac myocytes against injury and the mechanisms underlying myocyte protection are not known. Human c...
متن کاملThe Impact of Eltrombopag Administration on the Clinical Course of Severe Refractory Fatal Acquired Aplastic Anemia
Severe aplastic anemia (SAA) has an aggressive clinical course and represents a “difficult-to-treat” situation with current medications [1]. Eltrombopag is a c-mpl receptor agonist oral thrombopoietin-mimetic drug, mainly active in immune thrombocytopenic purpura (ITP) [2]. Single-agent oral eltrombopag produced hematological responses in 11 of 25 cases of aplastic pancytopenia, with trilineage...
متن کاملEffect of the nonpeptide thrombopoietin receptor agonist Eltrombopag on bone marrow cells from patients with acute myeloid leukemia and myelodysplastic syndrome.
Thrombocytopenia is a frequent symptom and clinical challenge in patients with myelodysplastic syndrome (MDS) and acute myeloid leukemia (AML). Eltrombopag is a small molecule thrombopoietin receptor agonist that might be a new option to treat thrombocytopenia in these diseases, provided that it does not stimulate malignant hematopoiesis. In this work, we studied the effects of Eltrombopag on p...
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ورودعنوان ژورنال:
- European review for medical and pharmacological sciences
دوره 16 6 شماره
صفحات -
تاریخ انتشار 2012