Eltrombopag, a second-generation thrombopoietin receptor agonist, for chronic lymphocytic leukemia-associated ITP

Eltrombopag--an oral thrombopoietin agonist.

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 ora...

Autoimmune thrombocytopenic purpura ("ITP" type) with chronic lymphocytic leukemia.

Metabolism and disposition of eltrombopag, an oral, nonpeptide thrombopoietin receptor agonist, in healthy human subjects.

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 ...

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) ...

HEMATOPOIESIS - BRIEF REPORT Phase I Clinical Study of Eltrombopag, an Oral, Non-peptide Thrombopoietin Receptor Agonist

1. All of the authors (JMJ, DW, YD, JU, VK, DC, CEM) have declared a financial interest in a company whose (potential) product was studied in the present work. 2. Several of the authors (CEM, DC )have declared a financial interest in a competitor of a company whose (potential) product was studied in the present work. 3. All of the authors (JMJ, DW, YD, JU, VK, DC, CEM) are employed by a company...