Catalog No.S2229 Synonyms: SB-497115-GR, SB497115
Molecular Weight(MW): 564.63
Eltrombopag Olamine is a member of the biarylhydrazone class, which is a nonpeptide agonist of the thrombopoietin receptor (TpoR).
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|Description||Eltrombopag Olamine is a member of the biarylhydrazone class, which is a nonpeptide agonist of the thrombopoietin receptor (TpoR).|
Eltrombopag demonstrates a half maximal effective concentration (EC50) of 0.27 μM in murine BAF3 cells transfected with the luciferase reporter gene under direction of the STAT-activated IRF-1 promoter and human TpoR (BAF3/IRF-1/hTpoR). Eltrombopag activates the receptor by association with metal ions (i.e., Zn2+) and specific amino acids within the transmembrane and juxtamembrane domains of the TpoR. Eltrombopag (30 μM) results in activation of STAT5 in N2C-Tpo cells, as detected with an antiphospho-STAT5 antibody on Western blots. Eltrombopag stimulates proliferation after a 2-day incubation with an EC50 of 0.03 μM in a BrdU assay conducted in BAF3/hTpoR cells. Eltrombopag also induces differentiation of hematopoietic stem cells into committed megakaryocyte progenitor cells. Eltrombopag increases the differentiation of bone marrow CD34+ cells into CD41+ megakaryocytes in a dose-dependent manner with an EC50 of 0.1 μM.  Eltrombopag inhibits N2C-Tpo cell and HEL92.1.7 cell proliferating with IC50 of 20.7 μg/mL and 2.3 μg/mL.  Eltrombopag (20 μg/mL) leads to a decreased cell division rate, a block in G(1) phase of cell cycle, and increased differentiation in human and murine leukemia cells. Eltrombopag (5 μg/mL) shows clear signs of differentiation, significant changes in the organization of the nuclear contents, and an increase in the cytoplasm/nucleus ratio in HL60 cells. Eltrombopag (5 μg/mL) causes an increase in CD11b, which is consistent with a premacrophage state in U937 cells, and also causes an increase in CD11b in URE cells. Eltrombopag leads to a reduction in free intracellular iron in leukemic cells in a dose-dependent manner in HL60 cells. 
|In vivo||Eltrombopag (10 mg/kg per day) increases platelet counts over twofold approximately 1 week after the last dose for one chimpanzee and approximately 1.5-fold for the other two chimpanzees.  Eltrombopag (1 mg/mL) prolongs survival in mouse models of leukemia. |
|In vitro||DMSO||89 mg/mL (157.62 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01772420||Unknown status||Adult Myelodysplastic Syndrome|Anemia|Chronic Myelomonocytic Leukemia||Albert Einstein College of Medicine Inc.|National Cancer Institute (NCI)||October 2012||Phase 2|
|NCT01636778||Completed||Hepatitis C Chronic||GlaxoSmithKline||July 2012||Phase 2|
|NCT01610180||Completed||Purpura Thrombocytopenic Idiopathic|Autoimmune Thrombocytopenic Purpura|Autoimmune Thrombocytopenia|Chronic Lymphocytic Leukemia|Non Hodgkin''s Lymphoma||Fondazione Progetto Ematologia||June 2012||Phase 2|
|NCT01550185||Terminated||Adult Acute Basophilic Leukemia|Adult Acute Eosinophilic Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Del(5q)|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Recurrent Adult Acute Myeloid Leukemia||Roswell Park Cancer Institute|National Cancer Institute (NCI)|GlaxoSmithKline||May 2012||Phase 1|
|NCT01147809||Completed||Thrombocytopaenia||GlaxoSmithKline||June 2010||Phase 2|
|NCT01098487||Completed||Purpura Thrombocytopaenic Idiopathic||GlaxoSmithKline||May 2010||Phase 4|
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