1. Immunology/Inflammation
  2. Thrombopoietin Receptor

Eltrombopag Olamine (Synonyms: Eltrombopag diethanolamine salt; SB-497115GR)

Cat. No.: HY-15306A Purity: >98.0%
Data Sheet SDS Handling Instructions

Eltrombopag olamine is a new, orally active thrombopoietin-receptor (c-mpl) agonist that stimulates thrombopoiesis.

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Eltrombopag Olamine Chemical Structure

Eltrombopag Olamine Chemical Structure

CAS No. : 496775-62-3

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Description

Eltrombopag olamine is a new, orally active thrombopoietin-receptor (c-mpl) agonist that stimulates thrombopoiesis. IC50 Value: 0.27 uM (EC50 in murine BAF3 cells) [1] Target: thrombopoietin-receptor (c-mpl) Potential advantages of eltrombopag may include a sustained platelet response and a good tolerability profile. in vitro: Eltrombopag demonstrated a half maximal effective concentration (EC50) of 0.27 uM 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) [1]. Eltrombopag stimulates the growth of TPO-dependent cell lines via JAK2 and STAT signaling pathways and stimulates isolated human CD34+ cells to become megakaryocytes and produce platelets [2]. in vivo: Twelve weeks of antiviral therapy, with concurrent receipt of eltrombopag or placebo, were completed by 36%, 53%, and 65% of patients receiving 30 mg, 50 mg, and 75 mg of eltrombopag, respectively, and by 6% of patients in the placebo group [3]. Eltrombopag was administered as once-daily oral capsules for 10 days at doses of 5, 10, 25, 30, 50, and 75 mg. The pharmacokinetics of eltrombopag was dose dependent and linear, and eltrombopag increased platelet counts in a dose-dependent manner [4]. Toxicity: There were no apparent differences in the incidence or severity of adverse events in subjects receiving active or placebo study medication [4]. Long-term treatment with eltrombopag was generally safe, well tolerated, and effective in maintaining platelet counts in the desired range [5]. Clinical trial: Eltrombopag In Cord Blood Or Haploidentical Bone Marrow Transplantation. Phase 2

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02093325 Chang Gung Memorial Hospital|GlaxoSmithKline Gynecologic Cancer March 2014 Phase 3
NCT01500538 Peter MacCallum Cancer Centre, Australia|GlaxoSmithKline|Merck Sharp & Dohme Corp. Follicular Lymphoma|Marginal Zone Lymphoma|Mantle Cell Lymphoma October 2012 Phase 2
NCT01610180 Fondazione Progetto Ematologia Purpura, Thrombocytopenic, Idiopathic|Autoimmune Thrombocytopenic Purpura|Autoimmune Thrombocytopenia|Chronic Lymphocytic Leukemia|Non Hodgkin's Lymphoma June 2012 Phase 2
NCT01488565 Peter MacCallum Cancer Centre, Australia|GlaxoSmithKline|Celgene Corporation Myelodysplastic Syndromes (MDS)|Acute Myeloid Leukaemia (AML) December 2010 Phase 2
NCT01757145 Rabin Medical Center Hematological Malignancy|Bone Marrow Failure Syndrome January 2013 Phase 2
NCT01133860 IRCCS Policlinico S. Matteo|University of Pavia|GlaxoSmithKline|Azienda Ospedaliera di Padova|Azienda Ospedaliera di Perugia|Fondazione Telethon Blood Platelet Disorders January 2009 Phase 2
NCT01940562 moshe yeshurun|GlaxoSmithKline|Rabin Medical Center Pediatric Patients Undergoing Allogeneic Cord Blood Transplantation. October 2013 Phase 2
NCT01880047 Weill Medical College of Cornell University|Novartis Immune Thrombocytopenia|Platelet Disorder February 2013 Phase 2
NCT02148133 Novartis Pharmaceuticals|Novartis Cytopaenia July 2014 Phase 2
NCT02402998 Gruppo Italiano Malattie EMatologiche dell'Adulto Primacy Immune Thrombocytopenia June 2015 Phase 2
NCT02254434 GlaxoSmithKline Cirrhosis, Liver August 2014 Phase 1
NCT00643929 GlaxoSmithKline Purpura, Thrombocytopaenic, Idiopathic February 2007
NCT01286675 Dana-Farber Cancer Institute Multiple Myeloma March 2011
NCT01652599 Hospital Universitario Dr. Jose E. Gonzalez Immune Thrombocytopenic Purpura June 2012 Phase 2
NCT02201290 Novartis Pharmaceuticals|Novartis Purpura, Thrombocytopenic, Idiopathic June 18, 2013 Phase 3
NCT01055600 GlaxoSmithKline Thrombocytopaenia March 2013 Phase 4
NCT01791101 Gruppo Italiano Malattie EMatologiche dell'Adulto Thrombocytopenia September 2013 Phase 2
NCT01286038 H. Lee Moffitt Cancer Center and Research Institute|GlaxoSmithKline Myelodysplastic Syndrome (MDS)|Thrombocytopenia March 2011 Phase 1|Phase 2
NCT01386723 Weill Medical College of Cornell University|Novartis Immune Thrombocytopenia June 2011
NCT00351468 Novartis Pharmaceuticals|Novartis Purpura, Thrombocytopaenic, Idiopathic June 2006 Phase 3
NCT00828750 GlaxoSmithKline Idiopathic Thrombocytopenic Purpura|Purpura, Thrombocytopenic, Idiopathic May 2008 Phase 3
NCT01927731 M.D. Anderson Cancer Center|Novartis Pharmaceuticals Blood And Marrow Transplantation October 2013 Phase 2
NCT01194167 University of Cincinnati|GlaxoSmithKline Thrombocytopenia August 2010 Phase 2
NCT00902018 Weill Medical College of Cornell University|GlaxoSmithKline Idiopathic Thrombocytopenic Purpura January 2009 Phase 2
NCT02422394 IRCCS Policlinico S. Matteo Inherited Platelet Disorder April 2015 Phase 2
NCT02010645 M.D. Anderson Cancer Center|GlaxoSmithKline Leukemia March 2014 Phase 2
NCT01397149 University of Ulm|GlaxoSmithKline|German CLL Study Group|WiSP Wissenschaftlicher Service Pharma GmbH Chronic Lymphocytic Leukemia|Thrombocytopenia October 2011 Phase 1|Phase 2
NCT00996216 GlaxoSmithKline Hepatitis C September 2009 Phase 3
NCT01491594 Duke University|GlaxoSmithKline Sarcoma, Soft Tissue|Osteosarcoma|Neoplasms, Connective and Soft Tissue April 2012 Phase 1
NCT02323178 Groupe Francophone des Myelodysplasies|GlaxoSmithKline|Novartis CMML|Thrombocytopenia August 7, 2014 Phase 1|Phase 2
NCT01893372 M.D. Anderson Cancer Center|GlaxoSmithKline|Novartis Leukemia October 2013 Phase 2
NCT01428635 M.D. Anderson Cancer Center|Novartis Pharmaceuticals Leukemia|Chronic Myeloid Leukemia|Myelofibrosis January 13, 2012 Phase 2
NCT01168921 M.D. Anderson Cancer Center|GlaxoSmithKline CLL|Leukemia November 2010 Phase 2
NCT01550185 Roswell Park Cancer Institute|National Cancer Institute (NCI)|GlaxoSmithKline 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) May 2012 Phase 1
NCT00888901 Ingrid Pabinger, MD|GlaxoSmithKline|Medical University of Vienna Idiopathic Thrombocytopenic Purpura May 2009 Phase 4
NCT01762761 Novartis Pharmaceuticals|Novartis Purpura, Thrombocytopenic, Idiopathic and Hepatitis C February 18, 2013 Phase 3
NCT00358540 GlaxoSmithKline Sarcoma|Thrombocytopenia|Thrombocytopaenia|Thrombopoiesis June 2006 Phase 1
NCT00487968 GlaxoSmithKline Healthy Subjects|Purpura, Thrombocytopenic, Idiopathic May 2007 Phase 1
NCT01703169 University of Utah|Novartis Severe Aplastic Anemia|Very Severe Aplastic Anemia|Moderate Aplastic Anemia November 2012 Phase 2
NCT02773225 B. Höchsmann|University of Ulm Anemia, Aplastic March 2015 Phase 2|Phase 3
NCT01656252 PrECOG, LLC.|GlaxoSmithKline|Novartis Acute Myeloid Leukemia July 2012 Phase 1|Phase 2
NCT00903929 Jane Liesveld|University of Rochester Thrombocytopenia|Acute Radiation Syndrome December 2009 Phase 1
NCT02281370 GlaxoSmithKline Purpura, Thrombocytopenic, Idiopathic November 2014 Phase 1
NCT00424177 GlaxoSmithKline Purpura, Thrombocytopaenic, Idiopathic March 2007 Phase 2
NCT01000051 M.D. Anderson Cancer Center|Novartis Pharmaceuticals Thrombocytopenia February 2010 Phase 2
NCT01439321 GlaxoSmithKline Immune Thrombocytopenic Purpura November 2010
NCT02071901 Case Comprehensive Cancer Center|National Cancer Institute (NCI) Acute Myeloid Leukemia With Multilineage Dysplasia Following Myelodysplastic Syndrome|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 in Remission|Adult Acute Mye August 2014 Phase 2
NCT01621204 McMaster University|GlaxoSmithKline|Hamilton Health Sciences Corporation|Novartis Immune Thrombocytopenic Purpura October 2012 Phase 3
NCT01481220 Nordic MDS Group|GlaxoSmithKline Myelodysplastic Syndrome|Thrombocytopenia October 2011 Phase 1
NCT02404025 Novartis Pharmaceuticals|Novartis Cytopaenia May 2015 Phase 2
NCT01891994 National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) Severe Aplastic Anemia (SAA) June 17, 2013 Phase 2
NCT01821625 University of Texas Southwestern Medical Center|GlaxoSmithKline Thrombocytopenia|Hepatitis C April 2013 Phase 2|Phase 3
NCT02998645 Novartis Pharmaceuticals|Novartis Severe Aplastic Anemia May 19, 2017 Phase 2
NCT01772420 Albert Einstein College of Medicine, Inc.|National Cancer Institute (NCI) Adult Myelodysplastic Syndrome|Anemia|Chronic Myelomonocytic Leukemia October 2012 Phase 2
NCT02158936 Novartis Pharmaceuticals|Novartis Thrombocytopaenia February 1, 2010 Phase 3
NCT01064336 GlaxoSmithKline Purpura, Thrombocytopaenic, Idiopathic March 2010
NCT00903422 GlaxoSmithKline Myelodysplastic Syndrome May 2009 Phase 1
NCT01147809 GlaxoSmithKline Thrombocytopaenia June 2010 Phase 2
NCT00908037 GlaxoSmithKline Purpura, Thrombocytopaenic, Idiopathic September 2009 Phase 2
NCT03206086 National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) Fanconi's Anemia July 28, 2017 Phase 2
NCT00861601 GlaxoSmithKline Liver Diseases January 2009 Phase 2
NCT01098487 GlaxoSmithKline Purpura, Thrombocytopaenic, Idiopathic May 2010 Phase 4
NCT02834286 Hospital Universitario Dr. Jose E. Gonzalez Immune Thrombocytopenia March 2015 Phase 2
NCT01657552 GlaxoSmithKline Thrombocytopaenia August 2012 Phase 1
NCT01440374 Novartis Pharmaceuticals|Novartis Thrombocytopaenia September 2011 Phase 2
NCT00909363 Weill Medical College of Cornell University|Novartis Pharmaceuticals Wiskott-Aldrich Syndrome|Thrombocytopenia|Bleeding June 2009 Phase 2
NCT01433978 Eisai Inc. Idiopathic Thrombocytopenic Purpura April 2012 Phase 3
NCT01484314 Dana-Farber Cancer Institute Thrombocytopenia|Multiple Myeloma April 2012 Phase 2
NCT02912208 Associazione Qol-one Myelodysplastic Syndromes|Thrombocytopenia June 2011 Phase 2
NCT02446145 Technische Universität Dresden|Novartis Acute Myeloid Leukemia May 2015 Phase 2
NCT01328587 National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) Eltrombopag|Aplastic Anemia|Aplastic Anemia Treatment|Moderate Aplastic Anemia|Moderate Aplastic Anemia Treatment|Unilineage Bone Marrow Failure Disorders March 25, 2011 Phase 2
NCT00370331 GlaxoSmithKline Purpura, Thrombocytopaenic, Idiopathic November 2006 Phase 3
NCT00688272 GlaxoSmithKline Healthy Subjects|Purpura, Thrombocytopenic, Idiopathic June 2008 Phase 1
NCT00833378 GlaxoSmithKline Hepatitis C|Thrombocytopenia January 2009 Phase 1
NCT01416311 Novartis Purpura, Thrombocytopaenic, Idiopathic December 2010
NCT00529568 GlaxoSmithKline Hepatitis C, Chronic October 2007 Phase 3
NCT01890746 Novartis Leukaemia, Acute September 5, 2013 Phase 2
NCT01072162 GlaxoSmithKline Purpura, Thrombocytopenic, Idiopathic January 2010 Phase 1
NCT00961064 National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) Myelodysplastic Syndromes|Thrombocytopenia July 21, 2009 Phase 2
NCT02877212 Armed Forces Bone Marrow Transplant Center, Rawalpindi, Pakistan|Novartis Immune Thrombocytopenic Purpura (ITP) July 2016 Phase 3
NCT01113502 Abramson Cancer Center of the University of Pennsylvania Male and Female Subjects, Greater Than 60 Years of Age With Non-M3 AML April 2010 Phase 1|Phase 2
NCT03025698 Novartis Pharmaceuticals|Novartis Aplastic Anemia June 30, 2017 Phase 2
NCT00922883 National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) Anemia, Aplastic|Anemia, Hypoplastic|Thrombocytopenia May 20, 2009 Phase 2
NCT00359463 GlaxoSmithKline Hepatic Impairment|Purpura, Thrombocytopenic, Idiopathic April 2006 Phase 1
NCT02928419 Associazione Qol-one Myelodysplastic Syndromes May 2015 Phase 2
NCT00516321 GlaxoSmithKline Hepatitis C, Chronic October 2007 Phase 3
NCT00678587 GlaxoSmithKline Non-alcoholic Steatohepatitis|Chronic Liver Disease|HCV|NASH.|HIV Infection|Thrombocytopenia|Hepatitis C Virus|HBV|Human Immunodeficiency Virus|Liver Diseases|Hepatitis B Virus June 2008 Phase 3
NCT00442871 GlaxoSmithKline Renal Impairment|Purpura, Thrombocytopenic, Idiopathic September 2006 Phase 1
NCT01235988 GlaxoSmithKline Thrombocytopaenia August 2009
NCT01623167 National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) Aplastic Anemia|Neutropenia|Pancytopenia|Anemia|Thrombocytopenia June 7, 2012 Phase 1|Phase 2
NCT02099747 European Group for Blood and Marrow Transplantation|Novartis|Pfizer Severe Aplastic Anemia May 2015 Phase 3
NCT01458080 GlaxoSmithKline Hepatitis C May 2011
NCT01520909 GlaxoSmithKline Idiopathic Thrombocytopenic Purpura March 2012 Phase 3
NCT01236014 GlaxoSmithKline Thrombocytopaenia August 2009
NCT01715779 Novartis Hepatitis C August 2012
NCT02298075 Gruppo Italiano Malattie EMatologiche dell'Adulto Immune Thrombocytopenia April 2016
NCT00540423 GlaxoSmithKline Chronic Idiopathic Thrombocytopenic Purpura|Purpura, Thrombocytopenic, Idiopathic September 2007 Phase 3
NCT01636778 GlaxoSmithKline Hepatitis C, Chronic July 2012 Phase 2
NCT00102726 GlaxoSmithKline Thrombocytopaenia February 2005 Phase 2
NCT00110799 GlaxoSmithKline Hepatitis C, Chronic|Hepatitis C|Thrombocytopenia April 2005 Phase 2
NCT00102739 GlaxoSmithKline Purpura, Thrombocytopaenic, Idiopathic February 2005 Phase 2
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References
Molecular Weight

564.63

Formula

C₂₉H₃₆N₆O₆

CAS No.

496775-62-3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: >98.0%

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Eltrombopag Olamine
Cat. No.:
HY-15306A
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