Eltrombopag Olamine

作者: 莫小枫 | 来源:发表于2017-12-01 13:44 被阅读0次

    "目录号: HY-15306A

    Immunology/Inflammation-

    Eltrombopag乙醇胺是口服活性的促血小板生成素受体激动剂。

    Thrombopoietin Receptor

    相关产品

    Eltrombopag-Avatrombopag-Lusutrombopag-TPO agonist 1-

    生物活性

    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

    NCT02093325

    Chang Gung Memorial Hospital-GlaxoSmithKline

    Gynecologic Cancer

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    Phase 3

    NCT01500538

    Peter MacCallum Cancer Centre, Australia-GlaxoSmithKline-Merck Sharp & Dohme Corp.

    Follicular Lymphoma-Marginal Zone Lymphoma-Mantle Cell Lymphoma

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    Phase 2

    NCT01610180

    Fondazione Progetto Ematologia

    Purpura, Thrombocytopenic, Idiopathic-Autoimmune Thrombocytopenic Purpura-Autoimmune Thrombocytopenia-Chronic Lymphocytic Leukemia-Non Hodgkin's Lymphoma

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    Phase 2

    NCT01488565

    Peter MacCallum Cancer Centre, Australia-GlaxoSmithKline-Celgene Corporation

    Myelodysplastic Syndromes (MDS)-Acute Myeloid Leukaemia (AML)

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    Phase 2

    NCT01757145

    Rabin Medical Center

    Hematological Malignancy-Bone Marrow Failure Syndrome

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    NCT01133860

    IRCCS Policlinico S. Matteo-University of Pavia-GlaxoSmithKline-Azienda Ospedaliera di Padova-Azienda Ospedaliera di Perugia-Fondazione Telethon

    Blood Platelet Disorders

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    NCT01940562

    moshe yeshurun-GlaxoSmithKline-Rabin Medical Center

    Pediatric Patients Undergoing Allogeneic Cord Blood Transplantation.

    October 2013

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    NCT01880047

    Weill Medical College of Cornell University-Novartis

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    NCT02148133

    Novartis Pharmaceuticals-Novartis

    Cytopaenia

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    NCT02402998

    Gruppo Italiano Malattie EMatologiche dell'Adulto

    Primacy Immune Thrombocytopenia

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    GlaxoSmithKline

    Cirrhosis, Liver

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    NCT00643929

    GlaxoSmithKline

    Purpura, Thrombocytopaenic, Idiopathic

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    Dana-Farber Cancer Institute

    Multiple Myeloma

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    NCT01652599

    Hospital Universitario Dr. Jose E. Gonzalez

    Immune Thrombocytopenic Purpura

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    Phase 2

    NCT02201290

    Novartis Pharmaceuticals-Novartis

    Purpura, Thrombocytopenic, Idiopathic

    June 18, 2013

    Phase 3

    NCT01055600

    GlaxoSmithKline

    Thrombocytopaenia

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    Gruppo Italiano Malattie EMatologiche dell'Adulto

    Thrombocytopenia

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    NCT01286038

    H. Lee Moffitt Cancer Center and Research Institute-GlaxoSmithKline

    Myelodysplastic Syndrome (MDS)-Thrombocytopenia

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    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

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    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

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    Phase 4

    NCT01762761

    Novartis Pharmaceuticals-Novartis

    Purpura, Thrombocytopenic, Idiopathic and Hepatitis C

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    Phase 3

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    GlaxoSmithKline

    Sarcoma-Thrombocytopenia-Thrombocytopaenia-Thrombopoiesis

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    GlaxoSmithKline

    Healthy Subjects-Purpura, Thrombocytopenic, Idiopathic

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    University of Utah-Novartis

    Severe Aplastic Anemia-Very Severe Aplastic Anemia-Moderate Aplastic Anemia

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    NCT02773225

    B. Höchsmann-University of Ulm

    Anemia, Aplastic

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    Phase 2-Phase 3

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    PrECOG, LLC.-GlaxoSmithKline-Novartis

    Acute Myeloid Leukemia

    July 2012

    Phase 1-Phase 2

    NCT00903929

    Jane Liesveld-University of Rochester

    Thrombocytopenia-Acute Radiation Syndrome

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    NCT02281370

    GlaxoSmithKline

    Purpura, Thrombocytopenic, Idiopathic

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    GlaxoSmithKline

    Purpura, Thrombocytopaenic, Idiopathic

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    Phase 2

    NCT01000051

    M.D. Anderson Cancer Center-Novartis Pharmaceuticals

    Thrombocytopenia

    February 2010

    Phase 2

    NCT01439321

    GlaxoSmithKline

    Immune Thrombocytopenic Purpura

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    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

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