抑制剂、调节剂、激动剂及化合物分子库

Eltrombopag

2017-12-01  本文已影响0人  莫小枫

"目录号: HY-15306

Immunology/Inflammation-

Eltrombopag(SB-497115)是口服活性的促血小板生成素受体激动剂,能刺激血小板生成。

Thrombopoietin Receptor

相关产品

Eltrombopag Olamine-Avatrombopag-Lusutrombopag-TPO agonist 1-

生物活性

Description

Eltrombopag(SB-497115) 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

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

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