"目錄號(hào): HY-15306A
Eltrombopag乙醇胺是口服活性的促血小板生成素受體激動(dòng)劑贾陷。
相關(guān)產(chǎn)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
Chang Gung Memorial Hospital-GlaxoSmithKline
Gynecologic Cancer
March 2014
Phase 3
Peter MacCallum Cancer Centre, Australia-GlaxoSmithKline-Merck Sharp & Dohme Corp.
Follicular Lymphoma-Marginal Zone Lymphoma-Mantle Cell Lymphoma
October 2012
Phase 2
Fondazione Progetto Ematologia
Purpura, Thrombocytopenic, Idiopathic-Autoimmune Thrombocytopenic Purpura-Autoimmune Thrombocytopenia-Chronic Lymphocytic Leukemia-Non Hodgkin's Lymphoma
June 2012
Phase 2
Peter MacCallum Cancer Centre, Australia-GlaxoSmithKline-Celgene Corporation
Myelodysplastic Syndromes (MDS)-Acute Myeloid Leukaemia (AML)
December 2010
Phase 2
Rabin Medical Center
Hematological Malignancy-Bone Marrow Failure Syndrome
January 2013
Phase 2
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
moshe yeshurun-GlaxoSmithKline-Rabin Medical Center
Pediatric Patients Undergoing Allogeneic Cord Blood Transplantation.
October 2013
Phase 2
Weill Medical College of Cornell University-Novartis
Immune Thrombocytopenia-Platelet Disorder
February 2013
Phase 2
Novartis Pharmaceuticals-Novartis
Cytopaenia
July 2014
Phase 2
Gruppo Italiano Malattie EMatologiche dell'Adulto
Primacy Immune Thrombocytopenia
June 2015
Phase 2
GlaxoSmithKline
Cirrhosis, Liver
August 2014
Phase 1
GlaxoSmithKline
Purpura, Thrombocytopaenic, Idiopathic
February 2007
Dana-Farber Cancer Institute
Multiple Myeloma
March 2011
Hospital Universitario Dr. Jose E. Gonzalez
Immune Thrombocytopenic Purpura
June 2012
Phase 2
Novartis Pharmaceuticals-Novartis
Purpura, Thrombocytopenic, Idiopathic
June 18, 2013
Phase 3
GlaxoSmithKline
Thrombocytopaenia
March 2013
Phase 4
Gruppo Italiano Malattie EMatologiche dell'Adulto
Thrombocytopenia
September 2013
Phase 2
H. Lee Moffitt Cancer Center and Research Institute-GlaxoSmithKline
Myelodysplastic Syndrome (MDS)-Thrombocytopenia
March 2011
Phase 1-Phase 2
Weill Medical College of Cornell University-Novartis
Immune Thrombocytopenia
June 2011
Novartis Pharmaceuticals-Novartis
Purpura, Thrombocytopaenic, Idiopathic
June 2006
Phase 3
GlaxoSmithKline
Idiopathic Thrombocytopenic Purpura-Purpura, Thrombocytopenic, Idiopathic
May 2008
Phase 3
M.D. Anderson Cancer Center-Novartis Pharmaceuticals
Blood And Marrow Transplantation
October 2013
Phase 2
University of Cincinnati-GlaxoSmithKline
Thrombocytopenia
August 2010
Phase 2
Weill Medical College of Cornell University-GlaxoSmithKline
Idiopathic Thrombocytopenic Purpura
January 2009
Phase 2
IRCCS Policlinico S. Matteo
Inherited Platelet Disorder
April 2015
Phase 2
M.D. Anderson Cancer Center-GlaxoSmithKline
Leukemia
March 2014
Phase 2
University of Ulm-GlaxoSmithKline-German CLL Study Group-WiSP Wissenschaftlicher Service Pharma GmbH
Chronic Lymphocytic Leukemia-Thrombocytopenia
October 2011
Phase 1-Phase 2
GlaxoSmithKline
Hepatitis C
September 2009
Phase 3
Duke University-GlaxoSmithKline
Sarcoma, Soft Tissue-Osteosarcoma-Neoplasms, Connective and Soft Tissue
April 2012
Phase 1
Groupe Francophone des Myelodysplasies-GlaxoSmithKline-Novartis
CMML-Thrombocytopenia
August 7, 2014
Phase 1-Phase 2
M.D. Anderson Cancer Center-GlaxoSmithKline-Novartis
Leukemia
October 2013
Phase 2
M.D. Anderson Cancer Center-Novartis Pharmaceuticals
Leukemia-Chronic Myeloid Leukemia-Myelofibrosis
January 13, 2012
Phase 2
M.D. Anderson Cancer Center-GlaxoSmithKline
CLL-Leukemia
November 2010
Phase 2
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
Ingrid Pabinger, MD-GlaxoSmithKline-Medical University of Vienna
Idiopathic Thrombocytopenic Purpura
May 2009
Phase 4
Novartis Pharmaceuticals-Novartis
Purpura, Thrombocytopenic, Idiopathic and Hepatitis C
February 18, 2013
Phase 3
GlaxoSmithKline
Sarcoma-Thrombocytopenia-Thrombocytopaenia-Thrombopoiesis
June 2006
Phase 1
GlaxoSmithKline
Healthy Subjects-Purpura, Thrombocytopenic, Idiopathic
May 2007
Phase 1
University of Utah-Novartis
Severe Aplastic Anemia-Very Severe Aplastic Anemia-Moderate Aplastic Anemia
November 2012
Phase 2
B. H?chsmann-University of Ulm
Anemia, Aplastic
March 2015
Phase 2-Phase 3
PrECOG, LLC.-GlaxoSmithKline-Novartis
Acute Myeloid Leukemia
July 2012
Phase 1-Phase 2
Jane Liesveld-University of Rochester
Thrombocytopenia-Acute Radiation Syndrome
December 2009
Phase 1
GlaxoSmithKline
Purpura, Thrombocytopenic, Idiopathic
November 2014
Phase 1
GlaxoSmithKline
Purpura, Thrombocytopaenic, Idiopathic
March 2007
Phase 2
M.D. Anderson Cancer Center-Novartis Pharmaceuticals
Thrombocytopenia
February 2010
Phase 2
GlaxoSmithKline
Immune Thrombocytopenic Purpura
November 2010
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
