메뉴 건너뛰기




Volumn 27, Issue 2, 2009, Pages 424-430

Preclinical activity of eltrombopag (sb-497115), an oral, nonpeptide thrombopoietin receptor agonist

Author keywords

Differentiation; Megakaryocyte; Thrombocytopenia; Thrombopoietin receptor agonist

Indexed keywords

CASPASE 3; CASPASE 7; CD34 ANTIGEN; ELTROMBOPAG; FIBRINOGEN RECEPTOR; STAT PROTEIN; STAT5 PROTEIN; THROMBOPOIETIN RECEPTOR;

EID: 62549153611     PISSN: 10665099     EISSN: None     Source Type: Journal    
DOI: 10.1634/stemcells.2008-0366     Document Type: Article
Times cited : (243)

References (31)
  • 1
    • 0036728936 scopus 로고    scopus 로고
    • Diagnosis and management of aplastic anemia and myclodysplaslic syndrome
    • Paquette RL. Diagnosis and management of aplastic anemia and myclodysplaslic syndrome. Oncology (Williston Park) 2002; 16(suppl 10):153-161.
    • (2002) Oncology (Williston Park) , vol.16 , Issue.SUPPL. 10 , pp. 153-161
    • Paquette, R.L.1
  • 2
    • 33751377242 scopus 로고    scopus 로고
    • Chronic Idiopathic Thrombocytopenic purpura: Present strategy, guidelines and new insights
    • Stevens W, Koene H, Zwaginga JJ et al. Chronic Idiopathic Thrombocytopenic purpura: Present strategy, guidelines and new insights. Neth J Med 2006;64:356-363.
    • (2006) Neth J Med , vol.64 , pp. 356-363
    • Stevens, W.1    Koene, H.2    Zwaginga, J.J.3
  • 3
    • 33748910858 scopus 로고    scopus 로고
    • Tijssen MR, van der School CE, Voermans C et al. Clinical approaches involving thrombopoietin to shorten the period of thrombocytopenia after high-dose chemotherapy. Transfus Med Rev 2006;20:253-293.
    • Tijssen MR, van der School CE, Voermans C et al. Clinical approaches involving thrombopoietin to shorten the period of thrombocytopenia after high-dose chemotherapy. Transfus Med Rev 2006;20:253-293.
  • 4
    • 33646862604 scopus 로고    scopus 로고
    • Review article: Thrombocytopenia in chronic liver disease and pharmacologic treatment options
    • Giannini EG. Review article: Thrombocytopenia in chronic liver disease and pharmacologic treatment options. Aliment Pharmacol Ther 2006;23: 1055-1065.
    • (2006) Aliment Pharmacol Ther , vol.23 , pp. 1055-1065
    • Giannini, E.G.1
  • 5
    • 0029553308 scopus 로고
    • A laboratory and thromhokinetic study of HCV-associated thrombocytopenia: A direct role of HCV in bone marrow exhaustion?
    • Bordin G. Ballare M Zigrossi P et al. A laboratory and thromhokinetic study of HCV-associated thrombocytopenia: A direct role of HCV in bone marrow exhaustion? Clin Exp Rheumatol 1995;13(suppl 13):S39-S43.
    • (1995) Clin Exp Rheumatol , vol.13 , Issue.SUPPL. 13
    • Bordin, G.1    Ballare, M.2    Zigrossi, P.3
  • 6
    • 0037071389 scopus 로고    scopus 로고
    • The molecular and cellular biology of thrombopoietin: The primary regulator of platelet production
    • Kaushansky K, Drachman JG. The molecular and cellular biology of thrombopoietin: The primary regulator of platelet production. Oncogene 2002;21:3359-3367.
    • (2002) Oncogene , vol.21 , pp. 3359-3367
    • Kaushansky, K.1    Drachman, J.G.2
  • 7
    • 0037111558 scopus 로고    scopus 로고
    • Recombinant human thrombopoietin: Basic biology and evaluation of clinical studies
    • Kilter DJ, Begley CG. Recombinant human thrombopoietin: Basic biology and evaluation of clinical studies. Blood 2002;100:3457-3469.
    • (2002) Blood , vol.100 , pp. 3457-3469
    • Kilter, D.J.1    Begley, C.G.2
  • 8
    • 0028827190 scopus 로고
    • Thrombopoietin, c-Mpl ligand, induces tyrosine phosphorylation of Tyk2, JAK2, and STAT3, and enhances agonists-induced aggregation in platelets in vitro
    • Ezumi Y, Takayama H, Okuma M. Thrombopoietin, c-Mpl ligand, induces tyrosine phosphorylation of Tyk2, JAK2, and STAT3, and enhances agonists-induced aggregation in platelets in vitro. FEBS Lett 1995;374:48-52.
    • (1995) FEBS Lett , vol.374 , pp. 48-52
    • Ezumi, Y.1    Takayama, H.2    Okuma, M.3
  • 9
    • 0033532069 scopus 로고    scopus 로고
    • Thrombopoietin signal transduction requires functional JAK2, not TYK2
    • Drachman JG, Millet KM, Kaushansky K. Thrombopoietin signal transduction requires functional JAK2, not TYK2. J Biol Chem 1999;274: 13480-13484.
    • (1999) J Biol Chem , vol.274 , pp. 13480-13484
    • Drachman, J.G.1    Millet, K.M.2    Kaushansky, K.3
  • 10
    • 0033566712 scopus 로고    scopus 로고
    • Thrombopoietin-induced activation of the milogen-activated protein kinase (MAPK) pathway in normal megakaryocytes: Role in endomitosis
    • Rojnuckarin P, Drachman JG, Kaushansky K. Thrombopoietin-induced activation of the milogen-activated protein kinase (MAPK) pathway in normal megakaryocytes: Role in endomitosis. Blood 1999;94:1273-1282.
    • (1999) Blood , vol.94 , pp. 1273-1282
    • Rojnuckarin, P.1    Drachman, J.G.2    Kaushansky, K.3
  • 11
    • 0028343099 scopus 로고    scopus 로고
    • Bartley TD, Bogenberger J, Hunt P et al. Identification and cloning of a megakaryocyte growth and development factor that is a ligand for the cytokine receptor Mpl. Cell 1994;77:1117-1124.
    • Bartley TD, Bogenberger J, Hunt P et al. Identification and cloning of a megakaryocyte growth and development factor that is a ligand for the cytokine receptor Mpl. Cell 1994;77:1117-1124.
  • 12
    • 0028302409 scopus 로고
    • Stimulation of megakaryocyto-poiesis and thrombopoiesis by the c-Mpl ligand
    • de Sanvage FJ, Hass PE, Spencer SD et al. Stimulation of megakaryocyto-poiesis and thrombopoiesis by the c-Mpl ligand. Nature 1994;369:533-538.
    • (1994) Nature , vol.369 , pp. 533-538
    • de Sanvage, F.J.1    Hass, P.E.2    Spencer, S.D.3
  • 13
    • 0028332474 scopus 로고
    • Promotion of megakaryocyte progenitor expansion and differentiation by the c-Mpl ligand thrombopoietin
    • Kaushansky K, Lok S, Holly RD et al. Promotion of megakaryocyte progenitor expansion and differentiation by the c-Mpl ligand thrombopoietin. Nature 1994;369:568-571.
    • (1994) Nature , vol.369 , pp. 568-571
    • Kaushansky, K.1    Lok, S.2    Holly, R.D.3
  • 14
    • 0028199208 scopus 로고
    • Cloning and expression of murine thrombopoietin cDNA and stimulation of platelet production in vivo
    • Lok S, Kaushansky K, Holly RD et al. Cloning and expression of murine thrombopoietin cDNA and stimulation of platelet production in vivo. Nature 1994;369:565-568.
    • (1994) Nature , vol.369 , pp. 565-568
    • Lok, S.1    Kaushansky, K.2    Holly, R.D.3
  • 15
    • 0028176283 scopus 로고
    • cMpl ligand is a humoral regulator of megakaryocytopoiesis
    • Wendling F, Maraskovsky E, Debili N et al. cMpl ligand is a humoral regulator of megakaryocytopoiesis. Nature 1994;369:571-574.
    • (1994) Nature , vol.369 , pp. 571-574
    • Wendling, F.1    Maraskovsky, E.2    Debili, N.3
  • 16
    • 0035760892 scopus 로고    scopus 로고
    • Thrombocytopenia caused by the development of antibodies to thrombopoietin
    • Li J, Yang C, Xia Y et al. Thrombocytopenia caused by the development of antibodies to thrombopoietin. Blood 2001;98:3241-3248.
    • (2001) Blood , vol.98 , pp. 3241-3248
    • Li, J.1    Yang, C.2    Xia, Y.3
  • 17
    • 19944432021 scopus 로고    scopus 로고
    • Discovery and characterization of a selective, nonpeptidyl thrombopoietin receptor agonist
    • Erickson-Miller CL, DeLorme E, Tian SS et al. Discovery and characterization of a selective, nonpeptidyl thrombopoietin receptor agonist. Exp Hematol 2005;33:85-93.
    • (2005) Exp Hematol , vol.33 , pp. 85-93
    • Erickson-Miller, C.L.1    DeLorme, E.2    Tian, S.S.3
  • 18
    • 0035950101 scopus 로고    scopus 로고
    • Hydrazinonaphthalene and azonaphthalene thrombopoietin mimics are nonpeptidyl promoters of megakaryocytopoiesis
    • Duffy KJ, Darcy MG, Delorme E et al. Hydrazinonaphthalene and azonaphthalene thrombopoietin mimics are nonpeptidyl promoters of megakaryocytopoiesis. J Med Chem 2001;44:3730-3745.
    • (2001) J Med Chem , vol.44 , pp. 3730-3745
    • Duffy, K.J.1    Darcy, M.G.2    Delorme, E.3
  • 19
    • 0037103339 scopus 로고    scopus 로고
    • Identification of a pharmacophore for thrombopoietie activity of small, non-peptidyl molecules. 1. Discovery and optimization of salicylaldehyde thiosemicarbazone thrombopoietin mimics
    • Duffy KJ, Shaw AN, Delorme E et al. Identification of a pharmacophore for thrombopoietie activity of small, non-peptidyl molecules. 1. Discovery and optimization of salicylaldehyde thiosemicarbazone thrombopoietin mimics. J Med Chem 2002;45:3573-3575.
    • (2002) J Med Chem , vol.45 , pp. 3573-3575
    • Duffy, K.J.1    Shaw, A.N.2    Delorme, E.3
  • 20
    • 0037103160 scopus 로고    scopus 로고
    • Identification of a pharmacophore for thrombopoietie activity of small, non-peptidyl molecules. 2. Rational design of naphtho[l .2-d]imidazole thrombopoietin mimics
    • Duffy KJ, Price AT, Delorme E et al. Identification of a pharmacophore for thrombopoietie activity of small, non-peptidyl molecules. 2. Rational design of naphtho[l .2-d]imidazole thrombopoietin mimics. J Med Chem 2002;45:3576-3578.
    • (2002) J Med Chem , vol.45 , pp. 3576-3578
    • Duffy, K.J.1    Price, A.T.2    Delorme, E.3
  • 21
    • 33744497342 scopus 로고    scopus 로고
    • Species specificity and receptor domain interaction of a small molecule TpoR agonist
    • Erickson-Miller C, DeLorme E, Iskandar M et al. Species specificity and receptor domain interaction of a small molecule TpoR agonist. Blood 2004; 104:2909.
    • (2004) Blood , vol.104 , pp. 2909
    • Erickson-Miller, C.1    DeLorme, E.2    Iskandar, M.3
  • 22
    • 33744456732 scopus 로고    scopus 로고
    • A novel nonpelidyl human c-Mpl activator stimulates human megakaryocytopoiesis and thrombosis
    • Nakamura T, Miyakawa Y, Miyamura A et al. A novel nonpelidyl human c-Mpl activator stimulates human megakaryocytopoiesis and thrombosis. Blood 2006:107:4300-4307.
    • (2006) Blood , vol.107 , pp. 4300-4307
    • Nakamura, T.1    Miyakawa, Y.2    Miyamura, A.3
  • 23
    • 34347210686 scopus 로고    scopus 로고
    • NMR structural studies of interactions of a small, nonpeptidyl Tpo mimic with the thrombopoietin receptor extracellular juxtamembrane and transmembrane domains
    • Kim M-J, Park SH, Opella SJ et al. NMR structural studies of interactions of a small, nonpeptidyl Tpo mimic with the thrombopoietin receptor extracellular juxtamembrane and transmembrane domains. J Biol Chem 2007;282:14253-14261.
    • (2007) J Biol Chem , vol.282 , pp. 14253-14261
    • Kim, M.-J.1    Park, S.H.2    Opella, S.J.3
  • 24
    • 33845316584 scopus 로고    scopus 로고
    • A low molecular weight, orally active TpoR agonist, SB-497115, does not prime platelets for activation or agonist-induced aggregation in vitro
    • Erhardt J, Tapley P, Erickson-Miller, C. A low molecular weight, orally active TpoR agonist, SB-497115, does not prime platelets for activation or agonist-induced aggregation in vitro. Exper Hematol 2005:33(1 suppl):365.
    • (2005) Exper Hematol , vol.33 , Issue.1 SUPPL. , pp. 365
    • Erhardt, J.1    Tapley, P.2    Erickson-Miller, C.3
  • 25
    • 34249719511 scopus 로고    scopus 로고
    • Phase I clinical study of eltrombopag. an oral, nonpeptide thrombopoietin receptor agonist
    • Jenkins JM, Williams D, Deng Y et al. Phase I clinical study of eltrombopag. an oral, nonpeptide thrombopoietin receptor agonist Blood 2007; 109:4739-4741.
    • (2007) Blood , vol.109 , pp. 4739-4741
    • Jenkins, J.M.1    Williams, D.2    Deng, Y.3
  • 26
    • 0029943307 scopus 로고    scopus 로고
    • Dose-response effects of pegylatcd human megakaryocyte growth and development factor on platelet production and function in nonhuman primates
    • Harker LA, Marzec UM, Hunt P et al. Dose-response effects of pegylatcd human megakaryocyte growth and development factor on platelet production and function in nonhuman primates. Blood 1996;88:511-521.
    • (1996) Blood , vol.88 , pp. 511-521
    • Harker, L.A.1    Marzec, U.M.2    Hunt, P.3
  • 27
    • 0034656323 scopus 로고    scopus 로고
    • Effects of megakaryocyte growth and development factor on platelet production, platelet life span, and platelet function in healthy human volunteers
    • Harker LA, Roskos LK, Marzec UM et al. Effects of megakaryocyte growth and development factor on platelet production, platelet life span, and platelet function in healthy human volunteers. Blood 2000; 95:2514-2522.
    • (2000) Blood , vol.95 , pp. 2514-2522
    • Harker, L.A.1    Roskos, L.K.2    Marzec, U.M.3
  • 28
    • 36549001698 scopus 로고    scopus 로고
    • Eltrombopag for the treatment of chronic idiopathic thrombocytopenic purpura
    • Bussel JB, Cheng G, Saleh MN et al. Eltrombopag for the treatment of chronic idiopathic thrombocytopenic purpura. N Engl J Med 2007;357: 2237-2247.
    • (2007) N Engl J Med , vol.357 , pp. 2237-2247
    • Bussel, J.B.1    Cheng, G.2    Saleh, M.N.3
  • 29
    • 37149046846 scopus 로고    scopus 로고
    • Evaluating safety and efficacy of AMG 531 for the treatment of thrombocytopenic patients with my-elodysplastic syndrome (MDS): Preliminary results of a phase 1/2 study
    • Kantaijian HM, Giles FJ, Fenaux P et al. Evaluating safety and efficacy of AMG 531 for the treatment of thrombocytopenic patients with my-elodysplastic syndrome (MDS): Preliminary results of a phase 1/2 study. J Clin Oncol 2007;25(18 suppl):7032.
    • (2007) J Clin Oncol , vol.25 , Issue.18 SUPPL. , pp. 7032
    • Kantaijian, H.M.1    Giles, F.J.2    Fenaux, P.3
  • 30
    • 36549047972 scopus 로고    scopus 로고
    • Eltrombopag for thrombocytopenia in patients with cirrhosis associated with hepatitis C
    • McFIutchison JG. Dusbeiko G, Shiftman ML et al. Eltrombopag for thrombocytopenia in patients with cirrhosis associated with hepatitis C. N Engl J Med 2007;357:2227-2236.
    • (2007) N Engl J Med , vol.357 , pp. 2227-2236
    • McFIutchison, J.G.1    Dusbeiko, G.2    Shiftman, M.L.3
  • 31
    • 62549113252 scopus 로고    scopus 로고
    • The discovery of eltrombopag, an orally bioavailable TpoR agonist
    • Metcalf BW, Dillon S, eds, Burlington. MA: Academic Press
    • Duffy KJ, Firickson-Miller CL. The discovery of eltrombopag, an orally bioavailable TpoR agonist. In: Metcalf BW, Dillon S, eds. Target Validation in Drug Discovery. Burlington. MA: Academic Press, 2007:241-254.
    • (2007) Target Validation in Drug Discovery , pp. 241-254
    • Duffy, K.J.1    Firickson-Miller, C.L.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.