메뉴 건너뛰기




Volumn 33, Issue 2, 2015, Pages 357-370

Pharmacokinetic, pharmacodynamic and biomarker evaluation of transforming growth factor-β receptor i kinase inhibitor, galunisertib, in phase 1 study in patients with advanced cancer

Author keywords

First in Human Dose; Galunisertib; Glioma; Pharmacodynamics; Pharmacokinetics; TGF inhibitor

Indexed keywords

ADAM PROTEIN; ADAM11 PROTEIN, HUMAN; ANTICONVULSIVE AGENT; LOMUSTINE; LY-2157299; MACROPHAGE DERIVED CHEMOKINE; PROTEIN SERINE THREONINE KINASE; PROTON PUMP INHIBITOR; PYRAZOLE DERIVATIVE; QUINOLINE DERIVATIVE; SMAD2 PROTEIN; TGF-BETA TYPE I RECEPTOR; TRANSFORMING GROWTH FACTOR BETA RECEPTOR; TUMOR SUPPRESSOR PROTEIN;

EID: 84939789948     PISSN: 01676997     EISSN: 15730646     Source Type: Journal    
DOI: 10.1007/s10637-014-0192-4     Document Type: Article
Times cited : (93)

References (32)
  • 1
    • 0346254671 scopus 로고
    • New class of transforming growth factors potentiated by epidermal growth factor: Isolation from non-neoplastic tissues
    • 348740 1:CAS:528:DyaL3MXlvVWmsLo%3D 6975480
    • Roberts AB, Anzano MA, Lamb LC, Smith JM, Sporn MB (1981) New class of transforming growth factors potentiated by epidermal growth factor: isolation from non-neoplastic tissues. Proc Natl Acad Sci U S A 78:5339-5343
    • (1981) Proc Natl Acad Sci U S A , vol.78 , pp. 5339-5343
    • Roberts, A.B.1    Anzano, M.A.2    Lamb, L.C.3    Smith, J.M.4    Sporn, M.B.5
  • 2
    • 0034644472 scopus 로고    scopus 로고
    • TGFbeta signaling in growth control, cancer, and heritable disorders
    • 1:CAS:528:DC%2BD3cXns1Clt7w%3D 11057902
    • Massague J, Blain SW, Lo RS (2000) TGFbeta signaling in growth control, cancer, and heritable disorders. Cell 103:295-309
    • (2000) Cell , vol.103 , pp. 295-309
    • Massague, J.1    Blain, S.W.2    Lo, R.S.3
  • 3
    • 7444226411 scopus 로고    scopus 로고
    • SD-208, a novel transforming growth factor beta receptor i kinase inhibitor, inhibits growth and invasiveness and enhances immunogenicity of murine and human glioma cells in vitro and in vivo
    • 1:CAS:528:DC%2BD2cXptFels78%3D 15520202
    • Uhl M, Aulwurm S, Wischhusen J, Weiler M, Ma JY, Almirez R et al (2004) SD-208, a novel transforming growth factor beta receptor I kinase inhibitor, inhibits growth and invasiveness and enhances immunogenicity of murine and human glioma cells in vitro and in vivo. Cancer Res 64:7954-7961
    • (2004) Cancer Res , vol.64 , pp. 7954-7961
    • Uhl, M.1    Aulwurm, S.2    Wischhusen, J.3    Weiler, M.4    Ma, J.Y.5    Almirez, R.6
  • 4
    • 78649986150 scopus 로고    scopus 로고
    • TGF-beta receptor inhibitors target the CD44(high)/Id1(high) glioma-initiating cell population in human glioblastoma
    • 1:CAS:528:DC%2BC3cXhsFGhsbjP 21156287
    • Anido J, Saez-Borderias A, Gonzalez-Junca A, Rodon L, Folch G, Carmona MA et al (2010) TGF-beta receptor inhibitors target the CD44(high)/Id1(high) glioma-initiating cell population in human glioblastoma. Cancer Cell 18:655-668
    • (2010) Cancer Cell , vol.18 , pp. 655-668
    • Anido, J.1    Saez-Borderias, A.2    Gonzalez-Junca, A.3    Rodon, L.4    Folch, G.5    Carmona, M.A.6
  • 5
    • 79951602633 scopus 로고    scopus 로고
    • Targeted therapy for high-grade glioma with the TGF-beta2 inhibitor trabedersen: Results of a randomized and controlled phase IIb study
    • 1:CAS:528:DC%2BC3MXhvFOiur8%3D
    • Bogdahn U, Hau P, Stockhammer G, Venkataramana NK, Mahapatra AK, Suri A et al (2011) Targeted therapy for high-grade glioma with the TGF-beta2 inhibitor trabedersen: results of a randomized and controlled phase IIb study. Neurol Oncol 13:132-142
    • (2011) Neurol Oncol , vol.13 , pp. 132-142
    • Bogdahn, U.1    Hau, P.2    Stockhammer, G.3    Venkataramana, N.K.4    Mahapatra, A.K.5    Suri, A.6
  • 6
    • 0037620888 scopus 로고    scopus 로고
    • Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type i receptor kinase domain
    • 1:CAS:528:DC%2BD3sXmtFOlsLw%3D 12954047
    • Sawyer JS, Anderson BD, Beight DW, Campbell RM, Jones ML, Herron DK et al (2003) Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain. J Med Chem 46:3953-3956
    • (2003) J Med Chem , vol.46 , pp. 3953-3956
    • Sawyer, J.S.1    Anderson, B.D.2    Beight, D.W.3    Campbell, R.M.4    Jones, M.L.5    Herron, D.K.6
  • 7
    • 84899071195 scopus 로고    scopus 로고
    • Defining a therapeutic window for the novel TGF-β inhibitor GALUNISERTIB monohydrate based on a pharmacokinetic/pharmacodynamic model
    • 1:CAS:528:DC%2BC2cXmvVyrtrs%3D 24868575
    • Gueorguieva I, Cleverly AL, Stauber A, Pillay NS, Rodon JA, Miles CP et al (2014) Defining a therapeutic window for the novel TGF-β inhibitor GALUNISERTIB monohydrate based on a pharmacokinetic/pharmacodynamic model. Br J Clin Pharmacol 77:796-807
    • (2014) Br J Clin Pharmacol , vol.77 , pp. 796-807
    • Gueorguieva, I.1    Cleverly, A.L.2    Stauber, A.3    Pillay, N.S.4    Rodon, J.A.5    Miles, C.P.6
  • 8
    • 84939936746 scopus 로고    scopus 로고
    • First-in-Human Dose Study of the Novel Transforming Growth Factor-β Receptor i Kinase Inhibitor LY2157299 Monohydrate in Patients with Advanced Cancer and Glioma
    • (In press 2014)
    • Rodon J, Carducci MA, Sepúlveda JM, Azaro A, Calvo E, Seoane J, et al. (2013) First-in-Human Dose Study of the Novel Transforming Growth Factor-β Receptor I Kinase Inhibitor LY2157299 Monohydrate in Patients with Advanced Cancer and Glioma. Clin Cancer Res (In press 2014)
    • (2013) Clin Cancer Res
    • Rodon, J.1    Carducci, M.A.2    Sepúlveda, J.M.3    Azaro, A.4    Calvo, E.5    Seoane, J.6
  • 9
    • 34247617701 scopus 로고    scopus 로고
    • Development and validation of a phosphorylated SMAD ex vivo stimulation assay
    • 1:CAS:528:DC%2BD2sXmtVOjtbw%3D 17453744
    • Farrington DL, Yingling JM, Fill JA, Yan L, Qian YW, Shou J et al (2007) Development and validation of a phosphorylated SMAD ex vivo stimulation assay. Biomarkers 12:313-330
    • (2007) Biomarkers , vol.12 , pp. 313-330
    • Farrington, D.L.1    Yingling, J.M.2    Fill, J.A.3    Yan, L.4    Qian, Y.W.5    Shou, J.6
  • 10
    • 39149139338 scopus 로고    scopus 로고
    • TGF-beta signalling-related markers in cancer patients with bone metastasis
    • 1:CAS:528:DC%2BD1cXhsleltrY%3D 18270872
    • Baselga J, Rothenberg ML, Tabernero J, Seoane J, Daly T, Cleverly A et al (2008) TGF-beta signalling-related markers in cancer patients with bone metastasis. Biomarkers 13:217-236
    • (2008) Biomarkers , vol.13 , pp. 217-236
    • Baselga, J.1    Rothenberg, M.L.2    Tabernero, J.3    Seoane, J.4    Daly, T.5    Cleverly, A.6
  • 11
    • 0025281789 scopus 로고
    • Response criteria for phase II studies of supratentorial malignant glioma
    • 1:STN:280:DyaK3c3ptlyitQ%3D%3D 2358840
    • Macdonald DR, Cascino TL, Schold SC Jr, Cairncross JG (1990) Response criteria for phase II studies of supratentorial malignant glioma. J Clin Oncol 8:1277-1280
    • (1990) J Clin Oncol , vol.8 , pp. 1277-1280
    • Macdonald, D.R.1    Cascino, T.L.2    Schold, Jr.S.C.3    Cairncross, J.G.4
  • 12
    • 58149125873 scopus 로고    scopus 로고
    • Influence of enzyme-inducing antiepileptic drugs on trough level of Imatinib in glioblastoma patients
    • 2748699 1:CAS:528:DC%2BD1MXitF2hsbc%3D 18781906
    • Pursche S, Schleyer E, von Bonin M, Ehninger G, Said SM, Prondzinsky R et al (2008) Influence of enzyme-inducing antiepileptic drugs on trough level of Imatinib in glioblastoma patients. Curr Clin Pharmacol 3:198-203
    • (2008) Curr Clin Pharmacol , vol.3 , pp. 198-203
    • Pursche, S.1    Schleyer, E.2    Von Bonin, M.3    Ehninger, G.4    Said, S.M.5    Prondzinsky, R.6
  • 13
    • 84887491073 scopus 로고    scopus 로고
    • Development and validation of a clinical cancer genomic profiling test based on massively parallel DNA sequencing
    • 1:CAS:528:DC%2BC3sXhs1CitLbE
    • Frampton GM, Fichtenholtz A, Otto GA, Wang K, Downing SR, He J et al (2013) Development and validation of a clinical cancer genomic profiling test based on massively parallel DNA sequencing. Nature Biotechnol 31:1023-1031
    • (2013) Nature Biotechnol , vol.31 , pp. 1023-1031
    • Frampton, G.M.1    Fichtenholtz, A.2    Otto, G.A.3    Wang, K.4    Downing, S.R.5    He, J.6
  • 14
    • 79961140711 scopus 로고    scopus 로고
    • Genomic profiles of glioma
    • 21465149
    • Brennan C (2011) Genomic profiles of glioma. Curr Neurol Neurosci Rep 11:291-297
    • (2011) Curr Neurol Neurosci Rep , vol.11 , pp. 291-297
    • Brennan, C.1
  • 15
    • 52949127312 scopus 로고    scopus 로고
    • An integrated genomic analysis of human glioblastoma multiforme
    • 2820389 1:CAS:528:DC%2BD1cXhtFCrtLrE 18772396
    • Parsons DW, Jones S, Zhang X, Lin JC, Leary RJ, Angenendt P et al (2008) An integrated genomic analysis of human glioblastoma multiforme. Science 321:1807-1812
    • (2008) Science , vol.321 , pp. 1807-1812
    • Parsons, D.W.1    Jones, S.2    Zhang, X.3    Lin, J.C.4    Leary, R.J.5    Angenendt, P.6
  • 16
    • 84865520089 scopus 로고    scopus 로고
    • IDH1(R132H) mutation increases murine haematopoietic progenitors and alters epigenetics
    • 4005896 1:CAS:528:DC%2BC38XhtFWmt7bL 22763442
    • Sasaki M, Knobbe CB, Munger JC, Lind EF, Brenner D, Brustle A et al (2012) IDH1(R132H) mutation increases murine haematopoietic progenitors and alters epigenetics. Nature 488:656-659
    • (2012) Nature , vol.488 , pp. 656-659
    • Sasaki, M.1    Knobbe, C.B.2    Munger, J.C.3    Lind, E.F.4    Brenner, D.5    Brustle, A.6
  • 17
    • 73649123907 scopus 로고    scopus 로고
    • Integrated genomic analysis identifies clinically relevant subtypes of glioblastoma characterized by abnormalities in PDGFRA, IDH1, EGFR, and NF1
    • 2818769 1:CAS:528:DC%2BC3cXkvFKgsL4%3D 20129251
    • Verhaak RG, Hoadley KA, Purdom E, Wang V, Qi Y, Wilkerson MD et al (2010) Integrated genomic analysis identifies clinically relevant subtypes of glioblastoma characterized by abnormalities in PDGFRA, IDH1, EGFR, and NF1. Cancer Cell 17:98-110
    • (2010) Cancer Cell , vol.17 , pp. 98-110
    • Verhaak, R.G.1    Hoadley, K.A.2    Purdom, E.3    Wang, V.4    Qi, Y.5    Wilkerson, M.D.6
  • 18
    • 76749138062 scopus 로고    scopus 로고
    • Application of T cell-based transcriptomics to identify three candidate biomarkers for monitoring anti-TGFbetaR therapy
    • 1:CAS:528:DC%2BC3cXhslOhurk%3D 20084050
    • Classen S, Muth C, Debey-Pascher S, Eggle D, Beyer M, Mallmann MR et al (2010) Application of T cell-based transcriptomics to identify three candidate biomarkers for monitoring anti-TGFbetaR therapy. Pharmacogenet Genomics 20:147-156
    • (2010) Pharmacogenet Genomics , vol.20 , pp. 147-156
    • Classen, S.1    Muth, C.2    Debey-Pascher, S.3    Eggle, D.4    Beyer, M.5    Mallmann, M.R.6
  • 19
    • 84856945806 scopus 로고    scopus 로고
    • TGF-beta: The sword, the wand, and the shield of FOXP3(+) regulatory T cells
    • 1:CAS:528:DC%2BC38XjtVGrt7o%3D 22158907
    • Tran DQ (2012) TGF-beta: the sword, the wand, and the shield of FOXP3(+) regulatory T cells. J Mol Cell Biol 4:29-37
    • (2012) J Mol Cell Biol , vol.4 , pp. 29-37
    • Tran, D.Q.1
  • 20
    • 84863987094 scopus 로고    scopus 로고
    • Blockade of cytotoxic T-lymphocyte antigen-4 by ipilimumab is associated with a profound long-lasting depletion of Foxp3+ regulatory T cells: A mechanistic explanation for ipilimumab-induced severe enterocolitis?
    • 1:STN:280:DC%2BC38znt12jsw%3D%3D 22069060
    • Nancey S, Boschetti G, Cotte E, Ruel K, Almeras T, Chauvenet M et al (2012) Blockade of cytotoxic T-lymphocyte antigen-4 by ipilimumab is associated with a profound long-lasting depletion of Foxp3+ regulatory T cells: a mechanistic explanation for ipilimumab-induced severe enterocolitis? Inflamm Bowel Dis 18:E1598-E1600
    • (2012) Inflamm Bowel Dis , vol.18 , pp. 1598-E1600
    • Nancey, S.1    Boschetti, G.2    Cotte, E.3    Ruel, K.4    Almeras, T.5    Chauvenet, M.6
  • 21
    • 84860358785 scopus 로고    scopus 로고
    • Soluble factors secreted by glioblastoma cell lines facilitate recruitment, survival, and expansion of regulatory T cells: Implications for immunotherapy
    • 1:CAS:528:DC%2BC38Xhtl2hsLfP
    • Crane CA, Ahn BJ, Han SJ, Parsa AT (2012) Soluble factors secreted by glioblastoma cell lines facilitate recruitment, survival, and expansion of regulatory T cells: implications for immunotherapy. Neurol Oncol 14:584-595
    • (2012) Neurol Oncol , vol.14 , pp. 584-595
    • Crane, C.A.1    Ahn, B.J.2    Han, S.J.3    Parsa, A.T.4
  • 22
    • 42549126264 scopus 로고    scopus 로고
    • The role of regulatory T cells in malignant glioma
    • Sonabend AM, Rolle CE, Lesniak MS (2008) The role of regulatory T cells in malignant glioma. Anticancer Res 28:1143-1150
    • (2008) Anticancer Res , vol.28 , pp. 1143-1150
    • Sonabend, A.M.1    Rolle, C.E.2    Lesniak, M.S.3
  • 23
    • 68949092126 scopus 로고    scopus 로고
    • Lactate promotes glioma migration by TGF-beta2-dependent regulation of matrix metalloproteinase-2
    • 1:CAS:528:DC%2BD1MXhtV2qurzO
    • Baumann F, Leukel P, Doerfelt A, Beier CP, Dettmer K, Oefner PJ et al (2009) Lactate promotes glioma migration by TGF-beta2-dependent regulation of matrix metalloproteinase-2. Neurol Oncol 11:368-380
    • (2009) Neurol Oncol , vol.11 , pp. 368-380
    • Baumann, F.1    Leukel, P.2    Doerfelt, A.3    Beier, C.P.4    Dettmer, K.5    Oefner, P.J.6
  • 24
    • 77953305545 scopus 로고    scopus 로고
    • Identification of potential serum biomarkers of glioblastoma: Serum osteopontin levels correlate with poor prognosis
    • 1:CAS:528:DC%2BC3cXntFCqtbY%3D 20530493
    • Sreekanthreddy P, Srinivasan H, Kumar DM, Nijaguna MB, Sridevi S, Vrinda M et al (2010) Identification of potential serum biomarkers of glioblastoma: serum osteopontin levels correlate with poor prognosis. Cancer Epidemiol Biomarkers Prev 19:1409-1422
    • (2010) Cancer Epidemiol Biomarkers Prev , vol.19 , pp. 1409-1422
    • Sreekanthreddy, P.1    Srinivasan, H.2    Kumar, D.M.3    Nijaguna, M.B.4    Sridevi, S.5    Vrinda, M.6
  • 25
    • 79956304247 scopus 로고    scopus 로고
    • Pro- and anti-inflammatory cytokines during immune stimulation: Modulation of iron status and red blood cell profile
    • 1:STN:280:DC%2BC3MvovFShsg%3D%3D
    • Koorts AM, Levay PF, Becker PJ, Viljoen M (2011) Pro- and anti-inflammatory cytokines during immune stimulation: modulation of iron status and red blood cell profile. Mediat Inflamm 2011:716301
    • (2011) Mediat Inflamm , vol.2011 , pp. 716301
    • Koorts, A.M.1    Levay, P.F.2    Becker, P.J.3    Viljoen, M.4
  • 26
    • 17844397949 scopus 로고    scopus 로고
    • The role of interleukin-8 and its receptors in gliomagenesis and tumoral angiogenesis
    • 1:CAS:528:DC%2BD2MXjvV2qsLg%3D
    • Brat DJ, Bellail AC, Van Meir EG (2005) The role of interleukin-8 and its receptors in gliomagenesis and tumoral angiogenesis. Neurol Oncol 7:122-133
    • (2005) Neurol Oncol , vol.7 , pp. 122-133
    • Brat, D.J.1    Bellail, A.C.2    Van Meir, E.G.3
  • 28
    • 33846821916 scopus 로고    scopus 로고
    • High TGFbeta-Smad activity confers poor prognosis in glioma patients and promotes cell proliferation depending on the methylation of the PDGF-B gene
    • 1:CAS:528:DC%2BD2sXitVartLk%3D 17292826
    • Bruna A, Darken RS, Rojo F, Ocana A, Penuelas S, Arias A et al (2007) High TGFbeta-Smad activity confers poor prognosis in glioma patients and promotes cell proliferation depending on the methylation of the PDGF-B gene. Cancer Cell 11:147-160
    • (2007) Cancer Cell , vol.11 , pp. 147-160
    • Bruna, A.1    Darken, R.S.2    Rojo, F.3    Ocana, A.4    Penuelas, S.5    Arias, A.6
  • 29
    • 80053502219 scopus 로고    scopus 로고
    • VEGFR2 expression and TGF-beta signaling in initial and recurrent high-grade human glioma
    • 1:CAS:528:DC%2BC3MXhtlKrtbvN 21985798
    • Kuczynski EA, Patten SG, Coomber BL (2011) VEGFR2 expression and TGF-beta signaling in initial and recurrent high-grade human glioma. Oncology 81:126-134
    • (2011) Oncology , vol.81 , pp. 126-134
    • Kuczynski, E.A.1    Patten, S.G.2    Coomber, B.L.3
  • 30
    • 0042425741 scopus 로고    scopus 로고
    • Characterization of gene expression profiles associated with glioma progression using oligonucleotide-based microarray analysis and real-time reverse transcription-polymerase chain reaction
    • 1868272 12937144
    • van den Boom J, Wolter M, Kuick R, Misek DE, Youkilis AS, Wechsler DS et al (2003) Characterization of gene expression profiles associated with glioma progression using oligonucleotide-based microarray analysis and real-time reverse transcription-polymerase chain reaction. Am J Pathol 163:1033-1043
    • (2003) Am J Pathol , vol.163 , pp. 1033-1043
    • Van Den Boom, J.1    Wolter, M.2    Kuick, R.3    Misek, D.E.4    Youkilis, A.S.5    Wechsler, D.S.6
  • 31
    • 84863325122 scopus 로고    scopus 로고
    • LY2109761 attenuates radiation-induced pulmonary murine fibrosis via reversal of TGF-beta and BMP-associated proinflammatory and proangiogenic signals
    • 1:CAS:528:DC%2BC38XpvVOjtLg%3D 22547771
    • Flechsig P, Dadrich M, Bickelhaupt S, Jenne J, Hauser K, Timke C et al (2012) LY2109761 attenuates radiation-induced pulmonary murine fibrosis via reversal of TGF-beta and BMP-associated proinflammatory and proangiogenic signals. Clin Cancer Res 18:3616-3627
    • (2012) Clin Cancer Res , vol.18 , pp. 3616-3627
    • Flechsig, P.1    Dadrich, M.2    Bickelhaupt, S.3    Jenne, J.4    Hauser, K.5    Timke, C.6
  • 32
    • 79958082880 scopus 로고    scopus 로고
    • Trimodal glioblastoma treatment consisting of concurrent radiotherapy, temozolomide, and the novel TGF-beta receptor i kinase inhibitor LY2109761
    • 1:CAS:528:DC%2BC3MXnsFalu7s%3D 21677877
    • Zhang M, Herion TW, Timke C, Han N, Hauser K, Weber KJ et al (2011) Trimodal glioblastoma treatment consisting of concurrent radiotherapy, temozolomide, and the novel TGF-beta receptor I kinase inhibitor LY2109761. Neoplasia 13:537-549
    • (2011) Neoplasia , vol.13 , pp. 537-549
    • Zhang, M.1    Herion, T.W.2    Timke, C.3    Han, N.4    Hauser, K.5    Weber, K.J.6


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.