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Publikationer som ChEBI hänvisar till för LY-2157299. Visa hela publikationsregistret

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Publications in the selection

22 hits

Bibliografisk träff 2017-05-16

Disposition and metabolism of [<sup>14</sup>C]-galunisertib, a TGF-βRI kinase/ALK5 inhibitor, following oral administration in healthy subjects and mechanistic prediction of the effect of itraconazole on galunisertib pharmacokinetics.

Cassidy KC, Gueorguieva I, Miles C, Rehmel J, Yi P, Ehlhardt WJ.

Xenobiotica · clinical trial; journal article · DOI 10.1080/00498254.2017.1323137

Bibliografisk träff 2017-05-06

Biomarker and Histopathology Evaluation of Patients with Recurrent Glioblastoma Treated with Galunisertib, Lomustine, or the Combination of Galunisertib and Lomustine.

Capper D, von Deimling A, Brandes AA, Carpentier AF, Kesari S, Sepulveda-Sanchez JM, Wheeler HR, Chinot O, Cher L, Steinbach JP, Specenier P, Rodon J, Cleverly A, Smith C, Gueorguieva I, Miles C, Guba SC, Desaiah D, Estrem ST, Lahn MM, Wick W.

Int J Mol Sci · research-article; multicenter study; randomized controlled trial; journal article · DOI 10.3390/ijms18050995

Bibliografisk träff 2017-04-27

Phase 1b study of galunisertib in combination with gemcitabine in Japanese patients with metastatic or locally advanced pancreatic cancer.

Ikeda M, Takahashi H, Kondo S, Lahn MMF, Ogasawara K, Benhadji KA, Fujii H, Ueno H.

Cancer Chemother Pharmacol · multicenter study; clinical trial, phase i; journal article · DOI 10.1007/s00280-017-3313-x

Bibliografisk träff 2017-04-06

Efficacy of ALK5 inhibition in myelofibrosis.

Yue L, Bartenstein M, Zhao W, Ho WT, Han Y, Murdun C, Mailloux AW, Zhang L, Wang X, Budhathoki A, Pradhan K, Rapaport F, Wang H, Shao Z, Ren X, Steidl U, Levine RL, Zhao ZJ, Verma A, Epling-Burnette PK.

JCI Insight · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1172/jci.insight.90932

Bibliografisk träff 2017-02-23

NGS-based transcriptome profiling reveals biomarkers for companion diagnostics of the TGF-β receptor blocker galunisertib in HCC.

Cao Y, Agarwal R, Dituri F, Lupo L, Trerotoli P, Mancarella S, Winter P, Giannelli G.

Cell Death Dis · research support, non-u.s. gov't; research-article; journal article · DOI 10.1038/cddis.2017.44

Bibliografisk träff 2016-12-02

Relative bioavailability of three formulations of galunisertib administered as monotherapy in patients with advanced or metastatic cancer.

Gueorguieva I, Cleverly A, Desaiah D, Azaro A, Seoane J, Braña I, Sicart E, Miles C, Lahn MM, Mitchell MI, Rodon J.

Drugs Context · research-article; journal article · DOI 10.7573/dic.212303

Bibliografisk träff 2016-10-10

TGFβR1 Blockade with Galunisertib (LY2157299) Enhances Anti-Neuroblastoma Activity of the Anti-GD2 Antibody Dinutuximab (ch14.18) with Natural Killer Cells.

Tran HC, Wan Z, Sheard MA, Sun J, Jackson JR, Malvar J, Xu Y, Wang L, Sposto R, Kim ES, Asgharzadeh S, Seeger RC.

Clin Cancer Res · research-article; journal article · DOI 10.1158/1078-0432.ccr-16-1743

Bibliografisk träff 2016-08-01

Galunisertib (LY2157299), a transforming growth factor-β receptor I kinase inhibitor, attenuates acute pancreatitis in rats.

Liu X, Yu M, Chen Y, Zhang J.

Braz J Med Biol Res · research-article; evaluation study; journal article · DOI 10.1590/1414-431x20165388

Bibliografisk träff 2016-04-13

Autophagy Differentially Regulates Distinct Breast Cancer Stem-like Cells in Murine Models via EGFR/Stat3 and Tgfβ/Smad Signaling.

Yeo SK, Wen J, Chen S, Guan JL.

Cancer Res · research-article; journal article · DOI 10.1158/0008-5472.can-15-2946

Bibliografisk träff 2016-03-15

Galunisertib inhibits glioma vasculogenic mimicry formation induced by astrocytes.

Zhang C, Chen W, Zhang X, Huang B, Chen A, He Y, Wang J, Li X.

Sci Rep · research support, non-u.s. gov't; research-article; journal article · DOI 10.1038/srep23056

Bibliografisk träff 2016-02-21

A Phase II randomized study of galunisertib monotherapy or galunisertib plus lomustine compared with lomustine monotherapy in patients with recurrent glioblastoma.

Brandes AA, Carpentier AF, Kesari S, Sepulveda-Sanchez JM, Wheeler HR, Chinot O, Cher L, Steinbach JP, Capper D, Specenier P, Rodon J, Cleverly A, Smith C, Gueorguieva I, Miles C, Guba SC, Desaiah D, Lahn MM, Wick W.

Neuro Oncol · clinical trial, phase ii; research support, non-u.s. gov't; research-article; randomized controlled trial; journal article · DOI 10.1093/neuonc/now009

Bibliografisk träff 2015-11-03

Phase 1 study of galunisertib, a TGF-beta receptor I kinase inhibitor, in Japanese patients with advanced solid tumors.

Fujiwara Y, Nokihara H, Yamada Y, Yamamoto N, Sunami K, Utsumi H, Asou H, TakahashI O, Ogasawara K, Gueorguieva I, Tamura T.

Cancer Chemother Pharmacol · research support, non-u.s. gov't; clinical trial, phase i; journal article · DOI 10.1007/s00280-015-2895-4

Bibliografisk träff 2015-10-01

Cardiac Safety of TGF-β Receptor I Kinase Inhibitor LY2157299 Monohydrate in Cancer Patients in a First-in-Human Dose Study.

Kovacs RJ, Maldonado G, Azaro A, Fernández MS, Romero FL, Sepulveda-Sánchez JM, Corretti M, Carducci M, Dolan M, Gueorguieva I, Cleverly AL, Pillay NS, Baselga J, Lahn MM.

Cardiovasc Toxicol · research support, non-u.s. gov't; research-article; multicenter study; clinical trial, phase i; journal article · DOI 10.1007/s12012-014-9297-4

Bibliografisk träff 2015-08-10

Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway.

Herbertz S, Sawyer JS, Stauber AJ, Gueorguieva I, Driscoll KE, Estrem ST, Cleverly AL, Desaiah D, Guba SC, Benhadji KA, Slapak CA, Lahn MM.

Drug Des Devel Ther · video-audio media; review-article; review; journal article · DOI 10.2147/dddt.s86621

Bibliografisk träff 2015-08-01

Effects of TGF-beta signalling inhibition with galunisertib (LY2157299) in hepatocellular carcinoma models and in ex vivo whole tumor tissue samples from patients.

Serova M, Tijeras-Raballand A, Dos Santos C, Albuquerque M, Paradis V, Neuzillet C, Benhadji KA, Raymond E, Faivre S, de Gramont A.

Oncotarget · research support, non-u.s. gov't; research-article; journal article · DOI 10.18632/oncotarget.4308

Bibliografisk träff 2015-04-08

Brain perfusion and permeability in patients with advanced, refractory glioblastoma treated with lomustine and the transforming growth factor-β receptor I kinase inhibitor LY2157299 monohydrate.

Sepulveda-Sanchez J, Ramos A, Hilario A, DE Velasco G, Castellano D, Garcia DE LA Torre M, Rodon J, Lahn MF.

Oncol Lett · research-article; journal article · DOI 10.3892/ol.2015.3106

Bibliografisk träff 2015-01-09

Anti-tumor activity of the TGF-β receptor kinase inhibitor galunisertib (LY2157299 monohydrate) in patient-derived tumor xenografts.

Maier A, Peille AL, Vuaroqueaux V, Lahn M.

Cell Oncol (Dordr) · research-article; journal article · DOI 10.1007/s13402-014-0210-8

Bibliografisk träff 2014-12-23

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

Rodón J, Carducci M, Sepulveda-Sánchez JM, Azaro A, Calvo E, Seoane J, Braña I, Sicart E, Gueorguieva I, Cleverly A, Pillay NS, Desaiah D, Estrem ST, Paz-Ares L, Holdhoff M, Blakeley J, Lahn MM, Baselga J.

Invest New Drugs · research support, non-u.s. gov't; research-article; clinical trial, phase i; journal article · DOI 10.1007/s10637-014-0192-4

Bibliografisk träff 2014-11-25

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.

Rodon J, Carducci MA, Sepulveda-Sánchez JM, Azaro A, Calvo E, Seoane J, Braña I, Sicart E, Gueorguieva I, Cleverly AL, Pillay NS, Desaiah D, Estrem ST, Paz-Ares L, Holdhoff M, Blakeley J, Lahn MM, Baselga J.

Clin Cancer Res · research support, non-u.s. gov't; research-article; multicenter study; clinical trial, phase i; journal article · DOI 10.1158/1078-0432.ccr-14-1380

Bibliografisk träff 2014-05-01

Defining a therapeutic window for the novel TGF-β inhibitor LY2157299 monohydrate based on a pharmacokinetic/pharmacodynamic model.

Gueorguieva I, Cleverly AL, Stauber A, Sada Pillay N, Rodon JA, Miles CP, Yingling JM, Lahn MM.

Br J Clin Pharmacol · research-article; journal article · DOI 10.1111/bcp.12256

Bibliografisk träff 2013-06-27

Differential Inhibition of the TGF-β Signaling Pathway in HCC Cells Using the Small Molecule Inhibitor LY2157299 and the D10 Monoclonal Antibody against TGF-β Receptor Type II.

Dituri F, Mazzocca A, Mazzocca A, Fernando J, Peidrò FJ, Papappicco P, Fabregat I, De Santis F, Paradiso A, Sabbà C, Giannelli G.

PLoS One · research-article; journal article · DOI 10.1371/journal.pone.0067109

Bibliografisk träff 2007-11-26

Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-beta kinase antagonist, in mice.

Bueno L, de Alwis DP, Pitou C, Yingling J, Lahn M, Glatt S, Trocóniz IF.

Eur J Cancer · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejca.2007.10.008