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Population pharmacokinetics and exposure-overall survival analysis of the transforming growth factor-β inhibitor galunisertib in patients with pancreatic cancer.

Gueorguieva I, Tabernero J, Melisi D, Macarulla T, Merz V, Waterhouse TH, Miles C, Lahn MM, Cleverly A, Benhadji KA.

Cancer Chemother Pharmacol. 2019 Nov;84(5):1003-1015. doi: 10.1007/s00280-019-03931-1. Epub 2019 Sep 3.


Phase 2 Study of the ALK5 Inhibitor Galunisertib in Very Low-, Low-, and Intermediate-Risk Myelodysplastic Syndromes.

Santini V, Valcárcel D, Platzbecker U, Komrokji RS, Cleverly A, Lahn MM, Janssen J, Zhao Y, Chiang A, Giagounidis A, Guba SC, Sridharan A, Gueorguieva I, Girvan A, da Silva Ferreira M, Bhagat TD, Pradhan K, Steidl U, Will B, Verma A.

Clin Cancer Res. 2019 Sep 3. pii: clincanres.1338.2019. doi: 10.1158/1078-0432.CCR-19-1338. [Epub ahead of print]


A Phase 2 Study of Galunisertib (TGF-β1 Receptor Type I Inhibitor) and Sorafenib in Patients With Advanced Hepatocellular Carcinoma.

Kelley RK, Gane E, Assenat E, Siebler J, Galle PR, Merle P, Hourmand IO, Cleverly A, Zhao Y, Gueorguieva I, Lahn M, Faivre S, Benhadji KA, Giannelli G.

Clin Transl Gastroenterol. 2019 Jul;10(7):e00056. doi: 10.14309/ctg.0000000000000056.


Novel transforming growth factor beta receptor I kinase inhibitor galunisertib (LY2157299) in advanced hepatocellular carcinoma.

Faivre S, Santoro A, Kelley RK, Gane E, Costentin CE, Gueorguieva I, Smith C, Cleverly A, Lahn MM, Raymond E, Benhadji KA, Giannelli G.

Liver Int. 2019 Aug;39(8):1468-1477. doi: 10.1111/liv.14113. Epub 2019 Jun 3.


TGFβ receptor inhibitor galunisertib is linked to inflammation- and remodeling-related proteins in patients with pancreatic cancer.

Melisi D, Garcia-Carbonero R, Macarulla T, Pezet D, Deplanque G, Fuchs M, Trojan J, Kozloff M, Simionato F, Cleverly A, Smith C, Wang S, Man M, Driscoll KE, Estrem ST, Lahn MMF, Benhadji KA, Tabernero J.

Cancer Chemother Pharmacol. 2019 May;83(5):975-991. doi: 10.1007/s00280-019-03807-4. Epub 2019 Mar 18.


Addressing current challenges and future directions in immuno-oncology: expert perspectives from the 2017 NIBIT Foundation Think Tank, Siena, Italy.

Maio M, Coukos G, Ferrone S, Fox BA, Fridman WH, Garcia PL, Lahn M, Provendier O, Russo V, Rüttinger D, Shalabi A, Trajanoski Z, Viallet J, Wolchok JD, Ibrahim R.

Cancer Immunol Immunother. 2019 Jan;68(1):1-9. doi: 10.1007/s00262-018-2285-y. Epub 2018 Dec 18.


Galunisertib plus gemcitabine vs. gemcitabine for first-line treatment of patients with unresectable pancreatic cancer.

Melisi D, Garcia-Carbonero R, Macarulla T, Pezet D, Deplanque G, Fuchs M, Trojan J, Oettle H, Kozloff M, Cleverly A, Smith C, Estrem ST, Gueorguieva I, Lahn MMF, Blunt A, Benhadji KA, Tabernero J.

Br J Cancer. 2018 Nov;119(10):1208-1214. doi: 10.1038/s41416-018-0246-z. Epub 2018 Oct 15.


A phase 1b study of transforming growth factor-beta receptor I inhibitor galunisertib in combination with sorafenib in Japanese patients with unresectable hepatocellular carcinoma.

Ikeda M, Morimoto M, Tajimi M, Inoue K, Benhadji KA, Lahn MMF, Sakai D.

Invest New Drugs. 2019 Feb;37(1):118-126. doi: 10.1007/s10637-018-0636-3. Epub 2018 Jul 11.


Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor.

Yingling JM, McMillen WT, Yan L, Huang H, Sawyer JS, Graff J, Clawson DK, Britt KS, Anderson BD, Beight DW, Desaiah D, Lahn MM, Benhadji KA, Lallena MJ, Holmgaard RB, Xu X, Zhang F, Manro JR, Iversen PW, Iyer CV, Brekken RA, Kalos MD, Driscoll KE.

Oncotarget. 2017 Dec 31;9(6):6659-6677. doi: 10.18632/oncotarget.23795. eCollection 2018 Jan 23.


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. 2017 May 6;18(5). pii: E995. doi: 10.3390/ijms18050995.


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. 2017 Jun;79(6):1169-1177. doi: 10.1007/s00280-017-3313-x. Epub 2017 Apr 27.


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. 2016 Dec 2;5:212303. eCollection 2016.


Combined inhibition of TGFβ and PDGF signaling attenuates radiation-induced pulmonary fibrosis.

Dadrich M, Nicolay NH, Flechsig P, Bickelhaupt S, Hoeltgen L, Roeder F, Hauser K, Tietz A, Jenne J, Lopez R, Roehrich M, Wirkner U, Lahn M, Huber PE.

Oncoimmunology. 2015 Dec 29;5(5):e1123366. doi: 10.1080/2162402X.2015.1123366. eCollection 2016 May.


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. 2016 Aug;18(8):1146-56. doi: 10.1093/neuonc/now009. Epub 2016 Feb 21.


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. 2015 Aug 10;9:4479-99. doi: 10.2147/DDDT.S86621. eCollection 2015. Review.


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. 2015 Jun;9(6):2442-2448. Epub 2015 Apr 8.


Glioblastoma treatment patterns, survival, and healthcare resource use in real-world clinical practice in the USA.

Girvan AC, Carter GC, Li L, Kaltenboeck A, Ivanova J, Koh M, Stevens J, Hayes-Larson E, Lahn MM.

Drugs Context. 2015 Mar 10;4. pii: 212274. doi: 10.7573/dic.212274. eCollection 2015.


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). 2015 Apr;38(2):131-44. doi: 10.1007/s13402-014-0210-8. Epub 2015 Jan 9.


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. 2015 Apr;33(2):357-70. doi: 10.1007/s10637-014-0192-4. Epub 2014 Dec 23.


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. 2015 Oct;15(4):309-23. doi: 10.1007/s12012-014-9297-4.


Evaluation of antitumor activity using change in tumor size of the survivin antisense oligonucleotide LY2181308 in combination with docetaxel for second-line treatment of patients with non-small-cell lung cancer: a randomized open-label phase II study.

Natale R, Blackhall F, Kowalski D, Ramlau R, Bepler G, Grossi F, Lerchenmüller C, Pinder-Schenck M, Mezger J, Danson S, Gadgeel SM, Summers Y, Callies S, André V, Das M, Lahn M, Talbot D.

J Thorac Oncol. 2014 Nov;9(11):1704-8. doi: 10.1097/JTO.0000000000000285.


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. 2015 Feb 1;21(3):553-60. doi: 10.1158/1078-0432.CCR-14-1380. Epub 2014 Nov 25.


A phase I dose-escalation study to a predefined dose of a transforming growth factor-β1 monoclonal antibody (TβM1) in patients with metastatic cancer.

Cohn A, Lahn MM, Williams KE, Cleverly AL, Pitou C, Kadam SK, Farmen MW, Desaiah D, Raju R, Conkling P, Richards D.

Int J Oncol. 2014 Dec;45(6):2221-31. doi: 10.3892/ijo.2014.2679. Epub 2014 Sep 26.


Why are we failing to implement imaging studies with radiolabelled new molecular entities in early oncology drug development?

Saleem A, Murphy P, Plisson C, Lahn M.

ScientificWorldJournal. 2014;2014:269605. doi: 10.1155/2014/269605. Epub 2014 Aug 18. Review.


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. 2014 May;77(5):796-807.


Mesenchymal stem cells are sensitive to treatment with kinase inhibitors and ionizing radiation.

Nicolay NH, Sommer E, Perez RL, Wirkner U, Bostel T, Ho AD, Lahn M, Debus J, Saffrich R, Huber PE.

Strahlenther Onkol. 2014 Oct;190(11):1037-45. doi: 10.1007/s00066-014-0686-1. Epub 2014 May 27.


Transforming growth factor-β as a therapeutic target in hepatocellular carcinoma.

Giannelli G, Villa E, Lahn M.

Cancer Res. 2014 Apr 1;74(7):1890-4. doi: 10.1158/0008-5472.CAN-14-0243. Epub 2014 Mar 17. Review.


A randomised phase 2 study combining LY2181308 sodium (survivin antisense oligonucleotide) with first-line docetaxel/prednisone in patients with castration-resistant prostate cancer.

Wiechno P, Somer BG, Mellado B, Chłosta PL, Cervera Grau JM, Castellano D, Reuter C, Stöckle M, Kamradt J, Pikiel J, Durán I, Wedel S, Callies S, André V, Hurt K, Brown J, Lahn M, Heinrich B.

Eur Urol. 2014 Mar;65(3):516-20. doi: 10.1016/j.eururo.2013.10.039. Epub 2013 Nov 6.


Safety and pharmacokinetics of the antisense oligonucleotide (ASO) LY2181308 as a single-agent or in combination with idarubicin and cytarabine in patients with refractory or relapsed acute myeloid leukemia (AML).

Erba HP, Sayar H, Juckett M, Lahn M, Andre V, Callies S, Schmidt S, Kadam S, Brandt JT, Van Bockstaele D, Andreeff M.

Invest New Drugs. 2013 Aug;31(4):1023-34. doi: 10.1007/s10637-013-9935-x. Epub 2013 Feb 10.


LY2109761 attenuates radiation-induced pulmonary murine fibrosis via reversal of TGF-β and BMP-associated proinflammatory and proangiogenic signals.

Flechsig P, Dadrich M, Bickelhaupt S, Jenne J, Hauser K, Timke C, Peschke P, Hahn EW, Gröne HJ, Yingling J, Lahn M, Wirkner U, Huber PE.

Clin Cancer Res. 2012 Jul 1;18(13):3616-27. doi: 10.1158/1078-0432.CCR-11-2855. Epub 2012 Apr 30.


Blockade of TGF-β signaling by the TGFβR-I kinase inhibitor LY2109761 enhances radiation response and prolongs survival in glioblastoma.

Zhang M, Kleber S, Röhrich M, Timke C, Han N, Tuettenberg J, Martin-Villalba A, Debus J, Peschke P, Wirkner U, Lahn M, Huber PE.

Cancer Res. 2011 Dec 1;71(23):7155-67. doi: 10.1158/0008-5472.CAN-11-1212. Epub 2011 Oct 17.


Molecular Imaging and Pharmacokinetic Analysis of Carbon-11 Labeled Antisense Oligonucleotide LY2181308 in Cancer Patients.

Saleem A, Matthews JC, Ranson M, Callies S, André V, Lahn M, Dickinson C, Prenant C, Brown G, McMahon A, Talbot DC, Jones T, Price PM.

Theranostics. 2011;1:290-301. Epub 2011 Jun 1.


Trimodal glioblastoma treatment consisting of concurrent radiotherapy, temozolomide, and the novel TGF-β receptor I kinase inhibitor LY2109761.

Zhang M, Herion TW, Timke C, Han N, Hauser K, Weber KJ, Peschke P, Wirkner U, Lahn M, Huber PE.

Neoplasia. 2011 Jun;13(6):537-49.


Dose study of the multikinase inhibitor, LY2457546, in patients with relapsed acute myeloid leukemia to assess safety, pharmacokinetics, and pharmacodynamics.

Wacheck V, Lahn M, Dickinson G, Füreder W, Meyer R, Herndlhofer S, Füreder T, Dorfner G, Pillay S, André V, Burkholder TP, Akunda JK, Flye-Blakemore L, Van Bockstaele D, Schlenk RF, Sperr WR, Valent P.

Cancer Manag Res. 2011;3:157-75. doi: 10.2147/CMR.S19341. Epub 2011 May 10.


Discovery of LY2457546: a multi-targeted anti-angiogenic kinase inhibitor with a novel spectrum of activity and exquisite potency in the acute myelogenous leukemia-Flt-3-internal tandem duplication mutant human tumor xenograft model.

Burkholder TP, Clayton JR, Rempala ME, Henry JR, Knobeloch JM, Mendel D, McLean JA, Hao Y, Barda DA, Considine EL, Uhlik MT, Chen Y, Ma L, Bloem LJ, Akunda JK, McCann DJ, Sanchez-Felix M, Clawson DK, Lahn MM, Starling JJ.

Invest New Drugs. 2012 Jun;30(3):936-49. doi: 10.1007/s10637-011-9640-6. Epub 2011 Mar 1. Erratum in: Invest New Drugs. 2012 Jun;30(3):1270-1.


Two-photon microscopy and fluorescence lifetime imaging reveal stimulus-induced intracellular Na+ and Cl- changes in cockroach salivary acinar cells.

Lahn M, Dosche C, Hille C.

Am J Physiol Cell Physiol. 2011 Jun;300(6):C1323-36. doi: 10.1152/ajpcell.00320.2010. Epub 2011 Feb 23.


Integrated analysis of preclinical data to support the design of the first in man study of LY2181308, a second generation antisense oligonucleotide.

Callies S, André V, Patel B, Waters D, Francis P, Burgess M, Lahn M.

Br J Clin Pharmacol. 2011 Mar;71(3):416-28. doi: 10.1111/j.1365-2125.2010.03836.x.


Window-of-opportunity trials to evaluate clinical activity of new molecular entities in oncology.

Glimelius B, Lahn M.

Ann Oncol. 2011 Aug;22(8):1717-25. doi: 10.1093/annonc/mdq622. Epub 2011 Jan 13. Review.


Reduced SMAD7 leads to overactivation of TGF-beta signaling in MDS that can be reversed by a specific inhibitor of TGF-beta receptor I kinase.

Zhou L, McMahon C, Bhagat T, Alencar C, Yu Y, Fazzari M, Sohal D, Heuck C, Gundabolu K, Ng C, Mo Y, Shen W, Wickrema A, Kong G, Friedman E, Sokol L, Mantzaris I, Pellagatti A, Boultwood J, Platanias LC, Steidl U, Yan L, Yingling JM, Lahn MM, List A, Bitzer M, Verma A.

Cancer Res. 2011 Feb 1;71(3):955-63. doi: 10.1158/0008-5472.CAN-10-2933. Epub 2010 Dec 28. Erratum in: Cancer Res. 2011 Apr 1;71(7):2806. Mantzaris, Giannis [corrected to Mantzaris, Ioannis].


Association of long-term administration of the survivin mRNA-targeted antisense oligonucleotide LY2181308 with reversible kidney injury in a patient with metastatic melanoma.

Herrington WG, Talbot DC, Lahn MM, Brandt JT, Callies S, Nagle R, Winearls CG, Roberts IS.

Am J Kidney Dis. 2011 Feb;57(2):300-3. doi: 10.1053/j.ajkd.2010.09.024. Epub 2010 Dec 21. Erratum in: Am J Kidney Dis. 2011 May;57(5):804.


TGF-β Receptor Inhibitors Target the CD44(high)/Id1(high) Glioma-Initiating Cell Population in Human Glioblastoma.

Anido J, Sáez-Borderías A, Gonzàlez-Juncà A, Rodón L, Folch G, Carmona MA, Prieto-Sánchez RM, Barba I, Martínez-Sáez E, Prudkin L, Cuartas I, Raventós C, Martínez-Ricarte F, Poca MA, García-Dorado D, Lahn MM, Yingling JM, Rodón J, Sahuquillo J, Baselga J, Seoane J.

Cancer Cell. 2010 Dec 14;18(6):655-68. doi: 10.1016/j.ccr.2010.10.023.


Inhibiting TGF-β signaling in hepatocellular carcinoma.

Giannelli G, Mazzocca A, Fransvea E, Lahn M, Antonaci S.

Biochim Biophys Acta. 2011 Apr;1815(2):214-23. doi: 10.1016/j.bbcan.2010.11.004. Epub 2010 Dec 1. Review.


Tumor survivin is downregulated by the antisense oligonucleotide LY2181308: a proof-of-concept, first-in-human dose study.

Talbot DC, Ranson M, Davies J, Lahn M, Callies S, André V, Kadam S, Burgess M, Slapak C, Olsen AL, McHugh PJ, de Bono JS, Matthews J, Saleem A, Price P.

Clin Cancer Res. 2010 Dec 15;16(24):6150-8. doi: 10.1158/1078-0432.CCR-10-1932. Epub 2010 Nov 1. Erratum in: Clin Cancer Res. 2011 Apr 15;17(8):2602.


Application of T cell-based transcriptomics to identify three candidate biomarkers for monitoring anti-TGFbetaR therapy.

Classen S, Muth C, Debey-Pascher S, Eggle D, Beyer M, Mallmann MR, Rudlowski C, Zander T, Pölcher M, Kuhn W, Lahn M, Schultze JL, Staratschek-Jox A.

Pharmacogenet Genomics. 2010 Mar;20(3):147-56. doi: 10.1097/FPC.0b013e328335731c.


A window of opportunity phase II study of enzastaurin in chemonaive patients with asymptomatic metastatic colorectal cancer.

Glimelius B, Lahn M, Gawande S, Cleverly A, Darstein C, Musib L, Liu Y, Spindler KL, Frödin JE, Berglund A, Byström P, Qvortrup C, Jakobsen A, Pfeiffer P.

Ann Oncol. 2010 May;21(5):1020-6. doi: 10.1093/annonc/mdp521. Epub 2009 Nov 9.


Analysis and variability of TGFbeta measurements in cancer patients with skeletal metastases.

O'Brien PJ, Ramanathan R, Yingling JM, Baselga J, Rothenberg ML, Carducci M, Daly T, Adcock D, Lahn M.

Biologics. 2008 Sep;2(3):563-9.


In Vivo Measurements of Tumor Metabolism and Growth after Administration of Enzastaurin Using Small Animal FDG Positron Emission Tomography.

Pollok KE, Lahn M, Enas N, McNulty A, Graff J, Cai S, Hartwell JR, Ernstberger A, Thornton D, Brail L, Hutchins G.

J Oncol. 2009;2009:596560. doi: 10.1155/2009/596560. Epub 2009 May 27.


Phase Ib safety and pharmacokinetic evaluation of daily and twice daily oral enzastaurin in combination with pemetrexed in advanced/metastatic cancer.

Hanauske AR, Lahn M, Musib LC, Weigang-Köhler K, Yilmaz E, Graefe T, Kuenen B, Thornton D, McNealy P, Giaccone G.

Ann Oncol. 2009 Sep;20(9):1565-75. doi: 10.1093/annonc/mdp049. Epub 2009 Jun 1.


Safety of multi-targeted kinase inhibitors as monotherapy treatment of cancer: a systematic review of the literature.

Crean S, Boyd DM, Sercus B, Lahn M.

Curr Drug Saf. 2009 May;4(2):143-54. Review.


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