Pharmacokinetics (PK) and pharmacodynamics (PD) of the oral transforming growth factor-beta (TGF-β) receptor I kinase inhibitor LY2157299 monohydrate (LY) in hepatocellular carcinoma (HCC) compared to glioma patients

被引：0

作者：

Raymond, Eric ^{[1
]}

Faivrel, Sandrine ^{[1
]}

Santoro, Armondo ^{[2
]}

Kelley, Robin K. ^{[3
]}

Merle, Philippe ^{[4
]}

Gane, Ed ^{[5
]}

Douillard, Jean-Yves ^{[6
]}

VValdschmidt, Dirk ^{[7
]}

Mulcahy, Mary ^{[8
]}

Costentin, Charlotte ^{[9
]}

Minguez, Beatriz ^{[10
]}

Di Lena, Luca ^{[11
]}

Gueorguieva, Ivelina ^{[12
]}

Miles, Colin ^{[12
]}

Cleverly, Ann ^{[12
]}

Lahn, Michael M. ^{[12
]}

Ameryckx, Sophie ^{[12
]}

Benhadji, Karim A. ^{[12
]}

Giannelli, Gianluigi ^{[11
]}

机构：

[1] Hop Beaujon, Clichy, France

[2] Humanitas Canc Ctr IRCCS, Milan, Italy

[3] Univ Calif San Francisco, San Francisco, CA 94143 USA

[4] Hop Croix Rousse, F-69317 Lyon, France

[5] Auckland City Hosp, Auckland, New Zealand

[6] Ctr Rene Gauducheau, St Herblain, France

[7] Univ Klinikum Koln, Cologne, Germany

[8] Northwestern Univ, Chicago, IL 60611 USA

[9] Hop Henri Mondor, F-94010 Creteil, France

[10] Vall dHebron, Liver Unit, Barcelona, Spain

[11] Univ Bari, Bari, Italy

[12] Eli Lilly & Co, Indianapolis, IN 46285 USA

来源：

MOLECULAR CANCER THERAPEUTICS | 2013年 / 12卷 / 11期

关键词：

D O I：

10.1158/1535-7163.TARG-13-C261

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

C261

引用

页数：2

共 38 条

[1] A phase 2 study of a novel transforming growth factor-beta (TGF-β1) receptor I kinase inhibitor, LY2157299 monohydrate (LY), in patients with advanced hepatocellular carcinoma (HCC)
Faivre, Sandrine J.
Santoro, Armando
Kelley, Robin Kate
Merle, Philippe
Gane, Ed
Douillard, Jean-Yves
Waldschmidt, Dirk
Mulcahy, Mary Frances
Costentin, Charlotte
Minguez, Beatriz
Papappicco, Pasqua
Gueorguieva, Ivelina
Cleverly, Ann
Desaiah, Durisala
Lahn, Michael M.
Ameryckx, Sophie
Benhadji, Karim A.
Raymond, Eric
Giannelli, Gianluigi
JOURNAL OF CLINICAL ONCOLOGY, 2014, 32 (03)
[2] Randomized dose comparison phase II study of the oral transforming growth factor-beta (TGF-β) receptor I kinase inhibitor LY2157299 monohydrate (LY) in patients with advanced hepatocellular carcinoma (HCC)
Faivre, Sandrine J.
Santoro, Armando
Kelley, Robin Katie
Merle, Philippe
Gane, Ed
Douillard, Jean-Yves
Waldschmidt, Dirk
Mulcahy, Mary Frances
Costentin, Charlotte
Minguez, Beatriz
Papappicco, Pasqua
Gueorguieva, Ivelina
Cleverly, Ann
Desaiah, Durisala
Lahn, Michael M. F.
Murray, Nicola
Benhadji, Karim A.
Raymond, Eric
Giannelli, Gianluigi
JOURNAL OF CLINICAL ONCOLOGY, 2013, 31 (15)
[3] Integrated data review of the first-in-human dose (FHD) study evaluating safety, pharmacokinetics (PK), and pharmacodynamics (PD) of the oral transforming growth factor-beta (TGF-β) receptor I kinase inhibitor, LY2157299 monohydrate (LY)
Rodon, Jordi
Anthony Carducci, Michael
Manuel Sepulveda, Juan
Azaro, Analia
Calvo, Emiliano
Seoane, Joan
Brana, Irene
Sicart, Elisabet
Gueorguieva, Ivelina
Cleverly, Ann
Pillay, Sada
Desaiah, Durisala
Lahn, Michael M. F.
Paz-Ares, Luis
Holdhoff, Matthias
O'Neill Blakeley, Jaishri
Baselga, Jose
JOURNAL OF CLINICAL ONCOLOGY, 2013, 31 (15)
[4] Phase Ib study evaluating safety and pharmacokinetics (PK) of the oral transforming growth factor-beta (TGF-β) receptor I kinase inhibitor LY2157299 monohydrate (LY) when combined with gemcitabine in patients with advanced cancer.
Kozloff, Mark
Carbonero, Rocio
Nadal, Tamara
Gueorguieva, Ivelina
Cleverly, Ann
Desaiah, Durisala
Lahn, Michael M. F.
Pillay, Sada
Blunt, Al
Tabernero, Josep
Macarulla, Teresa
JOURNAL OF CLINICAL ONCOLOGY, 2013, 31 (15)
[5] EVALUATION OF LY2157299 MONOHYDRATE (LY), A TGF-β RECEPTOR I KINASE INHIBITOR, IN PATIENTS WITH ADVANCED HEPATOCELLULAR CARCINOMA: PHASE 2 STUDY RESULTS OF SAFETY, EFFICACY AND PK/PD
Giannelli, G.
Faivre, S.
Santoro, A.
Kelley, R. K.
Merle, P.
Gane, E.
Douillard, J. -Y.
Waldschmidt, D.
Mulcahy, M.
Costentin, C.
Minguez, B.
Papappicco, P. P.
Gueorguieva, I.
Cleverly, A.
Desaiah, D.
Lahn, M. M.
Ameryckx, S.
Benhadji, K. A.
Raymond, E.
JOURNAL OF HEPATOLOGY, 2014, 60 (01) : S52 - S53
[6] Novel transforming growth factor beta receptor I kinase inhibitor galunisertib (LY2157299) in advanced hepatocellular carcinoma
Faivre, Sandrine
Santoro, Armando
Kelley, Robin K.
Gane, Ed
Costentin, Charlotte E.
Gueorguieva, Ivelina
Smith, Claire
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Raymond, Eric
Benhadji, Karim A.
Giannelli, Gianluigi
LIVER INTERNATIONAL, 2019, 39 (08) : 1468 - 1477
[7] The oral transforming growth factor-beta (TGF-β) receptor I kinase inhibitor LY2157299 plus lomustine in patients with treatment-refractory malignant glioma: The first human dose study.
Azaro, Analia
Baselga, Jose
Sepulveda, Juan Manuel
Seoane, Joan
Ahnert, Jordi Rodon
Brana, Irene
Gueorguieva, Ivelina
Cleverly, Ann
Lahn, Michael M. F.
Pillay, Sada
Paz-Ares, Luis
Holdhoff, Matthias
Blakeley, Jaishri O'Neill
Carducci, Michael Anthony
JOURNAL OF CLINICAL ONCOLOGY, 2012, 30 (15)
[8] A transforming growth factor kinase i inhibitor, galunisertib (ly2157299), modulates stemnessrelated biomarkers in hcc
Rani, B.
Dituri, F.
Malfettone, A.
Cao, Y.
Lupo, L.
Fabregat, I.
Giannelli, G.
EUROPEAN JOURNAL OF CLINICAL INVESTIGATION, 2016, 46 : 39 - 39
[9] PHASE 1B/2A STUDY EVALUATING SAFETY, PHARMACOKINETICS AND PHARMACODYNAMICS RESPONSES OF THE ORAL TRANSFORMING GROWTH FACTOR-BETA (TGF-β) RECEPTOR I KINASE INHIBITOR LY2157299 MONOHYDRATE COMBINED WITH CHEMORADIOTHERAPY IN NEWLY DIAGNOSED MALIGNANT GLIOMAS
Wick, Wolfgang
Suarez, Cristina
Rodon, Jordi
Desjardins, Annick
Forsyth, Peter
Gueorguieva, Ivelina
Cleverly, Ann
Burkholder, Tiana
Desaiah, Durisala
Lahn, Michael
NEURO-ONCOLOGY, 2013, 15 : 84 - 84
[10] TARGETING TGF-BETA I WITH THE TRANSFORMING GROWTH FACTOR RECEPTOR TYPE I KINASE INHIBITOR, LY2157299, MODULATES STEMNESS-RELATED BIOMARKERS IN HEPATOCELLULAR CARCINOMA
Rani, B.
Dituri, F.
Cao, Y.
Engstrom, U.
Lupo, L.
Dooley, S.
Moustakas, A.
Giannelli, G.
JOURNAL OF HEPATOLOGY, 2015, 62 : S429 - S429

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