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
J Rodon, MA Carducci, JM Sepulveda-Sánchez… - Clinical Cancer …, 2015 - AACR
Purpose: TGFβ signaling plays a key role in tumor progression, including malignant glioma.
Small-molecule inhibitors such as LY2157299 monohydrate (LY2157299) block TGFβ …
Small-molecule inhibitors such as LY2157299 monohydrate (LY2157299) block TGFβ …
Pharmacokinetic, pharmacodynamic and biomarker evaluation of transforming growth factor-β receptor I kinase inhibitor, galunisertib, in phase 1 study in patients with …
J Rodón, M Carducci, JM Sepulveda-Sánchez… - Investigational new …, 2015 - Springer
Purpose Transforming growth factor-beta (TGF-β) signaling plays a key role in epithelial-
mesenchymal transition (EMT) of tumors, including malignant glioma. Small molecule …
mesenchymal transition (EMT) of tumors, including malignant glioma. Small molecule …
Phase 1 study of galunisertib, a TGF-beta receptor I kinase inhibitor, in Japanese patients with advanced solid tumors
Y Fujiwara, H Nokihara, Y Yamada… - Cancer chemotherapy …, 2015 - Springer
Purpose Inhibition of transforming growth factor-beta receptor I (TGF-beta RI)-mediated
signaling pathways blocks tumor growth and metastases in nonclinical studies. Galunisertib …
signaling pathways blocks tumor growth and metastases in nonclinical studies. Galunisertib …
Cardiac safety of TGF-β receptor I kinase inhibitor LY2157299 monohydrate in cancer patients in a first-in-human dose study
RJ Kovacs, G Maldonado, A Azaro… - Cardiovascular …, 2015 - Springer
Transforming growth factor-beta (TGF-β) signaling plays an important role in the fetal
development of cardiovascular organs and in the repair mechanisms of the heart. Hence …
development of cardiovascular organs and in the repair mechanisms of the heart. Hence …
Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway
S Herbertz, JS Sawyer, AJ Stauber… - Drug design …, 2015 - Taylor & Francis
Transforming growth factor-beta (TGF-β) signaling regulates a wide range of biological
processes. TGF-β plays an important role in tumorigenesis and contributes to the hallmarks …
processes. TGF-β plays an important role in tumorigenesis and contributes to the hallmarks …
SB-431542, a small molecule transforming growth factor-β-receptor antagonist, inhibits human glioma cell line proliferation and motility
MD Hjelmeland, AB Hjelmeland… - Molecular cancer …, 2004 - AACR
Transforming growth factor-β (TGF-β) is a multifunctional cytokine that promotes malignant
glioma invasion, angiogenesis, and immunosuppression. Antisense oligonucleotide …
glioma invasion, angiogenesis, and immunosuppression. Antisense oligonucleotide …
Blockade of TGF-β signaling by the TGFβR-I kinase inhibitor LY2109761 enhances radiation response and prolongs survival in glioblastoma
M Zhang, S Kleber, M Röhrich, C Timke, N Han… - Cancer research, 2011 - AACR
Glioblastoma multiforme (GBM) is a highly aggressive primary brain tumor that tends to be
resistant to the ionizing radiotherapy used to treat it. Because TGF-β is a modifier of radiation …
resistant to the ionizing radiotherapy used to treat it. Because TGF-β is a modifier of radiation …
Phase 1b/2a study of galunisertib, a small molecule inhibitor of transforming growth factor-beta receptor I, in combination with standard temozolomide-based …
A Wick, A Desjardins, C Suarez, P Forsyth… - Investigational new …, 2020 - Springer
Purpose Galunisertib, a TGF-β inhibitor, has demonstrated antitumor effects in preclinical
and radiographic responses in some patients with malignant glioma. This Phase 1b/2a trial …
and radiographic responses in some patients with malignant glioma. This Phase 1b/2a trial …
Defining a therapeutic window for the novel TGF‐β inhibitor LY 2157299 monohydrate based on a pharmacokinetic/pharmacodynamic model
I Gueorguieva, AL Cleverly, A Stauber… - British journal of …, 2014 - Wiley Online Library
Aims To identify prospectively a safe therapeutic window for administration of a novel oral
transforming growth factor β (TGF‐β) inhibitor, LY 2157299 monohydrate, based on a …
transforming growth factor β (TGF‐β) inhibitor, LY 2157299 monohydrate, based on a …
[HTML][HTML] Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor
JM Yingling, WT McMillen, L Yan, H Huang… - Oncotarget, 2018 - ncbi.nlm.nih.gov
Transforming growth factor-β (TGFβ) is an important driver of tumor growth via intrinsic and
extrinsic mechanisms, and is therefore an attractive target for developing cancer …
extrinsic mechanisms, and is therefore an attractive target for developing cancer …