Population pharmacokinetics of vactosertib, a new TGF-β receptor type Ι inhibitor, in patients with advanced solid tumors

Jin CH(2014)Discovery of N-((4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent J Med Chem 57 4213-4238

Krishnaiah M(2012)Targeting the TGFβ signalling pathway in disease Nat Rev Drug Discov 11 790-227

Sreenu D(2001)TGF-β signaling in tumor suppression and cancer progression Nat Genet 29 117-588

Subrahmanyam VB(2010)TGF-β and immune cells: an important regulatory axis in the tumor microenvironment and progression Trends Immunol 31 220-1716

Rao KS(2016)TGF-beta type I receptor kinase inhibitor EW-7197 suppresses cholestatic liver fibrosis by inhibiting HIF1alpha-induced epithelial mesenchymal transition Cell Physiol Biochem 38 571-1739

Lee HJ(2014)EW-7197, a novel ALK-5 kinase inhibitor, potently inhibits breast to lung metastasis Mol Cancer Ther 13 1704-102

Park S-J(2013)Activin receptor-like kinase5 inhibition suppresses mouse melanoma by ubiquitin degradation of Smad4, thereby derepressing eomesodermin in cytotoxic T lymphocytes EMBO Mol Med 5 1720-635

Park H-J(2018)Association of TGF-β responsive signature with anti-tumor effect of vactosertib, a potent, oral TGF-β receptor type I (TGFBRI) inhibitor in patients with advanced solid tumors Journal of Clinical Oncology 36 3031-312

Lee K(2007)Pharmacometrics at FDA: evolution and impact on decisions Clin Pharmacol Ther 82 97-132

Sheen YY(2011)Impact of pharmacometric analyses on new drug approval and labelling decisions Clin Pharmacokinet 50 627-395

Jin CH(2014)Discovery of N-((4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent J Med Chem 57 4213-4238

Krishnaiah M(2012)Targeting the TGFβ signalling pathway in disease Nat Rev Drug Discov 11 790-227

Sreenu D(2001)TGF-β signaling in tumor suppression and cancer progression Nat Genet 29 117-588

Subrahmanyam VB(2010)TGF-β and immune cells: an important regulatory axis in the tumor microenvironment and progression Trends Immunol 31 220-1716

Rao KS(2016)TGF-beta type I receptor kinase inhibitor EW-7197 suppresses cholestatic liver fibrosis by inhibiting HIF1alpha-induced epithelial mesenchymal transition Cell Physiol Biochem 38 571-1739

Lee HJ(2014)EW-7197, a novel ALK-5 kinase inhibitor, potently inhibits breast to lung metastasis Mol Cancer Ther 13 1704-102

Park S-J(2013)Activin receptor-like kinase5 inhibition suppresses mouse melanoma by ubiquitin degradation of Smad4, thereby derepressing eomesodermin in cytotoxic T lymphocytes EMBO Mol Med 5 1720-635

Park H-J(2018)Association of TGF-β responsive signature with anti-tumor effect of vactosertib, a potent, oral TGF-β receptor type I (TGFBRI) inhibitor in patients with advanced solid tumors Journal of Clinical Oncology 36 3031-312

Lee K(2007)Pharmacometrics at FDA: evolution and impact on decisions Clin Pharmacol Ther 82 97-132

Sheen YY(2011)Impact of pharmacometric analyses on new drug approval and labelling decisions Clin Pharmacokinet 50 627-395