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US Approved Rx

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Primary Target

Vascular endothelial growth factor receptor 1

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Vascular endothelial growth factor receptor 2

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Vascular endothelial growth factor receptor 3

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Idiopathic pulmonary fibrosis

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Boehringer Ingelheim

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Nintedanib

G6HRD2P839

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Status:

US Approved Rx (2014)

First approved in 2014

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Vascular endothelial growth factor receptor 3

Vascular endothelial growth factor receptor 2

Vascular endothelial growth factor receptor 1

Conditions:

Idiopathic pulmonary fibrosis

Nintedanib is a receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. It is the only kinase inhibitor drug approved to treat idiopathic pulmonary fibrosis. that targets multiple receptor tyrosine kinases (RTK...

s) and non-receptor tyrosine kinases (nRTKs). Nintedanib inhibits the following RTKs: platelet-derived growth factor receptor (PDGFR) α and β, fibroblast growth factor receptor (FGFR) 1-3, vascular endothelial growth factor receptor (VEGFR) 1-3, and Fms-like tyrosine kinase-3 (FLT3). Among them, FGFR, PDGFR, and VEGFR have been implicated in IPF pathogenesis. Nintedanib binds competitively to the adenosine triphosphate (ATP) binding pocket of these receptors and blocks the intracellular signaling which is crucial for the proliferation, migration, and transformation of fibroblasts representing essential mechanisms of the IPF pathology.

Nintedanib Esylate

42F62RTZ4G

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Status:

US Approved Rx (2014)

First approved in 2014

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Vascular endothelial growth factor receptor 3

Vascular endothelial growth factor receptor 2

Vascular endothelial growth factor receptor 1

Conditions:

Idiopathic pulmonary fibrosis

Nintedanib is a receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. It is the only kinase inhibitor drug approved to treat idiopathic pulmonary fibrosis. that targets multiple receptor tyrosine kinases (RTK...

s) and non-receptor tyrosine kinases (nRTKs). Nintedanib inhibits the following RTKs: platelet-derived growth factor receptor (PDGFR) α and β, fibroblast growth factor receptor (FGFR) 1-3, vascular endothelial growth factor receptor (VEGFR) 1-3, and Fms-like tyrosine kinase-3 (FLT3). Among them, FGFR, PDGFR, and VEGFR have been implicated in IPF pathogenesis. Nintedanib binds competitively to the adenosine triphosphate (ATP) binding pocket of these receptors and blocks the intracellular signaling which is crucial for the proliferation, migration, and transformation of fibroblasts representing essential mechanisms of the IPF pathology.

NINTEDANIB ESYLATE HEMIHYDRATE

23O68KB9KV

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Status:

US Approved Rx (2014)

First approved in 2014

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Vascular endothelial growth factor receptor 3

Vascular endothelial growth factor receptor 2

Vascular endothelial growth factor receptor 1

Conditions:

Idiopathic pulmonary fibrosis

Nintedanib is a receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. It is the only kinase inhibitor drug approved to treat idiopathic pulmonary fibrosis. that targets multiple receptor tyrosine kinases (RTK...

s) and non-receptor tyrosine kinases (nRTKs). Nintedanib inhibits the following RTKs: platelet-derived growth factor receptor (PDGFR) α and β, fibroblast growth factor receptor (FGFR) 1-3, vascular endothelial growth factor receptor (VEGFR) 1-3, and Fms-like tyrosine kinase-3 (FLT3). Among them, FGFR, PDGFR, and VEGFR have been implicated in IPF pathogenesis. Nintedanib binds competitively to the adenosine triphosphate (ATP) binding pocket of these receptors and blocks the intracellular signaling which is crucial for the proliferation, migration, and transformation of fibroblasts representing essential mechanisms of the IPF pathology.

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