Drug intelligence / Profile preview

BIBF1000

Development stage
Preclinical
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

BIBF1000 is a **small molecule, orally active, triple tyrosine kinase inhibitor** that targets vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR), and fibroblast growth factor receptor (FGFR)[1][2][3][4]. It blocks signaling by these receptors, leading to inhibition of angiogenesis, fibrogenesis, and reduction of inflammatory and remodeling processes relevant to chronic airway diseases and fibrosis. BIBF1000 is mechanistically similar to nintedanib (BIBF1120), an approved drug for idiopathic pulmonary fibrosis, but BIBF1000 itself is a research compound primarily characterized in preclinical models for anti-remodeling, anti-inflammatory, and anti-fibrotic activities, particularly in asthma and pulmonary arterial hypertension models[1][2][4].

02

Targets

CDK1 (Cyclin-dependent kinase 1)FGFR1 (Fibroblast growth factor receptor 1)FLT3 (Fms related receptor tyrosine kinase 3)INSR (Insulin receptor)LCK (Proto-oncogene tyrosine-protein kinase Lck)LYN (LYN proto-oncogene, Src family tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)SRC (Proto-oncogene tyrosine-protein kinase Src)VEGFR2 (Vascular endothelial growth factor receptor 2)

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