Drug intelligence / Profile preview

nintedanib + sildenafil

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

Overview

Nintedanib + sildenafil is a **combination therapy** investigated for the treatment of idiopathic pulmonary fibrosis (IPF) in patients with severely impaired gas exchange, particularly in those with right heart dysfunction. Nintedanib is a small molecule tyrosine kinase inhibitor that targets multiple growth factor receptors, reducing fibroblast activity and slowing disease progression. Sildenafil is a phosphodiesterase type 5 (PDE5) inhibitor, approved for pulmonary arterial hypertension, that increases cyclic guanosine monophosphate (cGMP), leading to pulmonary vasodilation and potentially reducing right ventricular strain. The combination has been studied in the INSTAGE clinical trial, but showed no significant benefit over nintedanib monotherapy on quality of life scores, dyspnea, or lung function, although there may be some effect on brain natriuretic peptide (BNP) stabilization, especially in patients with right heart dysfunction. There is no unique brand or code name associated with this combination as a single marketed product[1][2][3][4].

02

Targets

PDE6 (Phosphodiesterase 6)PDE5 (Phosphodiesterase 5A)PDGFRB (Platelet-derived growth factor receptor beta)VEGFR2 (Vascular endothelial growth factor receptor 2)FGFR1 (Fibroblast growth factor receptor 1)FLT3 (Fms related receptor tyrosine kinase 3)LCK (Proto-oncogene tyrosine-protein kinase Lck)

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