Drug intelligence / Profile preview

deupirfenidone + nintedanib

Development stage
Phase 1
Lead developer
PureTech
Modality
Small Molecules
Administration
Oral
01

Overview

**deupirfenidone + nintedanib** is a combination therapy of two antifibrotic small molecules targeting progressive fibrosing interstitial lung diseases. *Deupirfenidone* (LYT-100) is a next-generation, deuterated analog of pirfenidone developed by PureTech, designed for improved tolerability compared to pirfenidone, with a similar mechanism as an inhibitor of transforming growth factor-beta (TGF-β)-mediated collagen synthesis and anti-inflammatory effects[4]. *Nintedanib* is a triple tyrosine kinase inhibitor acting primarily on the fibroblast growth factor receptor (FGFR), platelet-derived growth factor receptor (PDGFR), and vascular endothelial growth factor receptor (VEGFR), and inhibits pathways responsible for fibroblast proliferation and migration. This combination seeks to leverage complementary mechanisms: anti-inflammatory and anti-fibrotic actions (deupirfenidone) and inhibition of pro-fibrotic growth factor signaling (nintedanib). The main indication for this combination is idiopathic pulmonary fibrosis (IPF), with ongoing evaluation for silicosis and other fibrosing lung diseases[1][2][3][4]. Data support safety and tolerability of co-administration of the parent compounds (pirfenidone/nintedanib) and suggest a potential for additive efficacy in slowing progression of fibrosing interstitial diseases[1][2][3].

Brand names
deupirfenidone + nintedanib
Other names
deupirfenidone + nintedanib
02

Targets

FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FLT3 (Fms related receptor tyrosine kinase 3)LCK (Proto-oncogene tyrosine-protein kinase Lck)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)TPP1 (Tripeptidyl peptidase 1)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)TGFB (GARP–latent transforming growth factor beta 1 complex)

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