Nintedanib

Nintedanib is a small molecule kinase inhibitor API that has transformed the treatment of idiopathic pulmonary fibrosis and other fibrotic diseases. As a potent inhibitor of multiple receptor tyrosine kinases, Nintedanib targets VEGFR, FGFR, and PDGFR pathways that are key drivers of fibrosis and angiogenesis. The distinctive oxindole scaffold of Nintedanib enables simultaneous inhibition of these pro-fibrotic and pro-angiogenic signaling pathways, providing a multi-targeted approach to disease modification. In pharmaceutical manufacturing, Nintedanib requires stringent quality control to ensure batch-to-batch consistency and therapeutic efficacy. The synthetic route to Nintedanib involves construction of the oxindole core followed by functionalization with the piperazine and aniline substituents. For generic manufacturers and research institutions, Nintedanib represents both a high-value therapeutic API and a compound of significant interest for fibrotic disease research. As the first targeted therapy for IPF with clinically demonstrated efficacy in reducing lung function decline, Nintedanib has established a new standard of care in pulmonary fibrosis.

Product Parameters

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Parameter	Specification
Product Name	Nintedanib
CAS Number	656247-17-5
Molecular Formula	C₃₁H₃₃N₅O₄
Molecular Weight	539.64
Melting Point	>237 °C (dec.)
Boiling Point	742.2 ± 60.0 °C (Predicted)
Density	1.284 ± 0.06 g/cm³ (Predicted)
pKa	11.06 ± 0.20 (Predicted)
Appearance	Light yellow to light green solid
Solubility	DMSO (Slightly), Methanol (Slightly)
Storage Condition	Refrigerator

Application

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Nintedanib is a small-molecule tyrosine kinase inhibitor (TKI) developed by Boehringer Ingelheim specifically for idiopathic pulmonary fibrosis (IPF) [1]. It is the first targeted therapy for IPF to demonstrate consistent clinical evidence of significantly reducing the annual decline in lung function (by up to 50%) and thereby slowing disease progression. The drug simultaneously blocks three key receptors: platelet-derived growth factor receptor (PDGFR), vascular endothelial growth factor receptors (VEGFR1–3), and fibroblast growth factor receptors (FGFR1–3).

 

Pharmacological Action

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Nintedanib targets the platelet-derived growth factor receptors (PDGFα and β), fibroblast growth factor receptors (FGFR1–3), and vascular endothelial growth factor receptors (VEGFR1–3; Chemicalbook). It competitively binds to the adenosine triphosphate (ATP) binding sites of these receptors, thereby blocking the signaling pathways involved in fibrosis progression and inhibiting fibroblast proliferation, migration, and transformation, ultimately slowing the disease progression of idiopathic pulmonary fibrosis (IPF).

 

Bioactivity

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Nintedanib (BIBF 1120, Intedanib, Vargatef, Ofev) is an effective triple vascular kinase inhibitor that targets VEGFR1/2/3, FGFR1/2/3, and PDGFRα/β. In cell-free assays, its IC50 values were 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM, and 59 nM/65 nM, respectively. Phase 3 clinical trial.

Contact Us

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Partner with Cosperpharm for Nintedanib—the quality and reliability your kinase inhibitor program deserves.