Chemical Property of Nintedanib
Chemical Property:
- Vapor Pressure:0mmHg at 25°C
- Refractive Index:1.658
- Boiling Point:742.199°C at 760 mmHg
- PKA:11.06±0.20(Predicted)
- Flash Point:402.667°C
- PSA：94.22000
- Density:1.284g/cm3
- LogP:3.70270
- Storage Temp.:Refrigerator
- Solubility.:DMSO (Slightly), Methanol (Slightly)
- Purity/Quality:
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99%, *data from raw suppliers
Intedanib *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
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Description
Nintedanib is an oral administrated triple tyrosine kinase inhibitors developed by Boehringer Ingelheim, Germany. Its targets include platelet-derived growth factor (PDGF), vascular endothelial growth factor (VEGF) and basic fiber (BFGF), being able to also inhibit the activation of MAPK and Akt. At present, it is mainly used for cancer treatment, such as colorectal cancer, ovarian cancer and multiple myeloma. The study regarding to the respiratory diseases mainly focuses on the clinical treatment of advanced non-small cell lung cancer (NSCLC) and idiopathic pulmonary fibrosis (IPF). In June 2014, Boehringer Ingelheim has announced that the marketing authorization application of Nintedanib for the treatment of Idiopathic Pulmonary Fibrosis (IPF) had been confirmed by the European Medicines Agency (EMA) and been included in the accelerated approval list by the EMA.
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indications
Nintedanib ( Vargatef ) is an oral triple angiokinase inhibitor which simultaneously inhibits vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR) and fibroblast growth factor receptors (FGFR) signalling pathways. Growing scientific evidence shows that these three different angiokinase receptors play an important role not only in angiogenesis but also in tumour growth and metastasis.
Nintedanib is currently being investigated in patients with various solid tumours including Phase III studies in advanced NSCLC, colorectal cancer (refractory to standard treatment) and ovarian cancer, and also in Phase II studies in mesothelioma, kidney cancer (renal cell carcinoma) and liver cancer (hepatic cell carcinoma).
In the EU, nintedanib in the treatment of idiopathic pulmonary fibrosis (IPF) has recently received a positive CHMP opinion. The U.S. Food and Drug Administration (FDA) has approved nintedanib capsules under the brand name OFEV for oral use for the treatment of IPF.
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Uses
It is an indolinone derivative potently blocking VEGF-, PDGF-, and FGF-receptor kinases; an indolinone as triple angiokinase inhibitors. BIBF1120 (Vargatef) is a potent inhibitor of VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively. It is an indolinone derivative potently blocking VEGF-, PDGF-, and FGF-receptor kinases; an indolinone as triple angiokinase inhibitors. An antitumor agent.
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Clinical Use
Tyrosine kinase inhibitor:
Treatment of locally advanced, metastatic or locally
recurrent non-small cell lung cancer (NSCLC) of
adenocarcinoma tumour histology in combination
with docetaxel
Treatment of Idiopathic Pulmonary Fibrosis (IPF)
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Drug interactions
Potentially hazardous interactions with other drugs
Antibacterials: concentration reduced by rifampicin
- avoid.
Antifungals: concentration increased by
ketoconazole.
Antipsychotics: increased risk of agranulocytosis
with clozapine - avoid.
