Nintedanib
Nintedanib
|
|
| Clinical data | |
|---|---|
| Trade names | Vargatef, Ofev |
| AHFS/Drugs.com | Consumer Drug Information |
| Pregnancy category |
|
| Routes of administration |
Oral and intravenous |
| ATC code | |
| Legal status | |
| Legal status |
|
| Pharmacokinetic data | |
| Bioavailability | 4.7% |
| Protein binding | 97.8% |
| Metabolism | Esterases, glucuronidation |
| Biological half-life | 10–15 hrs |
| Excretion | 93% via faeces |
| Identifiers | |
|
|
| Synonyms | BIBF 1120 |
| CAS Number | |
| PubChem CID | |
| IUPHAR/BPS | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| ECHA InfoCard | 100.237.441 |
| Chemical and physical data | |
| Formula | C31H33N5O4 |
| Molar mass | 539.6248 g/mol |
| 3D model (Jmol) | |
|
|
|
|
  (what is this?)
|
|
Nintedanib, marketed under the brand names Ofev and Vargatef, is a medication used for the treatment of idiopathic pulmonary fibrosis (IPF) and along with other medications for some types of non-small-cell lung cancer.
Common side effects include abdominal pain, vomiting, and diarrhea. It is a small molecule tyrosine-kinase inhibitor, targeting vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR) and platelet derived growth factor receptor (PDGFR).
It was developed by Boehringer Ingelheim. At an assumed cost of 39,300 pounds per year it does not appear to be cost effective for IPF in the United Kingdom.
Nintedanib is used for the treatment of idiopathic pulmonary fibrosis (IPF). It has been shown to slow down decrease in forced vital capacity, and it also improves people's quality of life.
It is also used in combination with docetaxel as a second line treatment for adult patients with locally advanced, metastatic, or locally recurring NSCLC of adenocarcinoma histology. It is unclear how this combination compares to other second line agents as the comparisons have not been done as of 2014.
Nintedanib has not been tested in patients with moderate to severe impairment of liver function. Given that the drug is metabolised in the liver, it may not be safe in such patients.
Preclinical studies have shown that nintedanib binds in a highly selective manner to the ATP binding pocket of its three target receptor families, without binding to similarly shaped ATP domains in other proteins, which reduces the potential for undesirable side effects.
...
Wikipedia