Nintedanib esylate

Nintedanib esylate is a small molecule tyrosine kinase inhibitor developed by Boehringer Ingelheim for the treatment of idiopathic pulmonary fibrosis (IPF) and a variety of cancers. It is marketed under the brand name Ofev.

Mechanism of Action

Nintedanib esylate works by inhibiting multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs), which are involved in the pathogenesis of several diseases. These include vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR), and platelet-derived growth factor receptor (PDGFR), among others. By blocking these pathways, nintedanib esylate can inhibit angiogenesis (the formation of new blood vessels) and fibroblast proliferation, two key processes in the progression of diseases such as IPF and cancer.

Clinical Use

Nintedanib esylate was first approved by the Food and Drug Administration (FDA) in 2014 for the treatment of IPF. It has since been approved for use in several other countries and for additional indications, including non-small cell lung cancer (NSCLC) and ovarian cancer. In clinical trials, nintedanib esylate has been shown to slow the decline in lung function in patients with IPF and to improve progression-free survival in patients with NSCLC and ovarian cancer.

Side Effects

Common side effects of nintedanib esylate include diarrhea, nausea, vomiting, abdominal pain, and liver enzyme elevations. Less common but more serious side effects can include bleeding, gastrointestinal perforation, and liver failure. Patients taking nintedanib esylate are typically monitored closely for these and other potential side effects.

See Also

• Tyrosine kinase inhibitor
• Idiopathic pulmonary fibrosis
• Non-small cell lung cancer
• Ovarian cancer