Products
Nintedanib was approved in many countries in 2015 in soft capsule form (Ofev).
Structure and properties
Nintedanib (C31H33N5O4, Mr = 539.6 g/mol) is present in the drug as nintedanibesilate, a light yellow powder.
Effects
Nintedanib (ATC L01XE31) has antiproliferative and antitumor properties. It inhibits intracellular signaling pathways responsible for fibroblast proliferation, migration, and transformation. The effects are based on the inhibition of various tyrosine kinases. These include PDGFR, FGFR, VEGFR and FLT3, Lck, Lyn and Src. The half-life ranges from 10 to 15 hours.
Indications
For the treatment of idiopathic pulmonary fibrosis (IPF) and to slow the progression of the disease. Nintedanib is also approved in some countries for the treatment of lung cancer (Vargatef).
Dosage
According to the SmPC. Capsules are taken twice daily, 12 hours apart, with food.
Contraindications
- Hypersensitivity
- Pregnancy
Full precautions can be found in the drug label.
Interactions
Nintedanib is a substrate of P-glycoprotein and of CYP3A4, and corresponding and other interactions are possible.
Adverse effects
The most common possible adverse effects include diarrhea, nausea, vomiting, abdominal pain, lack of appetite, weight loss, headache, and elevation of liver enzymes.