Products
For ALS treatment, edaravone was approved in Japan in 2015 (Radicut) and in the United States in 2017 as an infusion product (Radicava). In the EU, edaravone has orphan drug status. In many countries, the drug has been registered since 2019.
Structure and properties
Edaravone (C10H10N2O, Mr = 174.2 g/mol) is a substituted 2-pyrazolin-5-one. It exists as a white crystalline powder that is sparingly soluble in water.
Effects
Edaravone is a free radical scavenger with antioxidant and neuroprotective properties. It reduces oxidative stress and slows disease progression. The half-life is between 4.5 to 6 hours.
Indications
For the treatment of amyotrophic lateral sclerosis (ALS). In Japan, additionally for the treatment of acute ischemic stroke (approved 2001). This article refers to ALS.
Dosage
According to the SmPC. The drug is administered as an intravenous infusion.
Contraindications
- Hypersensitivity
- Pregnancy
Full precautions can be found in the drug label.
Interactions
Edaravone is sulfated and conjugated. It is a substrate of glucuronsyltransferases (UGT) and sulfotransferases. It does not interact with CYP450 isoenzymes.
Adverse effects
The most common potential adverse effects include bruising, gait disturbance, and headache.
