Edaravone

Edaravone

Systematic (IUPAC) name
5-Methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one
Clinical data
Legal status	℞ (Prescription only)
Routes of administration	Oral
Identifiers
CAS Number	89-25-8 Y
ATC code	none
PubChem	CID: 4021
ChemSpider	3881 Y
UNII	S798V6YJRP Y
KEGG	D01552 Y
ChEBI	CHEBI:31530 Y
ChEMBL	CHEMBL290916 Y
Synonyms	MCI-186
Chemical data
Formula	C10H10N2O
Molecular mass	174.20 g/mol
SMILES O=C1N(/N=C(\C1)C)c2ccccc2
InChI InChI=1S/C10H10N2O/c1-8-7-10(13)12(11-8)9-5-3-2-4-6-9/h2-6H,7H2,1H3 Y Key:QELUYTUMUWHWMC-UHFFFAOYSA-N Y
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Edaravone (brand name Radicut) is a nootropic and neuroprotective agent used for the purpose of aiding neurological recovery following acute brain ischemia and subsequent cerebral infarction. It acts as a potent antioxidant and strongly scavenges free radicals, protecting against oxidative stress and neuronal apoptosis. It has been marketed solely in Japan by Mitsubishi Pharma since 2001. and marketed in India by Edinburgh Pharmaceuticals by the brand name Arone.

On June 26th, 2015, Mitsubishi Tanabe Pharma Corporation announced it has received approval to market Radicut for treatment of ALS in Japan. The phase III clinical trial began in 2011 in Japan. The company was awarded Orphan Drug Designation for Radicut by the FDA and EU in 2015. Radicut is an intravenous drug and administrated 14 days followed by 14 days drug holiday.

The biotech company Treeway is developing an oral formulation of edaravone (TW001) and is currently in clinical development. Treeway was awarded orphan drug designation for edaravone by the EMA in November 2014 and FDA in January 2015.

Edaravone has been shown to attenuate methamphetamine- and 6-OHDA-induced dopaminergic neurotoxicity in the striatum and substantia nigra, and does not affect methamphetamine-induced dopamine release or hyperthermia. It has also been demonstrated to protect against MPTP-mediated dopaminergic neurotoxicity to the substantia nigra, though notably not to the striatum.

External links

• http://www.alstdi.org/news/radicut-approved-for-als-in-japan/
• http://www.mt-pharma.co.jp/e/release/nr/2015/pdf/e_MTPC150626_2.pdf
• http://www.alstdi.org/als-research/clinical-trials/168/
• http://informahealthcare.com/doi/pdfplus/10.3109/21678421.2014.959024