Perampanel

Perampanel
Clinical data


Trade names	Fycompa
License data	EU EMA: Fycompa US FDA: Perampanel
Pregnancy category	US: C (Risk not ruled out)
ATC code	N03AX22 (WHO)
Legal status
Legal status	UK: POM (Prescription only) US: Schedule III
Pharmacokinetic data
Bioavailability	116%
Protein binding	95–96%
Metabolism	hepatic, mostly via CYP3A4 and/or CYP3A5
Biological half-life	105 hrs, 295 hrs (moderate hepatic impairment)
Excretion	70% faeces, 30% urine
Identifiers
IUPAC name 5'-(2-cyanophenyl)-1'-phenyl-2,3'-bipyridinyl-6'(1'H)-one
Synonyms	E2007
CAS Number	380917-97-5^Y
PubChem (CID)	9924495
IUPHAR/BPS	7050
ChemSpider	8100130^N
UNII	H821664NPK^N
KEGG	D08964^Y
ChEBI	CHEBI:71013^N
ChEMBL	CHEMBL1214124^N
PDB ligand ID	6ZP (PDBe, RCSB PDB)
ECHA InfoCard	100.219.846
Chemical and physical data
Formula	C₂₃H₁₅N₃O
Molar mass	349.384 g/mol
3D model (Jmol)	Interactive image
SMILES N#Cc2ccccc2-c1cc(-c4ncccc4)cn(c1=O)-c3ccccc3
InChI InChI=1S/C23H15N3O/c24-15-17-8-4-5-11-20(17)21-14-18(22-12-6-7-13-25-22) 16-26(23(21)27)19-9-2-1-3-10-19/h1-14,16H^N Key:PRMWGUBFXWROHD-UHFFFAOYSA-N^N
^NY (what is this?)

Perampanel (sold under the trade name Fycompa) is an antiepileptic drug developed by Eisai Co. that is used in addition to other drugs to treat partial seizures and generalized tonic-clonic seizures for people older than 12 years. It was first approved in 2012 and as of 2016 its optimal role in the treatment of epilepsy relative to other drugs was not clear. It was the first antiepileptic drug in the class of selective non-competitive antagonist of AMPA receptors.

The drug label has a black box warning that the drug cause may cause serious psychiatric and behavioral changes; it may cause homicidal or suicidal thoughts. Other side effects have included dizziness, somnolence, vertigo, aggression, anger, loss of coordination, blurred vision, irritability, and slurred speech. Permapanel reduced the effectiveness of levonorgestrel oral contraceptives by about 40%. Women who may get pregnant should not take it as studies in animals show it may harm a fetus. Perampanel is liable to be abused; very high doses produced euphoria responses similar to ketamine. It is designated as a Schedule III controlled substance by the Drug Enforcement Administration.

As of August 2016 perampanel had been studied and development discontinued in migraine, multiple sclerosis, neuropathic pain, and Parkinson's disease

Perampanel is used in addition to other drugs to treat partial seizures and generalized tonic-clonic seizures for people older than 12 years.

A 2016 review found it effective for both indications but due to the newness of the drug was unable to describe its optimal role in the treatment of epilepsy relative to other drugs. A 2014 review of the probability of added benefit of perampanel to the standard of care was unable to come to any conclusions, as no trial conducted by Eisai compared perampanel to a drug within the standard of care, but only to placebo.

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