Perampanel

Noncompetitive AMPA Glutamate Receptor Antagonist — NERVOUS SYSTEM

Key facts

Perampanel is an ofp drug in the Noncompetitive AMPA Glutamate Receptor Antagonist class catalogued in DrugCentral. It was first approved by the EMA in 2012. Its mechanism of action is classified as AMPA Receptor Antagonists, Cytochrome P450 2C8 Inhibitors and Cytochrome P450 3A4 Inhibitors. DrugCentral lists 1 molecular target, including GRIA1|GRIA2|GRIA3|GRIA4. Recorded indications include Idiopathic generalized epilepsy, Partial seizure and Secondarily generalized seizures.

• Approval status: ofp (first approved 2012 by the EMA).
• Drug class: Noncompetitive AMPA Glutamate Receptor Antagonist.
• Mechanism of action: AMPA Receptor Antagonists; Cytochrome P450 2C8 Inhibitors; Cytochrome P450 3A4 Inhibitors.
• Molecular targets: GRIA1|GRIA2|GRIA3|GRIA4 (1 listed in DrugCentral).
• Indications: Idiopathic generalized epilepsy, Partial seizure and Secondarily generalized seizures.
• ATC code: N03AX22 (Other antiepileptics).
• Molecular formula: C23H15N3O; molecular weight 349.39 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (3)

• Idiopathic generalized epilepsy
• Partial seizure
• Secondarily generalized seizures

Mechanism & targets

• Mechanism of action (MoA): AMPA Receptor Antagonists; Cytochrome P450 2C8 Inhibitors; Cytochrome P450 3A4 Inhibitors; UGT1A9 Inhibitors; UGT2B7 Inhibitors
• Established pharmacologic class: Noncompetitive AMPA Glutamate Receptor Antagonist

Molecular targets (1)

Target	Gene	Action	Activity
Glutamate receptor ionotropic AMPA	GRIA1|GRIA2|GRIA3|GRIA4	antagonist	IC50 6.61

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2020-01-23	PMDA	—	Eisai Co., Ltd.
2012-10-22	FDA	—	EISAI INC
2012-07-23	EMA	—	EISAI GMBH

ATC classification

ATC code	Therapeutic hierarchy
N03AX22	NERVOUS SYSTEM › ANTIEPILEPTICS › ANTIEPILEPTICS › Other antiepileptics

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Multiple-drug resistance	1247.1
Aggression	1200.8
Seizure	1102.5
Status epilepticus	813.5
Drug ineffective	566.9
Irritability	485.3
Somnolence	465.9
Epilepsy	352.8
Suicide attempt	295.4
Suicidal ideation	238.2
Off label use	235.0
Drug interaction	216.5

Chemical structure

• Molecular formula: C₂₃H₁₅N₃O
• Molecular weight: 349.39 g/mol
• CAS number: 380917-97-5
• InChIKey: PRMWGUBFXWROHD-UHFFFAOYSA-N
• PubChem CID: 9924495

O=C1N(C=C(C=C1C1=C(C=CC=C1)C#N)C1=CC=CC=N1)C1=CC=CC=C1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Perampanel used for?

DrugCentral lists the following indications for Perampanel: Idiopathic generalized epilepsy, Partial seizure and Secondarily generalized seizures.

How does Perampanel work?

Perampanel is classified as AMPA Receptor Antagonists, Cytochrome P450 2C8 Inhibitors and Cytochrome P450 3A4 Inhibitors; its molecular targets in DrugCentral include GRIA1|GRIA2|GRIA3|GRIA4 (antagonist).

When was Perampanel first approved?

Perampanel was first approved by the EMA in 2012.

What drug class does Perampanel belong to?

Perampanel is in the Noncompetitive AMPA Glutamate Receptor Antagonist class.

What is the chemical formula of Perampanel?

Perampanel has the molecular formula C23H15N3O and a molecular weight of 349.39 g/mol.

Sources

• DrugCentral drug card 4684 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1214124 — compound record and bioactivity
• PubChem CID 9924495 — chemical identifiers
• DrugBank DB08883 — drug record
• FDA UNII H821664NPK — substance identity
• DailyMed: FDA labels for Perampanel — current prescribing information (label search)
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

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