Perampanel

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Cat Number

API0232168

CAS Number

380917-97-5

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Product Detail Description Scientific Support Customer Q&A

CAS Number

380917-97-5

EINECS

691-969-4

Storage

Store at room temperature

Synonyms

Fycompa; E2007; ER-155055-90; perampanelum; 2-(2-oxo-1-phenyl-5-pyridin-2-ylpyridin-3-yl)benzonitrile

Molecular Formula

C23H15N3O

Molecular Weight

349.4

Smiles

C1=CC=C(C=C1)N2C=C(C=C(C2=O)C3=CC=CC=C3C#N)C4=CC=CC=N4

Appearance

White to yellowish white powder

Melting Point

71-75°C

Boiling Point

619.1±55.0°C at 760 mmHg (Predicted)

Relative Density

1.3±0.1

General Description

Perampanel is a first‑in‑class, selective, non‑competitive AMPA receptor antagonist. Its chemical structure is a pyridone derivative with a diphenyl ether group. The molecule is highly lipophilic and exists as a white powder with low solubility. Perampanel is a pure antagonist at the AMPA receptor, with no activity at kainate or NMDA receptors. It was the first antiepileptic drug targeting the glutamatergic system directly.

Mechanism of Action

Perampanel binds to a site on the AMPA receptor (GluA1‑4 subunits) distinct from the glutamate binding site, stabilizing the closed or desensitized state. This reduces the frequency of channel opening and decreases excitatory postsynaptic currents. By inhibiting glutamate‑mediated fast synaptic transmission, perampanel reduces neuronal hyperexcitability and seizure propagation. The effect is use‑dependent and does not involve changes in AMPA receptor expression.

Application

Perampanel is indicated as adjunctive therapy for partial‑onset seizures (with or without secondary generalization) and for primary generalized tonic‑clonic seizures in patients aged 12 years and older. It is also used for idiopathic generalized epilepsy.

This case series (11 patients with progressive myoclonic epilepsies) and systematic review (104 cases from literature) evaluated perampanel. Nine of 11 original patients improved in action myoclonus‑related disability (except two with Lafora disease). In the pooled analysis, more than half of patients improved in myoclonus and daily independence. Unverricht‑Lundborg disease responded best. Seizure reduction was achieved in almost all with active epilepsy. Only 11% dropped out due to inefficacy. Perampanel is beneficial and well‑tolerated for action myoclonus and seizures across different PMEs.

Fig. 1 Preferred Reporting Items for Systematic Reviews and Meta-analyses (PRISMA) diagram of the systematic revision of manuscripts. (Assenza G, et al., 2021)

References

Assenza G, et al. Perampanel Improves Cortical Myoclonus and Disability in Progressive Myoclonic Epilepsies: A Case Series and a Systematic Review of the Literature. Front Neurol. 2021;12:630366.

Does Perampanel require protection from light during long-term storage?

Yes, it is photosensitive. UV exposure can cause photodegradation of the pyridone ring. Store in light-resistant containers, preferably original opaque packaging.

What is the recommended storage temperature for Perampanel?

Store at controlled room temperature (15-25°C). Avoid excessive heat above 30°C, which can soften the material and accelerate oxidative degradation.

Is Perampanel stable under high-humidity conditions?

It is not hygroscopic and shows good stability. However, store in tightly sealed containers to prevent any potential surface effects.

How is the impurity perampanel N-oxide (an oxidative degradation product) monitored?

This degradation product is quantified using a stability-indicating HPLC method, ensuring it remains within ICH qualification thresholds.