Comprehensive Clinical Monograph: Perampanel (Fycompa®)

Part I: Introduction and Drug Profile

1.1 Overview and Therapeutic Class

Perampanel is a first-in-class antiepileptic drug (AED) that represents a novel therapeutic approach to the management of epilepsy.[1] Marketed by Eisai Co. under the brand name Fycompa®, it is distinguished by its unique mechanism of action as a selective, non-competitive antagonist of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-type glutamate receptor.[3] This positions it as a targeted therapy against the principal excitatory neurotransmitter pathway implicated in seizure generation and propagation.

Perampanel is primarily indicated for the treatment of epilepsy. Its initial approvals were for adjunctive therapy in patients with partial-onset seizures (POS), with or without secondary generalization, and for primary generalized tonic-clonic (PGTC) seizures.[4] Subsequently, its label has expanded to include monotherapy for POS in certain patient populations, broadening its clinical utility.[6]

1.2 Chemical and Physical Properties

From a chemical standpoint, perampanel is a complex small molecule belonging to the bipyridine class of compounds. Its structure is specifically defined as a 2,3'-bipyridin-6'-one substituted at the 1'-position with a phenyl group and at the 5'-position with a 2-cyanophenyl group. This unique configuration also classifies it as a pyridone and a nitrile.[5]

The molecular formula for perampanel is C23​H15​N3​O, and it has a molecular weight of 349.4 g/mol.[7] In its purified form, it exists as a crystalline solid. Its solubility characteristics show it is soluble in acetonitrile at concentrations greater than 1 mg/ml, while being only slightly soluble in common laboratory solvents like chloroform and dimethyl sulfoxide (DMSO).[8]

Table 1: Perampanel Drug Identifiers