Pre-clinical Studies

Adverse reactions not observed in clinical studies, but seen in animals at exposure levels similar to clinical exposure levels and with possible relevance to clinical use were as follows: In the fertility study in rats, prolonged and irregular estrous cycles were observed at the maximum tolerated dose (30 mg/kg) in females; however, these changes did not affect fertility and early embryonic development. There were no effects on male fertility.

The excretion into breast milk was measured in rats at 10 days post-partum. Levels peaked at one hour and were 3.65-times the levels in plasma.

In a pre- and postnatal development toxicity study in rats, abnormal delivery and nursing conditions were observed at maternally toxic doses, and the number of stillbirths was increased in offsprings. Behavioral and reproductive development of the offspring was not affected, but some parameters of physical development showed some delay, which is probably secondary to the pharmacology-based CNS effects of perampanel. The placental transfer was relatively low; 0.09% or less of administered dose was detected in the fetus.

Nonclinical data reveal that perampanel was not genotoxic and had no carcinogenic potential. The administration of maximum tolerated doses to rats and monkeys resulted in pharmacologically-based CNS clinical signs and decreased terminal body weight. There were no changes directly attributable to perampanel in clinical pathology or histopathology.