Pharmacokinetics of Perampanel in Healthy Korean, White, and Japanese Adult Subjects.

Abstract

Perampanel is a highly selective, orally active, noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonist that has been approved in many countries as a treatment for partial-onset seizures and primary generalized tonic-clonic seizures. The pharmacokinetics (PK) of perampanel following multiple doses in healthy Korean, white, and Japanese male subjects were assessed in 3 studies. Noncompartmental PK parameters were derived from plasma concentration-time data. At steady state of perampanel 2-, 4-, and 6-mg oral multiple administration, perampanel was rapidly absorbed, as plasma perampanel concentration reached maximum concentration after 0.55-1 hour (median) after dosing in all 3 ethnic groups. The elimination was slow, with terminal elimination phase half-life values ranging from 63.9-129 hours (mean) for doses of 2-6 mg; there was no specific tendency suggesting a dose-related effect, and perampanel PK were linear in Korean subjects. There were no clinically relevant ethnic differences in PK following multiple doses of perampanel 2 and 4 mg between Korean, white, or Japanese subjects. Perampanel was well tolerated by all 3 ethnic groups. This outcome indicates that with respect to PK, the dosing regimens established in white and Japanese patients are applicable to Korean patients.

• Authors: Hiroko Tabuchi, Sari Shiba, Sanae Yasuda, Akihiro Ohnishi, Jae-Gook Shin
• Journal: Clinical pharmacology in drug development (Clin Pharmacol Drug Dev) Vol. 7 Issue 6 Pg. 613-620 (08 2018) ISSN: 2160-7648 [Electronic] United States
• PMID: 29870595 (Publication Type: Clinical Trial, Journal Article, Randomized Controlled Trial, Research Support, Non-U.S. Gov't)
• Copyright: © 2018, The American College of Clinical Pharmacology.

Chemical References

• Anticonvulsants
• Nitriles
• Pyridones
• perampanel

Topics

• Adult
• Anticonvulsants (administration & dosage, adverse effects, blood, pharmacokinetics)
• Area Under Curve
• Asian People
• Double-Blind Method
• Healthy Volunteers
• Humans
• Inactivation, Metabolic
• Male
• Middle Aged
• Nitriles
• Pyridones (administration & dosage, adverse effects, blood, pharmacokinetics)
• White People
• Young Adult