Dataset Information

Bioequivalence of perampanel fine granules and tablets in healthy Japanese subjects.

ABSTRACT:

Objective

Perampanel is an approved anti-seizure drug. A new formulation of perampanel fine granules (FG; 1% perampanel) has been developed for patients who are unable to take tablets. Bioequivalence between the 4-mg FG and tablet perampanel formulations, as well as their safety and tolerability, were assessed.

Materials and methods

In this phase I, single-center, open-label, 2-period, 2-sequence, crossover, bioequivalence study (NCT03399734), healthy Japanese subjects were randomized to receive single doses of the 4-mg FG perampanel and 4-mg perampanel tablet (separated by a ≥ 6-week washout period). Plasma samples for perampanel concentration analysis were collected pre-dose and at intervals up to 168 hours post-dose. The maximum observed concentration (C_max) and area under the concentration-time curve from time zero to 168 hours (AUC_(0-168h)) were used to assess the bioequivalence of the two formulations.

Results

The 90% confidence intervals (CIs) for the geometric mean ratio of test/reference for C_max and AUC_(0-168h) were within the bioequivalence criteria of 80 - 125% (C_max 90% CI 90.8%, 110%; AUC_(0-168h) 90% CI 98.2%, 112%; N = 21). 10/24 (41.7%) subjects with FG experienced ≥ 1 treatment-emergent adverse event (TEAE). The events were mild in severity and resolved within 4 hours of onset. There were no deaths, severe TEAEs, serious AEs, or TEAEs leading to study-drug withdrawal.

Conclusion

Bioequivalence of 4-mg FG and 4-mg tablet of perampanel was demonstrated. Both perampanel formulations were generally safe and well tolerated. These data suggest that perampanel FG may be a suitable alternative formulation for patients with epilepsy who have difficulties taking perampanel tablets.

SUBMITTER: Shiba S

PROVIDER: S-EPMC7659282 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature

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Publications

Bioequivalence of perampanel fine granules and tablets in healthy Japanese subjects.

Shiba Sari S Sekino Hisakuni H Ishiba Kaeko K Yasuda Sanae S Inoue Syuhei S Kotaka Ken K Reyderman Larisa L Uchida Naoki N

International journal of clinical pharmacology and therapeutics 20201201 12

<h4>Objective</h4>Perampanel is an approved anti-seizure drug. A new formulation of perampanel fine granules (FG; 1% perampanel) has been developed for patients who are unable to take tablets. Bioequivalence between the 4-mg FG and tablet perampanel formulations, as well as their safety and tolerability, were assessed.<h4>Materials and methods</h4>In this phase I, single-center, open-label, 2-period, 2-sequence, crossover, bioequivalence study (NCT03399734), healthy Japanese subjects were random ...[more]

PMID: 32870153

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Dataset Information

Bioequivalence of perampanel fine granules and tablets in healthy Japanese subjects.

Objective

Materials and methods

Results

Conclusion

Publications

Bioequivalence of perampanel fine granules and tablets in healthy Japanese subjects.

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