Brexpiprazole Oral Soluble Film: A Randomized, Open-Label, Single-Dose, Crossover Bioequivalence Study in Healthy...

Brexpiprazole oral soluble film (OSF) is a novel dosage form under clinical development indicated for the treatment of schizophrenia in adults. This study aimed to investigate the bioequivalence, safety and tolerability of brexpiprazole OSF 2 mg compared with brexpiprazole orally disintegrating tablet (ODT) 2 mg (Rexulti®OD) in healthy Chinese adults.

A single-center, randomized, open-label, single-dose, crossover study was conducted, including a six-sequence three-period crossover intervention under fasting condition and a two-sequence two-period crossover intervention under postprandial condition. Pharmacokinetic sampling for brexpiprazole was carried out until 72 hours after dosing with a 28-day washout period. Participants were monitored for any adverse events throughout the study. The maximum plasma concentration (C_max) and the area under the plasma concentration-time curve (AUC) from time 0 to 72 hours (AUC_0-72h) were statistically analyzed using a linear mixed-effects model for bioequivalence evaluation.

In the fasting trial, 30 eligible individuals were enrolled and completed the study. Compared to brexpiprazole ODT 2 mg administered without water, the geometric mean ratios for C_max and AUC_0-72h of brexpiprazole OSF 2 mg taken without or with water were all close to 100%, and the corresponding 90% confidence intervals were within the established bioequivalence limit of 80.00-125.00%. In the postprandial trial, 26 participants were randomized and 2 participants withdrew from the study during the washout period. The bioequivalence range of C_max and AUC_0-72h for brexpiprazole OSF and ODT 2 mg administered without water were both within 80.00-125.00%. Generally, both formulations of brexpiprazole displayed comparable safety profiles, with no serious or unexpected adverse events reported during the study.

Brexpiprazole OSF 2 mg is bioequivalent to brexpiprazole ODT 2 mg with favorable safety, tolerability and acceptability under fasting and postprandial conditions. Due to its ease of administration, brexpiprazole OSF 2 mg may be expected to improve medication adherence, and provide a viable treatment option for patients with schizophrenia.