Otsuka Pharmaceutical's Rexulti orally disintegrating tablet is approved for marketing in Japan to treat schizophrenia

Otsuka recently announced that its antipsychotic drug Rexulti (brexpiprazole, epipiprazole) orally disintegrating (OD) tablets has been approved by Japanese regulatory authorities
.

In addition to the existing conventional tablets (Rexulti 1mg, 2mg), the launch of Rexulti OD (0.

brexpiprazole is a once-daily second-generation (atypical) oral antipsychotic drug, discovered by Otsuka and jointly developed by Lingbei and Otsuka
.

In the US market, brexpiprazole (brand name: Rexulti) was approved for the treatment of major depression (MDD) and schizophrenia in July 2015, and was approved for the maintenance treatment of adult patients with schizophrenia in 2016

Schizophrenia (schizophrenia) is a chronic and severe mental health disorder, often disabling; patients may experience cognitive, emotional, and behavioral changes, of which delusions and hallucinations are the most common symptoms
.

The course of schizophrenia is generally protracted, showing repeated attacks, aggravation, or deterioration.

The exact mechanism of action of brexpiprazole in the treatment of major depression (MDD) and schizophrenia is not yet clear.
The drug's efficacy may be through the partial agonist activity of 5-HT1A receptor and dopamine D2 receptor, serotonin 5-HT2A receptor The antagonist activity is jointly mediated
.

In addition, brexpiprazole not only shows high affinity for these receptors (subnanomolar), it also shows high affinity for norepinephrine α1B/2C receptors

The chemical structure of brexpiprazole (picture source: selleckchem.
com)

On August 18, Otsuka Pharmaceutical also announced the top-line results of the Phase 2 clinical trial (NCT04100096) of brexpiprazole for the treatment of borderline personality disorder (BPD)
.

This is a randomized, double-blind, placebo-controlled Phase 2 trial, which was launched in 2019 and was carried out jointly with Lundbeck

The results showed that the study did not meet the primary endpoint: at a predefined time point, there was no statistically significant separation between brexpiprazole and placebo in the change of the BPD Zanarini score scale from baseline
.

However, at other time points in the study, statistically greater numerical improvements than placebo were observed

In February 2019, two global phase 3 clinical studies of brexpiprazole in the treatment of patients with bipolar type I disorder (BP-I) related manic episodes also did not meet the primary endpoint
.

The main efficacy indicators of the two studies were the psychiatric symptoms and signs determined by the Youth Mania Rating Scale (YMRS)

Original source: Otsuka Obtains Approval in Japan for Orally-Disintegrating-Dose Form of REXULTI Tablets