Brexpiprazole

Abstract

Brexpiprazole showed efficacy for the treatment of schizophrenia in the range of 2 to 4 mg/d and as an adjunct to antidepressant therapy in MDD when dosed at 2 to 3 mg/d. Advantages of this drug include once-daily dosing, good tolerability, and lack of effect on sexual function. Disadvantages include the lack of long-term safety data and potentially high cost.

Regulation of Reactive Oxygen Species-Mediated Damage in the Pathogenesis of Schizophrenia

“…Like aripiprazole, the drug acts as an antagonist of serotonin 5-HT2A receptors and a partial agonist for serotonin 5-HT1A and dopamine D2 receptors [ 236 , 237 , 238 , 239 , 240 ]. Phase 3 clinical trials indicate that 2–4 mg of brexpiprazole per day is effective short-term in reducing PANSS scores and alleviating symptoms of acute schizophrenia [ 221 , 241 , 242 ]. An analysis of twelve clinical trials demonstrated that brexpiprazole was superior to placebo in improving PANSS scores in patients with schizophrenia at doses of 1 mg, 2 mg, and 4 mg over six weeks [ 243 ].…”

“…An analysis of twelve clinical trials demonstrated that brexpiprazole was superior to placebo in improving PANSS scores in patients with schizophrenia at doses of 1 mg, 2 mg, and 4 mg over six weeks [ 243 ]. Brexpiprazole is well-tolerated and is administered daily [ 242 , 244 ].…”

Evidence for Therapeutic Drug Monitoring of Atypical Antipsychotics

“…Following its oral administration, brexpiprazole is extensively absorbed, with peak plasma concentrations occurring within 4 hours and the absolute oral bioavailability of the tablet formulation of 95% (Ishigooka et al, 2018). Brexpiprazole steady-state concentrations are attained within 10 to 12 days of dosing (Markovic et al, 2017;Mauri et al, 2017;Brexpiprazole, 2018). Brexpiprazole is highly protein-bound in plasma (more than 99%) (Brexpiprazole, 2018).…”

“…It should be noted that in vivo preclinical studies have shown that at clinically relevant plasma exposures of brexpiprazole, DM-3411 brain exposures were below the detection limit. Thus, DM-3411 is considered not to contribute to the therapeutic effects of brexpiprazole (Markovic et al, 2017;Brexpiprazole, 2018). After multiple once-daily administration of brexpiprazole, the terminal elimination half-life of brexpiprazole and DM-3411 is 91 and 85 hours, respectively (Markovic et al, 2017;Brexpiprazole, 2018).…”

“…Thus, DM-3411 is considered not to contribute to the therapeutic effects of brexpiprazole (Markovic et al, 2017;Brexpiprazole, 2018). After multiple once-daily administration of brexpiprazole, the terminal elimination half-life of brexpiprazole and DM-3411 is 91 and 85 hours, respectively (Markovic et al, 2017;Brexpiprazole, 2018). Population pharmacokinetic evaluation shows that CYP2D6 poor metabolisers have 47% higher exposure to brexpiprazole compared to extensive metabolisers (Ishigooka et al, 2018).…”