3 de julio de 2016

Brexpiprazole, previously known as OPC-34712) is a novel atypical antipsychotic drug



Brexpiprazole, previously known as OPC-34712) is a novel atypical antipsychotic drug. It is a D2 dopamine partial agonist called serotonin-dopamine activity modulator (SDAM). The drug received FDA approval on July 13, 2015 for the treatment of schizophrenia, and as an adjunctive treatment for depression.Although it failed Phase II clinical trials for ADHD, it has been designed to provide improved efficacy and tolerability (e.g., less akathisia, restlessness and/or insomnia) over established adjunctive treatments for major depressive disorder (MDD).

The drug was developed by Otsuka and Lundbeck, and is considered to be a successor of Otsuka's top-selling antipsychotic agent aripiprazole (brand names: Abilify, Aripiprex). Otsuka's US patent on aripiprazole expired on October 20, 2014; however, due to a pediatric extension, a generic will become available in the near future.
Pharmacology

Brexpiprazole acts as a partial agonist of the 5-HT1A. D2, and D3 receptors. Partial agonists have both blocking properties and stimulating properties at the receptor they bind to. The ratio of blocking activity to stimulating activity determines a portion of its clinical effects. Brexpiprazole has more blocking and less stimulating activity than its predecessor, aripiprazole, which may decrease its risk for agitation and restlessness. It is also an antagonist of the 5-HT2A, 5-HT2B, 5-HT7, α1A-, α1B-, α1D-, and α2C-adrenergic, and H1 receptors.[22] It has negligible affinity for the mACh receptors.
Dosage

    As an adjunct to standard antidepressant therapy in adult patients with major depressive disorder:
        Phase II trials: 1.5 ± 0.5 mg.
        Phase III trials: 1 or 3 mg depending on group.
    For schizophrenic/schizoaffective subjects, dosage is 4 or 12 mg.
    For ADHD, the dose was thought to be 0.25 to 2 mg/day.

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