Brexpiprazole

Products

Brexpiprazole was approved in the United States in 2015 and in the EU and many countries in 2018 in film-coated tablet form (Rexulti).

Structure and properties

Brexpiprazole (C₂₅H₂₇N₃O₂S, M_r = 433.6 g/mol) is structurally closely related to aripiprazole (Abilify, generics).

Effects

Brexpiprazole (ATC N05AX16) has antipsychotic properties. The effects are due to partial agonism at serotonin-5-HT_1A– and dopamine-D₂ receptors as well as antagonism at serotonin-5-HT_2A receptors. The half-life is long, approximately 90 hours.

Indications

For the treatment of schizophrenia in adult patients. Also used in some countries for the treatment of a depressive episode (major depression) in combination with antidepressants.

Dosage

According to the SmPC. Tablets are taken once daily, independent of meals. Treatment is started gradually.

Contraindications

• Hypersensitivity

For complete precautions, see the drug label.

Interactions

Brexpiprazole is a substrate of CYP3A4 and CYP2D6 and corresponding interactions with CYP inhibitors and inducers are possible.

Adverse effects

The most common potential adverse effects include weight gain and akathisia (motor agitation).