Brilaroxazine is a new medication recently approved for treating certain mental health conditions. It represents progress in managing complex psychiatric disorders, noted for its unique pharmacological properties and potential to improve symptom control.
What Brilaroxazine Is and What It Treats
Brilaroxazine is classified as an atypical antipsychotic, a newer generation medication used to address various mental health conditions. It is characterized as a “dopamine and serotonin modulator” due to its interaction with brain chemicals.
Brilaroxazine is currently under development for several neuropsychiatric conditions. It has completed the first of two Phase III clinical trials for schizophrenia, with an expected New Drug Application (NDA) submission to the FDA by the fourth quarter of 2026. Reviva Pharmaceuticals, the developer, also intends to investigate brilaroxazine for conditions such as schizoaffective disorder, bipolar disorder, and major depressive disorder. It is also being explored for:
Attention deficit hyperactivity disorder (ADHD)
Irritability in autism
Tics
Psychosis or agitation linked to Alzheimer’s and Parkinson’s diseases
How Brilaroxazine Affects the Brain
Brilaroxazine works by interacting with various receptors in the brain, particularly those involved with dopamine and serotonin. It acts as a partial agonist at dopamine D2, D3, and D4 receptors, meaning it activates these receptors partially. This partial activation helps stabilize dopamine activity, which can be overactive in conditions like schizophrenia.
The medication also interacts with serotonin receptors, acting as a partial agonist at 5-HT1A receptors and an antagonist at 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6, and 5-HT7 receptors. Partial agonism at 5-HT1A receptors may help reduce symptoms of anxiety and depression. Its antagonistic action at 5-HT2A and 5-HT7 receptors contributes to its antipsychotic effects and potential cognitive improvements. By modulating both dopamine and serotonin systems, brilaroxazine rebalances neurotransmitter activity in the brain.
Taking Brilaroxazine and Managing Effects
Brilaroxazine is administered once daily by mouth. Clinical trials have investigated fixed doses of 15 mg, 30 mg, and 50 mg. For long-term treatment, a flexible dosing schedule of 15-50 mg daily has been explored for 52 weeks.
Common side effects observed in studies include headache, insomnia, sleep disturbance, and mild tremor. In initial studies, treatment-emergent adverse events (TEAEs) were reported by about 34.5% of patients at 15 mg and 35.5% at 50 mg doses. Nausea and dizziness were also reported, particularly in single-dose studies.
More serious, though less common, effects are monitored during treatment. While some older antipsychotics can cause significant weight gain or metabolic issues, brilaroxazine has shown mild weight gain (around 1.52 kg over one year), which was not dose-dependent. There were no clinically meaningful changes in movement disorder scales, such as those for akathisia (restlessness) or extrapyramidal symptoms, which are often concerns with older antipsychotics. Serious adverse events have been reported, but none were deemed related to brilaroxazine treatment in a one-year open-label extension study.
Brilaroxazine’s Role in Treatment
Brilaroxazine enters the mental health treatment landscape as an atypical antipsychotic with a unique pharmacological profile. Its multimodal action, modulating both dopamine and serotonin systems, may offer a broader spectrum of efficacy, potentially addressing both positive and negative symptoms of conditions like schizophrenia.
Clinical data suggest that brilaroxazine may have a favorable efficacy and a potentially improved side effect profile compared to existing second- and third-generation antipsychotics. Discontinuation rates in studies have been reported as lower for brilaroxazine compared to placebo and other antipsychotics. Its mild weight gain is a notable improvement over some other third-generation antipsychotics, which can have more significant weight gain as a side effect. This profile positions brilaroxazine as a potential alternative for individuals who have not responded well to other medications or have experienced intolerable side effects, offering a new option for managing complex neuropsychiatric disorders.