FDA Approves Milsaperidone as First-Line Treatment for Schizophrenia and Bipolar I Disorder

The U.S. Food and Drug Administration has approved milsaperidone (Bysanti) tablets as a first-line therapy for adults with schizophrenia and manic or mixed episodes of bipolar I disorder, as announced by Vanda Pharmaceuticals.

Milsaperidone is the active metabolite of iloperidone (Fanapt) and is classified as a new chemical entity within the atypical antipsychotic class. Clinical research demonstrated that milsaperidone is bioequivalent to iloperidone across all therapeutic doses, supporting its efficacy and dosing consistency.

BYSANTI™ is a new chemical entity (NCE) that belongs in the class of atypical antipsychotics. In clinical studies BYSANTI™ demonstrated bioequivalence to iloperidone across the therapeutic dosing spectrum enabling it to leverage well-established knowledge of efficacy and safety derived from a rich clinical development program and more than 100,000 patient-years of real-world experience with Fanapt® (iloperidone). As such BYSANTI™ represents a novel therapeutic option with a trusted safety profile in the treatment of these serious psychiatric conditions.

"The BYSANTI™ approval marks a significant step forward, offering patients and providers a reliable new treatment grounded in extensive clinical heritage," said Mihael H. Polymeropoulos, M.D., President, CEO and Chairman of the Board of Vanda Pharmaceuticals. "BYSANTI™ exemplifies a new era of accelerated innovation in drug development that can transform how we address unmet needs in behavioral health."

BYSANTI™ is currently being tested as a once-daily adjunctive treatment in treatment-resistant major depressive disorder in an ongoing clinical study expected to complete by the end of this year.

BYSANTI™ (milsaperidone), a new chemical entity, rapidly interconverts to iloperidone, providing dual active molecules that work in tandem by antagonizing dopamine D2, serotonin 5-HT2A, and alpha1-adrenergic receptors to modulate key pathways in these disorders. Its safety profile aligns closely with that established for iloperidone.

BYSANTI™'s unique in-class receptor binding profile, featuring strong alpha-adrenergic binding in excess of dopamine and serotonin receptor binding, makes it suitable for further investigation in conditions that include symptoms of hostility, agitation, and hyperarousal.

Vanda anticipates commercial availability of BYSANTI™ in Q3 of 2026. BYSANTI™ marketing exclusivity is expected to be protected by regulatory data exclusivity and issued US patents, with the latest expiring in 2044, providing a robust foundation for long-term innovation and patient benefit.

BYSANTI™ is the second new drug approval for Vanda in less than 2 months following the approval of NEREUS™ in December of 2025.

About Bipolar I Disorder and Schizophrenia

Bipolar I disorder impacts a significant portion of the roughly 10 million Americans with bipolar disorder, characterized by manic or mixed episodes that require effective symptom management to enhance outcomes.1 Schizophrenia affects approximately 1% of the U.S. adult population (about 2.8 million people), often causing substantial functional impairment, frequent hospitalizations, and diminished quality of life.