Key Takeaways
- FDA greenlights BYSANTI™ (milsaperidone) as first-line therapy for bipolar I manic/mixed episodes and schizophrenia in adults.
- Ongoing Phase 3 study tests once-daily BYSANTI™ as adjunct for treatment-resistant depression, completion by end-2026.
- Bioequivalent to iloperidone with >100,000 patient-years data; aligns with established atypical antipsychotic profile.
- Protected by data exclusivity and patents to 2044; launch planned for Q3 2026
Edited and Written By: Pharmacally Medical News Desk
Assisted By: Nikita Jha, BPharm
Reviewed By: Pharmacally Editorial Team
Vanda Pharmaceuticals Inc. has secured U.S. Food and Drug Administration (FDA) approval for BYSANTI™ (milsaperidone) tablets, marking a fresh option for adults facing acute manic or mixed episodes in bipolar I disorder and schizophrenia.
As a new chemical entity (NCE) in the atypical antipsychotics class, BYSANTI™ builds directly on the proven foundation of Fanapt® (iloperidone). Clinical studies confirmed its bioequivalence to iloperidone across key doses, tapping into over 100,000 patient-years of real-world data for efficacy and safety.
This approval underscores accelerated drug development, as highlighted by Mihael H. Polymeropoulos, M.D., Vanda’s President, CEO, and Chairman. “BYSANTI™ marks a significant step forward, offering patients and providers a reliable new treatment grounded in extensive clinical heritage,” he stated. It arrives as Vanda’s second new drug in under two months, following NEREUS™ in December 2025.
Mechanism of Action
BYSANTI™ rapidly converts to iloperidone in the body, delivering dual active molecules. These antagonize dopamine D2, serotonin 5-HT2A, and alpha1-adrenergic receptors, modulating critical pathways in psychotic and mood disorders. What sets it apart is its strong alpha-adrenergic binding stronger than its dopamine or serotonin effects potentially suiting it for symptoms like hostility, agitation, and hyperarousal.
Clinical Evidence Summary
BYSANTI™ demonstrated bioequivalence to iloperidone in dedicated studies, where iloperidone and milsaperidone rapidly interconvert in vivo; efficacy for schizophrenia and bipolar I manic/mixed episodes is thus established from four well-controlled iloperidone trials (three short-/long-term schizophrenia studies and one bipolar study).
Safety Profile
Common adverse reactions for BYSANTI™ include dizziness, dry mouth, fatigue, nasal congestion, orthostatic hypotension, somnolence, tachycardia, weight increase, and increased hepatic enzymes.
BYSANTI™ is advancing in a Phase 3 trial as a once-daily adjunct for treatment-resistant major depressive disorder, with results expected by year-end 2026. This could expand its role in behavioral health.
Expect BYSANTI™ on the market in Q3 2026. Strong safeguards include regulatory data exclusivity and U.S. patents lasting until 2044, ensuring long-term availability.
Bipolar I disorder affects millions among the 10 million U.S. adults with bipolar conditions, where manic episodes demand rapid control. Schizophrenia impacts about 2.8 million Americans, leading to hospitalizations and reduced quality of life. BYSANTI™ offers a novel yet familiar tool for these challenges.
For full details, including the BOXED WARNING, check the Prescribing Information.
References
Vanda Pharmaceuticals Announces FDA Approval of BYSANTI™ (milsaperidone) for the treatment of Bipolar I Disorder and Schizophrenia – A New Chemical Entity Opening New Horizons in Psychiatric Innovation, 20 February 2026, Vanda Pharmaceuticals Announces FDA Approval of BYSANTI™ (milsaperidone) for the treatment of Bipolar I Disorder and Schizophrenia – A New Chemical Entity Opening New Horizons in Psychiatric Innovation
BYSANTI Prescribing Information, https://assets.vandapharma.com/Bysanti/Prescribing_Information.pdf