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Milsaperidone: First Approval
1Springer Nature, Mairangi Bay, Private Bag 65901, Auckland, 0754, New Zealand. cdi@adis.com.
Milsaperidone, an active metabolite of iloperidone, is a new atypical antipsychotic approved for schizophrenia and bipolar I disorder. Clinical trials confirmed its bioequivalence, paving the way for its US market entry.
Area of Science:
- Psychiatry and Pharmacology
- Neuroscience
- Drug Development
Background:
- Milsaperidone is an atypical antipsychotic developed for schizophrenia, bipolar I disorder, and major depressive disorder.
- It is the active metabolite of iloperidone, an existing atypical antipsychotic.
- Iloperidone is approved for schizophrenia (since 2009) and acute treatment of bipolar I disorder (since 2024).
Purpose of the Study:
- To summarize the development milestones of milsaperidone.
- To highlight its recent US approval for schizophrenia and bipolar I disorder.
Main Methods:
- Review of clinical trial data demonstrating pharmacokinetic bioequivalence between milsaperidone and iloperidone.
- Summary of regulatory milestones leading to US approval.
Main Results:
- Milsaperidone demonstrated pharmacokinetic bioequivalence to iloperidone.
- US approval granted on February 20, 2026, for schizophrenia and acute manic/mixed episodes of bipolar I disorder in adults.
Conclusions:
- Milsaperidone represents a significant advancement in the treatment of schizophrenia and bipolar I disorder.
- Further clinical evaluation is ongoing for major depressive disorder.
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