.Pharmacolibrary.Drugs.N_NervousSystem.N05A_Antipsychotics.N05AX16_Brexpiprazole.Brexpiprazole

Information

Brexpiprazole is a second-generation (atypical) antipsychotic medication used in the treatment of schizophrenia and as an adjunct in major depressive disorder. It acts as a partial agonist at serotonin 5-HT1A and dopamine D2 receptors, and as an antagonist at serotonin 5-HT2A receptors. It is approved for clinical use in multiple countries.

Pharmacokinetics

Pharmacokinetic parameters reported in healthy adult subjects after single-dose oral administration.

References

1. Higashi, K, et al., & Kawai, Y (2025). Population pharmacokinetics of brexpiprazole in Japanese healthy subjects and patients with schizophrenia. Drug metabolism and pharmacokinetics 62 101057–None. DOI:10.1016/j.dmpk.2025.101057 PUBMED:https://pubmed.ncbi.nlm.nih.gov/40157325

2. Bruno, CD, et al., & Greenblatt, DJ (2022). Impact of Obesity on Brexpiprazole Pharmacokinetics: Proposal for Improved Initiation of Treatment. Journal of clinical pharmacology 62(1) 55–65. DOI:10.1002/jcph.1947 PUBMED:https://pubmed.ncbi.nlm.nih.gov/34339048

3. Elmokadem, A, et al., & Greenblatt, DJ (2022). Brexpiprazole Pharmacokinetics in CYP2D6 Poor Metabolizers: Using Physiologically Based Pharmacokinetic Modeling to Optimize Time to Effective Concentrations. Journal of clinical pharmacology 62(1) 66–75. DOI:10.1002/jcph.1946 PUBMED:https://pubmed.ncbi.nlm.nih.gov/34328221

Revisions

• 06/2025 initial generated model