Clinical Pharmacology
Pharmacodynamic Profile
Pharmacodynamics Video
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REXULTI® (brexpiprazole) targets 3 neurotransmitter systems
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The only atypical antipsychotic indicated as an adjunctive therapy to antidepressants for the treatment of MDD with high binding affinity to norepinephrine, serotonin, and dopamine receptors.1-4
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The only atypical antipsychotic indicated as an adjunctive therapy to antidepressants for the treatment of MDD with high binding affinity to norepinephrine, serotonin, and dopamine receptors.1-4
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Many antidepressants, such as SSRIs, are reuptake inhibitors and are thought to work by blocking the presynaptic reabsorption of serotonin. SNRIs and NDRIs function in similar ways for other neurotransmitter transports.
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REXULTI is thought to work differently by acting as an antagonist and partial agonist on norepinephrine, serotonin, and dopamine receptors.
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The mechanism of action of REXULTI is unknown. The activity of these compounds is based on in vitro data. The clinical significance of the in vitro data is unknown. Reuptake inhibitors modulate neurotransmitter activity through different processes than partial agonists and antagonists.5
The pharmacology data of REXULTI do not provide further insights on the mechanism of action.
The pharmacology data of REXULTI do not provide further insights on the mechanism of action.
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REXULTI has high binding affinity to 3 neurotransmitter systems: norepinephrine, serotonin, and dopamine6
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Pharmacodynamic profile—binding affinities across neurotransmitter systems7,a
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Pharmacodynamic profile—binding affinities across neurotransmitter systems7,a
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Norepinephrine, serotonin, and dopamine modulate each other’s activity8
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Norepinephrine, serotonin, and dopamine
modulate each other’s activity8
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While the mechanism of action of REXULTI is unknown, the efficacy of REXULTI may be mediated through a combination of partial agonist activity at serotonin 5-HT1A and dopamine D2 receptors, and antagonist activity at serotonin 5-HT2A receptors.
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aThe binding affinity of brexpiprazole was determined in vitro in cells overexpressing human receptors and is expressed as an nM concentration with lower values representing higher affinity. High binding affinity Ki <1 nM.7
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5-HT, serotonin; D, dopamine; H, histamine; Ki, binding affinity; M, muscarinic; MDD, major depressive disorder; nM, nanomolar; NDRI, norepinephrine and dopamine reuptake inhibitor; NE, norepinephrine; SNRI, serotonin and norepinephrine reuptake inhibitor; SSRI, selective serotonin reuptake inhibitor.
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Explore the pharmacodynamics of REXULTI with Dr. Jain
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Rakesh Jain, MD, MPH
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Clinical Professor
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Department of Psychiatry
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Texas Tech University School of Medicine
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Austin, Texas
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PHARMACOLOGY BROCHURE
Access a digital brochure detailing the binding profile for REXULTI,
including the pharmacodynamic profile.
including the pharmacodynamic profile.
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Continue exploring REXULTI
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Please see FULL PRESCRIBING INFORMATION,
including BOXED WARNING.
including BOXED WARNING.
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References: 1. Seroquel XR. Prescribing information. AstraZeneca Pharmaceuticals LP; 2022. 2. Abilify. Prescribing information. Otsuka Pharmaceutical Company; 2019. 3. Latuda. Prescribing information. Sunovision Pharmaceuticals Inc; 2022. 4. Vraylar. Prescribing information. Allergan Pharmaceuticals International Limited; 2024. 5. Ross EM, Kenakin TP. Pharmacodynamics: mechanisms of drug action and the relationship between drug concentration and effect. In: Hardman JG, Limbird LE, eds. Goodman & Gilman's The Pharmacological Basis of Therapeutics. 10th ed. New York, NY: McGraw-Hill; 2001:31-43. 6. Stahl SM. Stahl's Essential Psychopharmacology: Neuroscientific Basis and Practical Applications. 4th ed. Cambridge University Press; 2013. 7. Maeda K, Sugino H, Akazawa H, et al. Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator. J Pharmacol Exp Ther. 2014;350(3):589-604. 8. Mansari M, Guiard BP, Chernoloz O, Ghanbari R, Katz N, Blier P. Relevance of norepinephrine-dopamine interactions in the treatment of major depressive disorder. CNS Neurosci Ther. 2010;16(3):e1-17. doi:10.1111/j.1755-5949.2010.00146.x
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