Drug intelligence / Profile preview

bifeprunox + olanzapine

Development stage
Unknown
Lead developer
Abbott
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Bifeprunox + olanzapine is a combination of two atypical antipsychotic drugs, each with distinct but complementary mechanisms of action. Bifeprunox acts as a partial agonist at dopamine D2 receptor and serotonin 5-HT1A receptor, functioning as a dopamine system stabilizer by increasing dopamine activity where it is low and decreasing it where it is high. This mechanism aims to treat both positive and negative symptoms of schizophrenia while minimizing side effects such as weight gain or hyperprolactinemia[1][3][5]. Olanzapine, on the other hand, primarily acts as an antagonist at multiple neuronal receptors including dopamine (D1–D4) and serotonin (5HT2A/2C/3/6) receptors, alpha-1 adrenergic receptor, histamine H1 receptor, and muscarinic receptors. It is approved for the treatment of schizophrenia and bipolar disorder in adults and adolescents[2][4][6]. The combination could theoretically provide broad-spectrum antipsychotic efficacy by targeting multiple neurotransmitter systems.

Other names
none
02

Targets

HTR2A (Serotonin receptor 5-HT2A)HTR3A (5-hydroxytryptamine receptor 3A)HRH1 (Histamine H1 Receptor)HTR6 (5-hydroxytryptamine receptor 6)HTR2C (5-hydroxytryptamine 2C receptor)ADRA1A (α1A)DRD2 (Dopamine D2 Receptor)M1 (Muscarinic acetylcholine receptor M1)DRD4 (Dopamine D4 Receptor)DRD3 (Dopamine receptor D3)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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