Drug intelligence / Profile preview

olanzapine + aripiprazole

Development stage
Phase 4
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Olanzapine + aripiprazole is a combination of two atypical antipsychotic drugs used primarily in the management of schizophrenia, particularly in patients who have an inadequate response to monotherapy. Olanzapine acts mainly as an antagonist at dopamine D1, D2, D3, and D4 receptors and serotonin 5HT2A, 5HT2C, 5HT3, and 5HT6 receptors; it also blocks alpha-1 adrenergic receptors, histamine H1 receptor, and multiple muscarinic receptors[6]. Aripiprazole is a partial agonist at dopamine D2 and serotonin 5HT1A receptors and an antagonist at serotonin 5HT2A receptors. The combination has been shown to improve both positive and negative symptoms of schizophrenia as well as cognitive function compared to monotherapy[3][4][5]. It may also mitigate some metabolic side effects associated with olanzapine alone by reducing weight gain and improving lipid profiles[4]. Both drugs are small molecule pharmaceuticals developed for psychiatric indications.

Other names
olanzapine + aripiprazole
02

Targets

HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))HTR2C (5-hydroxytryptamine 2C receptor)HTR3A (5-hydroxytryptamine receptor 3A)HTR6 (5-hydroxytryptamine receptor 6)DRD1 (Dopamine D1 Receptor)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)DRD4 (Dopamine D4 Receptor)HRH1 (Histamine H1 Receptor)M1 (Muscarinic acetylcholine receptor M1)CHRM2 (M2)ADRA1A (α1A)HTR2A (Serotonin receptor 5-HT2A)

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