Drug intelligence / Profile preview

5-HT3 receptor antagonist + olanzapine

Development stage
Unknown
Lead developer
Teva Pharmaceutical Industries
Modality
Small Molecules
Administration
Oral, Intravenous, Transdermal
01

Overview

This is a combination therapy consisting of a 5-hydroxytryptamine type 3 (5-HT3) receptor antagonist and olanzapine. The combination is primarily used for the prevention and management of chemotherapy-induced nausea and vomiting (CINV), especially in patients receiving highly or moderately emetogenic chemotherapy. The 5-HT3 receptor antagonist component blocks serotonin receptors in the central nervous system and gastrointestinal tract, reducing nausea and vomiting. Olanzapine, an atypical antipsychotic, acts as an antagonist at multiple neurotransmitter receptors including dopamine D1-D4, serotonin (including 5-HT2A/2C/3/6), histamine H1, alpha-1 adrenergic, and muscarinic acetylcholine receptors. This broad antagonism contributes to its antiemetic effects by modulating several pathways involved in emesis[1][4][5][6]. Clinical studies have shown that this combination significantly reduces both acute and delayed CINV compared to regimens without olanzapine[1][6][7].

02

Targets

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

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