Drug intelligence / Profile preview

olanzapine + NK1 receptor antagonist + 5HT3 receptor antagonist + dexamethasone

Development stage
Unknown
Lead developer
Feixue Song
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This quadruple antiemetic regimen is a combination therapy consisting of the atypical antipsychotic olanzapine, a neurokinin-1 (NK1) receptor antagonist, a 5-hydroxytryptamine-3 (5-HT3) receptor antagonist, and the corticosteroid dexamethasone. It is specifically designed for the prevention of chemotherapy-induced nausea and vomiting (CINV) in patients receiving highly emetogenic chemotherapy (HEC), such as those with breast cancer. Olanzapine contributes to the antiemetic effect by blocking multiple receptors including dopamine D2 and serotonin 5-HT2C and 5-HT3. The NK1 receptor antagonist (e.g., aprepitant) inhibits substance P-mediated emesis, while the 5-HT3 receptor antagonist (e.g., palonosetron) blocks serotonin-induced emetic signals in the peripheral and central nervous systems. Dexamethasone acts as a synergistic adjunct, likely through anti-inflammatory mechanisms and modulation of the solitary tract nucleus. This specific combination is being evaluated in Phase 3 clinical trials led by Feixue Song, often as a pharmacological baseline to assess the adjunctive benefits of non-pharmacological interventions like electroacupuncture.

Other names
antiemetic therapy-Feixue Songolanzapine-containing quadruple antiemetic therapyolanzapine-containing four-drug antiemetic therapy
02

Targets

HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)HRH1 (Histamine H1 Receptor)mAChR (Muscarinic acetylcholine receptors)HTR3A (5-hydroxytryptamine receptor 3A)ADRA1A (α1A)TACR1 (Neurokinin‑1 Receptor)DRD2 (Dopamine D2 Receptor)GR (Glucocorticoid receptor)

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