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olanzapine + neurokinin-1 receptor antagonist + serotonin 5-HT3 receptor antagonist
- Development stage
- Unknown
- Lead developer
- The Fifth Affiliated Hospital of Sun Yat-sen University
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
This investigational combination therapy consists of olanzapine, a neurokinin-1 (NK-1) receptor antagonist, and a serotonin 5-HT3 receptor antagonist. It is being evaluated by the Fifth Affiliated Hospital, Sun Yat-Sen University, as a dexamethasone-free antiemetic regimen for the prevention of chemotherapy-induced nausea and vomiting (CINV) in patients receiving highly emetogenic, cisplatin-based chemotherapy. Olanzapine is an atypical antipsychotic that acts as a multi-receptor antagonist, targeting dopamine, serotonin, histamine, and muscarinic receptors, which helps suppress both acute and delayed emesis. The NK-1 receptor antagonist (such as aprepitant or fosaprepitant) inhibits the binding of substance P to neurokinin receptors, while the 5-HT3 receptor antagonist (such as ondansetron) blocks serotonin-mediated signaling in the peripheral and central nervous systems. This triplet regimen aims to provide non-inferior efficacy to standard dexamethasone-containing protocols while avoiding corticosteroid-related side effects like hyperglycemia and insomnia.
- Other names
- olanzapine + NK-1 RA + 5-HT3 RAolanzapine-containing triplet antiemetic regimendexamethasone-free antiemetic protocol
02
Targets
DRD2 (Dopamine D2 Receptor)HRH1 (Histamine H1 Receptor)HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)HTR3A (5-hydroxytryptamine receptor 3A)HTR6 (5-hydroxytryptamine receptor 6)mAChR (Muscarinic acetylcholine receptors)TACR1 (Neurokinin‑1 Receptor)
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