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casopitant + ondansetron
- Development stage
- Unknown
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Casopitant + ondansetron is a combination of two antiemetic drugs used together, often as part of triple regimens with corticosteroids like dexamethasone, for the prevention of chemotherapy-induced nausea and vomiting (CINV). Casopitant is a selective, oral or intravenous neurokinin-1 (NK-1) receptor antagonist that inhibits substance P-mediated emetic signaling in the central nervous system. Ondansetron is a selective 5-hydroxytryptamine 3 (5-HT3) receptor antagonist that blocks serotonin-mediated emetic signaling from the gut and CNS. The combination acts synergistically to improve prophylaxis of acute and delayed emesis related to moderately or highly emetogenic chemotherapy.
- Brand names
- ZofranZuplenz
- Other names
- casopitant + ondansetron
02
Targets
TACR1 (Neurokinin‑1 Receptor)HTR3A (5-hydroxytryptamine receptor 3A)
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