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casopitant + ondansetron + dexamethasone
- Development stage
- Phase 3
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
A combination of **casopitant** (an oral or intravenous neurokinin-1 receptor antagonist), **ondansetron** (a 5-HT3 receptor antagonist), and **dexamethasone** (a corticosteroid) is used as a three-drug antiemetic regimen for the prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV) in patients receiving moderately or highly emetogenic chemotherapy. - **Casopitant** antagonizes substance P at the neurokinin-1 receptor, blocking emetic signaling centrally. - **Ondansetron** blocks serotonin 5-HT3 receptors in the chemoreceptor trigger zone and gastrointestinal tract, inhibiting emetic signaling peripherally and centrally. - **Dexamethasone** exerts anti-inflammatory and antiemetic effects, though its precise antiemetic mechanism is not fully understood, and may involve inhibition of prostaglandin synthesis and interaction with neurotransmitter pathways. Clinical studies have shown that this triple therapy improves control of CINV compared to two-drug regimens. Dose adjustments for dexamethasone are recommended due to pharmacokinetic interactions (casopitant increases dexamethasone exposure)[1][2][3][4].
- Other names
- casopitant + ondansetron + dexamethasone
02
Targets
HTR3A (5-hydroxytryptamine receptor 3A)GR (Glucocorticoid receptor)TACR1 (Neurokinin‑1 Receptor)
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