Drug intelligence / Profile preview

ondansetron + granisetron + palonosetron + dexamethasone + fosaprepitant + aprepitant

Development stage
Unknown
Lead developer
GSK
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous, Intramuscular, Transdermal, Subcutaneous
01

Overview

This is a combination regimen consisting of six active pharmaceutical ingredients—ondansetron, granisetron, palonosetron, dexamethasone, fosaprepitant, and aprepitant—used for the prevention and management of chemotherapy-induced nausea and vomiting (CINV) or postoperative nausea and vomiting (PONV). - Ondansetron, granisetron, and palonosetron are selective serotonin 5-HT3 receptor antagonists that block serotonin-mediated signaling in both the gastrointestinal tract and central nervous system to prevent emesis[1][5][8]. Palonosetron is a second-generation agent with higher binding affinity and longer half-life compared to ondansetron or granisetron[1][6]. - Dexamethasone is a synthetic glucocorticoid corticosteroid with anti-inflammatory properties; it also enhances antiemetic efficacy when combined with other agents. - Fosaprepitant (a prodrug of aprepitant) and aprepitant are neurokinin 1 (NK1) receptor antagonists that inhibit substance P–mediated emetic signaling in the brain. These agents are often used together for highly emetogenic chemotherapy regimens. This multi-drug combination targets multiple pathways involved in nausea/vomiting reflexes to provide broad-spectrum prophylaxis against acute as well as delayed CINV/PONV.

02

Targets

HTR3A (5-hydroxytryptamine receptor 3A)TACR1 (Neurokinin‑1 Receptor)GR (Glucocorticoid receptor)

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