Drug intelligence / Profile preview

5-HT3 antagonist + dexamethasone

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

Overview

A combination therapy consisting of a 5-hydroxytryptamine type 3 (5-HT3) receptor antagonist and dexamethasone is widely used for the prevention of nausea and vomiting, particularly in patients undergoing chemotherapy or surgery. The 5-HT3 antagonists (such as ondansetron, granisetron, tropisetron, palonosetron) block serotonin receptors in the central nervous system and gastrointestinal tract that are involved in triggering emesis. Dexamethasone is a synthetic glucocorticoid corticosteroid with anti-inflammatory and antiemetic properties; its precise mechanism for preventing nausea is not fully understood but may involve inhibition of prostaglandin synthesis or reduction of inflammation at the chemoreceptor trigger zone. The combination has demonstrated superior efficacy compared to either agent alone for both acute and delayed phases of chemotherapy-induced or postoperative nausea and vomiting[1][2][7]. This regimen is recommended by major oncology guidelines as standard prophylaxis for moderate to highly emetogenic chemotherapy regimens[4][7].

Other names
5-HT3 receptor antagonist plus dexamethasoneserotonin 5-HT3 antagonist and dexamethasone combinationserotonin5-HT3 antagonist and dexamethasone combinationserotonin-5-HT3 antagonist and dexamethasone combination
02

Targets

GR (Glucocorticoid receptor)HTR3A (5-hydroxytryptamine receptor 3A)

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