Drug intelligence / Profile preview

fosaprepitant dimeglumine + palonosetron hydrochloride + dexamethasone acetate

Development stage
Unknown
Lead developer
Zhuhai Beihai Biotech
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

Fosaprepitant dimeglumine + palonosetron hydrochloride + dexamethasone acetate is a triple-drug antiemetic combination regimen used for the prevention of chemotherapy-induced nausea and vomiting (CINV). The regimen consists of **fosaprepitant dimeglumine**, a prodrug of aprepitant that acts as a neurokinin-1 (NK-1) receptor antagonist; **palonosetron hydrochloride**, a second-generation serotonin (5-HT3) receptor antagonist; and **dexamethasone acetate**, a corticosteroid. This combination targets multiple emetic pathways, addressing both the acute and delayed phases of nausea and vomiting associated with highly or moderately emetogenic chemotherapy. It is currently being evaluated in Phase 2 clinical trials, specifically for patients with esophageal and lung cancer undergoing multi-cycle immunotherapy and chemotherapy, following guidelines from organizations like ASCO that recommend triple-agent prophylaxis for high-risk regimens.

Other names
fosaprepitant + palonosetron + dexamethasonefosaprepitant dimeglumine/palonosetron hydrochloride/dexamethasone acetate
02

Targets

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

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