Drug intelligence / Profile preview

dexamethasone + fosaprepitant + granisetron

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a three-drug antiemetic combination used primarily to prevent chemotherapy-induced nausea and vomiting (CINV). The combination has been studied in clinical trials for patients receiving highly emetogenic chemotherapy, particularly in breast cancer patients receiving anthracycline and cyclophosphamide (AC-based) regimens. The combination works through complementary mechanisms: dexamethasone (a corticosteroid), fosaprepitant (a neurokinin-1 receptor antagonist), and granisetron (a serotonin 5-HT3 receptor antagonist). Together, they target different pathways involved in chemotherapy-induced nausea and vomiting. Clinical studies have shown that this three-drug combination is effective in preventing both acute (0-24 hours) and delayed (24-120 hours) phases of CINV. In one randomized study comparing palonosetron versus granisetron (both combined with dexamethasone and fosaprepitant), the complete response rates were similar between the two 5-HT3 antagonists when used in this three-drug regimen[1]. The typical dosing regimen includes: - Fosaprepitant: 150 mg IV on day 1 - Granisetron: 1 mg IV on day 1 - Dexamethasone: 12 mg orally on day 1, followed by 8 mg orally on days 2 and 3 This combination represents the current standard of care for preventing CINV in patients receiving highly emetogenic chemotherapy, with efficacy demonstrated in multiple clinical trials.

02

Targets

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

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