Aprepitant/Fosaprepitant

Class: Neurokinin-1 Receptor Antagonists
VA Class: GA605
Chemical Name: 5-[[(2R,3S)-2-[(1R)-1-[3,5,bis (trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2,-dihydro-3H-1,2,4,-triazol-3-one
Molecular Formula: C₂₃H₂₁F₇N₄O₃C₂₃H₂₂F₇N₄O₆P•2C₇H₁₇NO₅
CAS Number: 170729-80-3
Brands: Emend

Medically reviewed by Drugs.com on Nov 25, 2021. Written by ASHP.

Introduction

Antiemetic; aprepitant is a selective, high-affinity antagonist at substance P/neurokinin-1 (NK₁) receptors; fosaprepitant dimeglumine is a lyophilized prodrug of aprepitant.

Uses for Aprepitant/Fosaprepitant

Cancer Chemotherapy-induced Nausea and Vomiting

Prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy, including high-dose cisplatin therapy. Used in combination with other antiemetic agents.

Prevention of nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy. Used in combination with other antiemetic agents.

For prevention of nausea and vomiting associated with highlyemetogenic chemotherapy regimens (including an anthracycline plus cyclophosphamide), ASCO recommends a 3-drug antiemetic regimen consisting of an NK₁ receptor antagonist (e.g., either oral aprepitant or IV fosaprepitant), a 5-HT₃ receptor antagonist (e.g., dolasetron, granisetron, ondansetron, palonosetron), and dexamethasone. ASCO states that fixed-combination netupitant and palonosetron plus dexamethasone is an additional treatment option.

For moderatelyemetogenic chemotherapy regimens, ASCO recommends a 2-drug antiemetic regimen preferably consisting of palonosetron and dexamethasone. If palonosetron is not available, a first-generation 5-HT₃ receptor antagonist (preferably granisetron or ondansetron) may be substituted. Limited evidence suggests that aprepitant may be added to this regimen; in such cases, use of any 5-HT₃ receptor antagonist is appropriate.

For chemotherapy regimens with a low emetogenic risk, ASCO recommends administration of a single dose of dexamethasone prior to chemotherapy.

For chemotherapy regimens with minimal emetogenic risk, ASCO states that routine antiemetic administration is not necessary.

Safety and efficacy for chronic use or for treatment of established nausea and vomiting not established.

Postoperative Nausea and Vomiting

Prevention of postoperative nausea and vomiting.

Safety and efficacy for chronic use or for treatment of established nausea and vomiting not established.

Aprepitant/Fosaprepitant Dosage and Administration

Administration

Dispensing and Administration Precautions

Because of similarities in spelling and/or pronunciation between Emend (the trade name for aprepitant) ...