Safety evaluation of aprepitant for the prevention of chemotherapy-induced nausea and vomiting

Abstract

Introduction: Aprepitant is the only neurokinin (NK₁) receptor antagonist (RA) approved for prevention of chemotherapy-induced nausea and vomiting (CINV). Aprepitant is co-administered with a 5-HT₃ RA and a corticosteroid. Although aprepitant is safe, in most clinical settings potential drug–drug interactions need to be considered before prescription.

Areas covered: This article thoroughly reviews aprepitant and, in particular, clinically relevant safety aspects of the drug. The literature review was performed using Medline with the following search terms: adverse events, aprepitant, chemotherapy, CYP3A4, MK-0869, neurokinin₁ receptor antagonist, safety and tolerability.

Expert opinion: The recommended antiemetic regimen of aprepitant, a 5-HT₃ RA and a corticosteroid is safe. The combination of aprepitant, a 5-HT₃ RA and dexamethasone is now the gold standard of antiemetic treatment in prevention of CINV induced by HEC, or by the combination of an anthracycline and cyclophosphamide. The intravenous formulation of aprepitant used as a single dose is expected to be of benefit to cancer patients.

Keywords::

• adverse events
• aprepitant
• CYP3A4
• fosaprepitant
• MK-0869
• neurokinin₁ receptor antagonist
• safety
• tolerability