Mechanism of Action: Novel Mechanisms in CINV Treatment

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The role of the neurokinin-1 (NK-1) pathway in chemotherapy-induced nausea and vomiting (CINV) is now well established following approval of the US Food and Drug Administration (FDA) of aprepitant (Emend; Merck), the first NK-1 receptor antagonist (RA), for the treatment of CINV in 2003. The combination of aprepitant with a serotonin/5-hydroxytryptamine (5-HT3) RA plus dexamethasone resulted in significantly improved efficacy in patients receiving highly emetogenic chemotherapy (HEC). Although FDA approval of a new drug class marked a major breakthrough in combating CINV, aprepitant and its prodrug fosaprepitant, remain the only approved NK-1 agents to date. The need for new additions to this drug class, or new approaches to improve on current efficacy in CINV, remains substantial.


Last modified: July 11, 2023