Drug intelligence / Profile preview

aprepitant

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

Overview

Aprepitant is a selective, high-affinity antagonist of the human substance P/neurokinin 1 (NK1) receptor. It is an antiemetic medication used in combination with other agents to prevent both acute and delayed nausea and vomiting associated with highly emetogenic cancer chemotherapy, as well as to prevent postoperative nausea and vomiting. Aprepitant works by blocking the action of substance P at NK1 receptors in the brain, thereby inhibiting signals that trigger nausea and vomiting. It has little or no affinity for serotonin (5-HT3), dopamine, or corticosteroid receptors. The drug was developed by Merck & Co., first approved in 2003, and is available for oral or intravenous administration (the latter via its prodrug fosaprepitant)[2][4][7].

Brand names
EmendCinvantiAponvieAprecap
Other names
fosaprepitant
02

Targets

TACR1 (Neurokinin‑1 Receptor)

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