A New Drug Antiemetic:Neurokinin I Receptor Antagonist Fosaprepitant / 中国药师

ABSTRACT

Neurokinin I receptor antagonist (NK1RA) fosaprepitant is a new antiemetic drug. Fosaprepitant dimeglumine was ap-proved by FDA in January 2008, while it is still in the approval stage in China. Fosaprepitant, as a prodrug of aprepitant, is rapidly converted to aprepitant after intravenous administration in vivo. The indication of fosaprepitant is the prevention of chemotherapy in-duced nausea and vomiting ( CINV) , especially the delayed CINV. Fosaprepitant as a unique intravenous preparation overcomes the drawbacks of aprepitant with oral administration only. Its bioavailability is not affected by the vomiting of patients. It is also suitable for patients with oral mucositis, who are unfavorable for oral medication. The action mechanisms, pharmacokinetics, and clinical trials of fosaprepitant were reviewed in the paper.