Background:

Fosaprepitant (L-758,298 MK-0517) is an antagonist of neurokinin-1[1].

Fosaprepitant has shown the pharmacodynamic function by its active metabolite aprepitant. Fosaprepitanot has been found to be a highly selective antagonist of the NK-1 receptor and inhibit the cation of substance P. In addition, Fosaprepitant has been exhibited to have the effect on cisplatin induced emesis in the classical ferret model. Besides, because of the brain penetrating of aprepitant, Fosaprepitant has been revealed to have a very high affinity for the NK-1 receptor and increase the efficacy by dexamethasone, granisetron and so on. Fosaprepitant has been evaluated to use in the prevention of chemotherapy-induced nausea and vomiting (CINV) by combination with a 5-HT3 antagonist and a steroid [1].

参考文献:
[1] Van Belle SJ1, Cocquyt V. Fosaprepitant dimeglumine (MK-0517 or L-785,298), an intravenous neurokinin-1 antagonist for the prevention of chemotherapy induced nausea and vomiting.Expert Opin Pharmacother. 2008 Dec; 9(18):3261-70.