Fosnetupitant chloride monohydrochloride (Pronetupitant chloride monohydrochloride) is an NK1 antagonist with pKi values of 9.5, 6.1 for human NK1 and NK3receptor, respectively. Fosnetupitant chloride monohydrochloride is a methylene phosphate prodrug of Netupitant[1].
in vivo
Fosnetupitant chloride monohydrochloride (i.v.) is converted in few minutes to Netupitant (HY-16346) invivo[1].
IC 50
hNK1: 9.5 (pKi); hNK3: 6.1 (pKi)
References
[1] Ruzza C, et al. In vitro and in vivo pharmacological characterization of Pronetupitant, a prodrug of the neurokinin 1 receptor antagonist Netupitant. Peptides. 2015 Jul;69:26-32. DOI:10.1016/j.peptides.2015.03.021
