Orvepitant (GW823296) is a drug developed by
GlaxoSmithKline which acts as a selective
antagonist for the
NK1receptor.[1] It was under development as a potential
antidepressant drug, and early stage human
clinical trials showed it to have some antidepressant effects, though not with sufficient efficacy to justify further development for this application. It was however considered a successful
proof of concept for NK1 antagonists as potential antidepressants, and efforts are continuing to find more potent compounds which might be more effective.[2]
References
^Di Fabio R, Alvaro G, Braggio S, Carletti R, Gerrard PA, Griffante C, et al. (November 2013). "Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate". Bioorganic & Medicinal Chemistry. 21 (21): 6264–73.
doi:
10.1016/j.bmc.2013.09.001.
PMID24075145.
^Ratti E, Bettica P, Alexander R, Archer G, Carpenter D, Evoniuk G, et al. (May 2013). "Full central neurokinin-1 receptor blockade is required for efficacy in depression: evidence from orvepitant clinical studies". Journal of Psychopharmacology. 27 (5): 424–34.
doi:
10.1177/0269881113480990.
PMID23539641.
S2CID6523822.