Aprepitant

General information

Aprepitant is a neurokinin-1 (NK ₁ ) receptor antagonist. Substance P, a regulatory peptide that is the preferred endogenous ligand at NK ₁ receptors, is found in the gastrointestinal tract (vagal afferents) and areas of the central nervous system thought to be involved in the vomiting reflex (including the nucleus tractus solitarius and area postrema). Aprepitant is a substrate and a weak inhibitor of P glycoprotein.

Aprepitant is the first NK ₁ receptor antagonist available for use as an antiemetic. It is a highly selective NK ₁ antagonist with a long half-life (9–12 hours) and is efficacious against opioid-induced emesis in animals.

Drug studies