Rolapitant (SCH619734) Hydrochloride is the hydrochloride salt form of rolapitant, an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy. Compared to other NK1-receptor antagonists, rolapitant has both a more rapid onset of action and a much longer half-life.

Fosnetupitant chloride monohydrochloride (Pro-netupitant chloride monohydrochloride) is a selective NK1 antagonist exhibiting high affinity for the human NK1 receptor with a pK i value of 9.5, and a lower affinity for the NK3 receptor with a pK i of 6.1. It serves as a methylene phosphate prodrug of Netupitant [1].

[D-Pro2] Spantide I TFA is an analog of Spantide I, a selective antagonist of the NK1 receptor [1].

Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a K i of 0.66 nM. Rolapitant hydrochloride (Rolapitant HCl) does not interact with CYP3A4. Rolapitant hydrochloride shows potent centrally-mediated anti-emetic activity in both acute and delayed ferret emesis models [1] [2].

Spantide acetate is a selective antagonist of NK1 receptor with Kis of 230 nM and 8150 nM for NK1 and NK2.