Rolapitant Hydrochloride

**Semantic type:** Pharmacologic Substance

**Definition:** 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.

**Synonyms:** - 1,7-Diazaspiro(4.5)decan-2-one, 8-(((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-, Monohydrochloride, Monohydrate, (5S,8S)- - ROLAPITANT HYDROCHLORIDE - Rolapitant HCl - Rolapitant Hydrochloride Monohydrate - Rolapitant Monohydrochloride Monohydrate - SCH 619734 - SCH-619734 - SCH619734 - Varubi - Varuby