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rolapitant hydrochloride

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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.
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Synonym:rolapitant HCl
rolapitant hydrochloride monohydrate
rolapitant monohydrochloride monohydrate
US brand name:Varubi
Foreign brand name:Varuby
Code name:SCH-619734
SCH619734
Chemical structure:1,7-diazaspiro(4.5)decan-2-one, 8-(((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-, monohydrochloride, monohydrate, (5S,8S)-
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