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National Cancer Institute Thesaurus
| Preferred Name | Rolapitant Hydrochloride | |
| Synonyms |
Rolapitant Hydrochloride Rolapitant Monohydrochloride Monohydrate Rolapitant Hydrochloride Monohydrate Rolapitant HCl 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 SCH-619734 SCH619734 Varubi Varuby |
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| Definitions |
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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| ID |
http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C97955 |
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| CAS_Registry |
914462-92-3
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| Chemical_Formula |
C25H26F6N2O2.ClH.H2O
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| code |
C97955
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| Concept_In_Subset | ||
| Contributing_Source |
FDA
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| 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.
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| FDA_UNII_Code |
57O5S1QSAQ
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| FULL_SYN |
Rolapitant Hydrochloride Rolapitant Monohydrochloride Monohydrate Rolapitant Hydrochloride Monohydrate Rolapitant HCl 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 SCH-619734 SCH619734 Varubi Varuby
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| Has_Free_Acid_Or_Base_Form | ||
| label |
Rolapitant Hydrochloride
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| NCI_Drug_Dictionary_ID |
747816
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| PDQ_Closed_Trial_Search_ID |
747816
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| PDQ_Open_Trial_Search_ID |
747816
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| Preferred_Name |
Rolapitant Hydrochloride
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| prefixIRI |
Thesaurus:C97955
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| Semantic_Type |
Pharmacologic Substance
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| UMLS_CUI |
C3273721
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| subClassOf |
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