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National Cancer Institute Thesaurus
| Preferred Name | Rolapitant | |
| Synonyms |
1,7-diazaspiro(4.5)decan-2-one, 8-(((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-, (5S,8S)- ROLAPITANT Rolapitant |
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| Definitions |
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#C97952 |
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| CAS_Registry |
552292-08-7
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| Chemical_Formula |
C25H26F6N2O2
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| code |
C97952
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| Concept_In_Subset | ||
| Contributing_Source |
FDA HemOnc
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| DEFINITION |
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 |
NLE429IZUC
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| FULL_SYN |
1,7-diazaspiro(4.5)decan-2-one, 8-(((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-, (5S,8S)- ROLAPITANT Rolapitant
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|
| Has_Salt_Form | ||
| label |
Rolapitant
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|
| Preferred_Name |
Rolapitant
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| prefixIRI |
Thesaurus:C97952
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|
| Semantic_Type |
Pharmacologic Substance
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| UMLS_CUI |
C3273719
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| subClassOf |
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