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Physician Data Query
| Preferred Name | rolapitant hydrochloride | |
| Synonyms |
Varubi SCH619734 rolapitant monohydrochloride monohydrate 1,7-diazaspiro(4.5)decan-2-one, 8-(((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-, monohydrochloride, monohydrate, (5S,8S)- SCH-619734 rolapitant hydrochloride monohydrate |
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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. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C97955" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C97955" NCI Thesaurus) |
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| ID |
http://purl.bioontology.org/ontology/PDQ/CDR0000747816 |
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| altLabel |
Varubi SCH619734 rolapitant monohydrochloride monohydrate 1,7-diazaspiro(4.5)decan-2-one, 8-(((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-, monohydrochloride, monohydrate, (5S,8S)- SCH-619734 rolapitant hydrochloride monohydrate
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| CAS Registry |
914462-92-3
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| cui |
C3467952 C3273721 C4053548
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| DATE FIRST PUBLISHED |
2013-03-18
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| Date last modified |
2015-09-04
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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. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C97955" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C97955" NCI Thesaurus)
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| LT |
TRD
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| NCI ID |
C97955
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| notation |
CDR0000747816
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| ORIG STY |
Drug/agent
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| prefLabel |
rolapitant hydrochloride
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| tui |
T109 T121
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