About: Rolapitant Hydrochloride     Goto   Sponge   NotDistinct   Permalink

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AttributesValues
rdf:type
rdfs:label
  • Rolapitant Hydrochloride
rdfs:subClassOf
Has_Free_Acid_Or_Base_Form
Concept_In_Subset
Semantic_Type
  • Pharmacologic Substance
Preferred_Name
  • Rolapitant Hydrochloride
NCI_META_CUI
  • CL430561
CAS_Registry
  • 914462-92-3
FDA_UNII_Code
  • 57O5S1QSAQ
Contributing_Source
  • FDA
PDQ_Open_Trial_Search_ID
  • 747752
PDQ_Closed_Trial_Search_ID
  • 747752
Chemical_Formula
  • C25H26F6N2O2.ClH.H2O
FULL_SYN
  • Rolapitant HydrochloridePTNCI
  • ROLAPITANT HYDROCHLORIDEPTFDA57O5S1QSAQ
  • 1,7-Diazaspiro(4.5)decan-2-one, 8-(((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-, Monohydrochloride, Monohydrate, (5S,8S)-SNNCI
  • SCH619734CNNCI
  • SCH-619734CNNCI
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, by 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.NCI
code
  • C97955
is Has_Salt_Form of
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