Preferred Label : Fosnetupitant/Palonosetron Hydrochloride;
NCIt synonyms : Pro-netupitant/Palonosetron; Fosnetupitant-Palonosetron HCl; IV NEPA FDC; Pronetupitant/Palonosetron; Fosnetupitant/Palonosetron HCl Combination;
NCIt definition : A combination formulation containing the prodrug of netupitant, fosnetupitant, a selective
neurokinin 1 receptor (NK1R; TACR1) antagonist, and the hydrochloride salt form of
palonosetron, a selective serotonin (5-hydroxytrytamine; 5-HT) receptor subtype 3
(5-HT3R) antagonist, with potential antiemetic activity. Upon intravenous administration,
fosnetupitant is converted by phosphatases to its active form netupitant. Netupitant
competitively binds to and blocks the activity of NK1Rs in the central nervous system
(CNS), by inhibiting binding of the endogenous tachykinin-derived neuropeptide substance
P (SP) to NK1R. This prevents delayed emesis, which is associated with SP secretion.
Palonosetron competitively blocks the interaction of 5-HT with 5-HT3Rs located on
vagal afferent nerves in the chemoreceptor trigger zone (CTZ). This inhibits acute
emesis associated with 5-HT secretion and subsequent 5-HT3R activation. Altogether,
this results in inhibition of acute and delayed nausea and vomiting, and may prevent
chemotherapy-induced nausea and vomiting (CINV).;
NCI Metathesaurus CUI : CL544714;
Origin ID : C146720;
UMLS CUI : C4687438;
Semantic type(s)
- concept_is_in_subset
- has_free_acid_or_base_form
- has_target
