Preferred Label : Fosrolapitant/Palonosetron;
NCIt synonyms : Palonosetron/Fosrolapitant; Anti-emetic Agent HR20013; Palonosetron-Fosrolapitant; Fosrolapitant-Palonosetron;
NCIt definition : An injectable, ultra-long-acting combination formulation containing fosrolapitant,
a selective neurokinin 1 (NK1) receptor antagonist, and the hydrochloride salt form
of palonosetron, a selective serotonin (5-hydroxytryptamine; 5-HT) receptor subtype
3 (5-HT3) antagonist, with antiemetic activity. Upon administration of fosrolapitant/palonosetron,
palonosetron competitively blocks the action of 5-HT at 5-HT3 receptors located on
vagal afferent nerves in the chemoreceptor trigger zone (CTZ). This inhibits acute
emesis associated with 5-HT secretion and subsequent 5-HT3 activation. Fosrolapitant,
able to cross the blood brain barrier (BBB), competitively binds to and blocks the
activity of the human NK1 receptors in the central nervous system (CNS), thereby inhibiting
NK1 receptor binding of the endogenous tachykinin neuropeptide substance P (SP). This
prevents delayed emesis, which is associated with SP secretion. Altogether, this results
in the prevention of chemotherapy-induced nausea and vomiting (CINV). By combing fosrolapitant
with palonosetron both the acute and delayed emesis phases are covered.;
CAS number : 2573694-38-7;
Molecule name : H R20013; H-R20013;
NCI Metathesaurus CUI : CL1798652;
Origin ID : C189825;
UMLS CUI : C5706557;
Semantic type(s)
- concept_is_in_subset
