NCI Drug Dictionary

The NCI Drug Dictionary contains technical definitions and synonyms for drugs/agents used to treat patients with cancer or conditions related to cancer. Each drug entry includes links to check for clinical trials listed in NCI's List of Cancer Clinical Trials.

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fosnetupitant/palonosetron hydrochloride
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). Check for active clinical trials using this agent. (NCI Thesaurus)

Synonym:fosnetupitant/palonosetron HCl combination
fosnetupitant-palonosetron HCl
pronetupitant/palonosetron HCl
pro-netupitant/palonosetron HCl
Abbreviation:IV NEPA FDC