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.
- netupitant and palonosetron hydrochloride
An orally available combination formulation containing netupitant, 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 oral administration, 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. Netupitant 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). Check for active clinical trials using this agent. (NCI Thesaurus)
Synonym: netupitant/palonosetron hydrochloride US brand name: Akynzeo