WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 100695
CAS#: 135729-62-3 (HCl); 135729-61-2 (free base).
Description: Palonosetron (INN, trade name Aloxi) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). It is used for the control of delayed CINVÂ—nausea and vomiting and there are tentative data to suggest that it may be better than granisetron. Palonosetron is administered intravenously, as a single dose, 30 minutes before chemotherapy, or as a single oral capsule one hour before chemotherapy. The oral formulation was approved on August 22, 2008 for prevention of acute CINV alone, as a large clinical trial did not show oral administration to be as effective as intravenous use against delayed CINV. (Source: http://en.wikipedia.org/wiki/Palonosetron).
MedKoo Cat#: 100695
Name: Palonosetron HCl
CAS#: 135729-62-3 (HCl); 135729-61-2 (free base).
Chemical Formula: C19H25ClN2O
Molecular Weight: 332.87
Elemental Analysis: C, 68.56; H, 7.57; Cl, 10.65; N, 8.42; O, 4.81
Synonym: RS 25233-197; RS25233-197; RS-25233-197; RS25233-198; RS-25233-198; RS 25233-198; RS-25259-197; Palonosetron hydrochloride; US brand name: Aloxi.
IUPAC/Chemical Name: (R)-2-((S)-quinuclidin-3-yl)-2,3,3a,4,5,6-hexahydro-1H-benzo[de]isoquinolin-1-one hydrochloride
InChi Key: OLDRWYVIKMSFFB-KPVRICSOSA-N
InChi Code: InChI=1S/C19H24N2O.ClH/c22-19-16-6-2-4-14-3-1-5-15(18(14)16)11-21(19)17-12-20-9-7-13(17)8-10-20;/h2,4,6,13,15,17H,1,3,5,7-12H2;1H/t15-,17+;/m0./s1
SMILES Code: O=C1N([C@@H]2CN3CCC2CC3)C[C@@]4([H])C5=C1C=CC=C5CCC4.[H]Cl
P alonosetron hydrochloride is the hydrochloride salt of palonosetron, a carbazole derivative and a selective serotonin receptor antagonist with antiemetic activity. Palonosetron competitively blocks the action of serotonin at 5-hydroxytryptamine type 3 (5-HT3) receptors located on vagal afferents in the chemoreceptor trigger zone (CTZ), resulting in suppression of chemotherapy-induced nausea and vomiting. The CTZ is located in the area postrema on the dorsal surface of the medulla oblongata at the caudal end of the fourth ventricle and outside the blood-brain barrier (BBB). Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
Palonosetron is administered intravenously, as a single dose, 30 minutes before chemotherapy, or as a single oral capsule one hour before chemotherapy. The oral formulation was approved on August 22, 2008 for prevention of acute CINV alone, as a large clinical trial did not show oral administration to be as effective as intravenous use against delayed CINV.
ALOXI is an antiemetic and antinauseant agent. It is a serotonin subtype 3 (5-HT3) receptor antagonist with a strong binding affinity for this receptor. The empirical formula is C19H24N2O.HCl, with a molecular weight of 332.87. Palonosetron hydrochloride is a white to off-white crystalline powder. It is freely soluble in water, soluble in propylene glycol, and slightly soluble in ethanol and 2-propanol. ALOXI Injection is a sterile, clear, colorless, non-pyrogenic, isotonic, buffered solution for intravenous administration. Each 5 mL vial of ALOXI Injection contains 0.25 mg palonosetron base as hydrochloride, 207.5 mg mannitol, disodium edetate and citrate buffer in water for intravenous administration. The pH of the solution is 4.5 to 5.5.
Mechanism of Action
Palonosetron is a 5-HT3 receptor antagonist with a strong binding affinity for this receptor and little or no affinity for other receptors. Cancer chemotherapy may be associated with a high incidence of nausea and vomiting, particularly when certain agents, such as cisplatin, are used. 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema. It is thought that chemotherapeutic agents produce nausea and vomiting by releasing serotonin from the enterochromaffin cells of the small intestine and that the released serotonin then activates 5-HT3 receptors located on vagal afferents to initiate the vomiting reflex.
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