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• CAS: 135729-62-3 Palonosetron Hydrochloride

  Product Name: Palonosetron Hydrochloride
  

  Synonyms: (S)-2-((S)-quinuclidin-3-yl)-2,3,3a,4,5;Palonosetron hydrochloride, 99.5%, a 5-HT3 antagonist;PALONOSETRON HCL;PALONOSETRON HYDROCHLORIDE;CS-292;Palonosetronhydrochloride hydrochloride;Palonosetron-d3 HCl;(3aS)-2-(3S)-1-Azabicyclo[2.2.2]oct-3-yl-2,3,3a,4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one Hydrochloride

  CAS: 135729-62-3

  MF: C19H25ClN2O

  MW: 332.87

  EINECS: 680-630-6

  Product Categories: Selective 5-HT3 Receptor Antagonist;Chiral Reagents;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;API

  
  

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Product Introduction:

Description Palonosetron is a novel 5-HT3 receptor antagonist launched as an injectable agent for the prevention of acute and delayed nausea and vomiting associated with cancer chemotherapy. It has a much longer half-life (～ 40 h) than the other currently available 5-HT3 antagonists, which provides efficacy advantages in the prevention of delayed nausea and vomiting that typically occurs after 24 h and up to six days post chemotherapy administration. Palonosetron was developed as a conformationally restricted analog of the previously known 5HT3 antagonists tropisetron and granisetron. It is synthesized in four steps starting with the condensation of 1,8- naphthalic anhydride and (S)-3-aminoquinuclidine to produce the corresponding imide. The subsequent steps include catalytic hydrogenation of one of the aromatic rings of the imide intermediate, selective reduction of one of the carbonyls to a hydroxyl group, dehydration to an olefin and catalytic hydrogenation. The recommended dosage of palonosteron is 0.25 mg, administered as a single intravenous dose approximately 30 min before the start of chemotherapy. Palonosetron exhibits dose-proportional pharmacokinetics and it is moderately bound to plasma proteins (62%). Fifty percent of the dose is metabolized in the liver, and 40% is excreted unchanged in the urine. In comparative clinical studies with two other 5- HT3 receptor antagonists, palonosetron is shown to be as effective as dolasetron and more effective than ondansetron in controlling acute nausea and vomiting and superior to both in the control of delayed nausea and vomiting. Efficacy of palonosetron has been demonstrated in patients receiving initial and repeat courses of both moderately and highly emetogenic chemotherapy, including cisplatin, cyclophosphamide and dacarbazine. At 0.25 and 0.75 mg doses, palonosetron is well tolerated and the most occurring adverse events are headache, diarrhea, fatigue, abdominal pain and insomnia.

Uses (S,S)-Palonosetron Hydrochloride is a serotonin 5-HT3 receptor antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). Antiemetic.

Uses Palonosetron HCl is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting

Uses specifically inhibits cells of the adrenal cortex and their production of hormones for adrenocortical tumor therapy, causes CNS damage, but no bone marrow depression.

Uses Palonosetron is a potent, selective antagonist of the serotonin (5-HT) receptor 5-HT3 (pKi = 10.4 in rat cortex) that minimally effects a wide range of other neuronal receptors. It is orally bioavailable and potently inhibits emesis induced by chemotherapeutic drugs, like cisplatin , but not by apomorphine , which acts by dopamine receptor antagonism. Palonosetron is remarkable for its long duration of action, related to its high receptor-binding affinity and long half-life. It is effective in managing chemotherapy-induced nausea and vomiting."

Chemical Properties White Solid