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palonosetron hydrochloride CAS:135729-62-3

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palonosetron hydrochloride CAS:135729-62-3

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Place of Origin: Weifang,China
Brand Name: RuzE
Model Number: TC-5045

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Detailed Product Description
Product Name: Palonosetron Hydrochloride Synonyms: (3aS)-2-(3S)-1-Azabicyclo[2.2.2]oct-3-yl-2,3,3a,4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one Monohydrochloride;(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;Aloxi;Onicit;RS-25259-197;(S,S)-Palono
CAS: 135729-62-3 MF: C19H25ClN2O
MW: 332.87 EINECS: 680-630-6

Weifang Ruze New Material Co.,LTD a China supplier of palonosetron hydrochloride (CAS No.:135729-62-3),CAS 135729-62-3 offers for your requirements of RND, evaluation, pilots and commercial along with supportive technical package required for evaluation.

palonosetron hydrochloride  CAS:135729-62-3

                                                                                                                                                                                   

                                                        palonosetron hydrochloride

 

[PRODUCT NAME]:palonosetron hydrochloride

[CATALOG NUMBER]:

[CAS NUMBER]:135729-62-3

[MOLECULAR FORMULA]:C19H25ClN2O

[MOLECULAR WEIGHT]:332.86800

[BATCH NO]: 20190226

[TEST]:SPECIFICATION

[APPEARANCE]: White Crystal Powder

[ASSAY]: 99%min

[WATER]: 0.5%max

[MELTING POINT]: >290ºC


Palonosetron Hydrochloride Chemical Properties

Melting point >290°C
alpha D25 -94.1° (c = 0.4 in water)
storage temp. Refrigerator
Merck 14,6997
CAS DataBase Reference 135729-62-3(CAS DataBase Reference)

Safety Information

HS Code 29339900

 

Palonosetron Hydrochloride Usage And Synthesis

Nausea and vomiting drug Palonosetron hydrochloride is a drug to inhibit nausea and vomiting, which is a new type highly selective, high-affinity 5-HT3 receptor antagonist that can block the vomiting reflex center peripheral neurons presynaptic 5-HT. Receptor excitement directly affects the central nervous system in 5-HT. Impulse receptor excitement generated by the role of vagal afferent nerve after area, blocking the vagus nerve endings in the gut, preventing signals to 5-HT. Receptor trigger zone can reduce the incidence of nausea and vomiting. Central clinically for the treatment of acute severe emetogenic chemotherapy induced delayed nausea and vomiting. Because of its high curative effect, little side effect, long half-life (about 40 h), small dosage, and so on, it has attracted much attention.
With 1,2,3,4-tetrahydro-1-naphthoic acid as the starting material, the split, amination, reduction, cyclization, salt of palonosetron hydrochloride granisetron.
Clinical studies showed that palonosetron can be used safely with corticosteroids, analgesics, antiemetics, antispasmodics and anticholinergic drugsas the starting material, the split, amination, reduction, cyclization, salt of palonosetron hydrochloride granisetron.
Murine tumor model studies indicate that palonosetron does not inhibit the five kinds of chemotherapy drugs studied (cisplatin, cyclophosphamide, cytarabine, doxorubicin and mitomycin C) anti-cancer activity.
Adverse effects The most common adverse effects are headache, which occurs in 4–11% of patients, and constipation in up to 6% of patients. In less than 1% of patients, other gastrointestinal disorders occur, as well as sleeplessness, first-and second-degree atrioventricular block, muscle pain and shortness of breath. Palonosetron is similarly well tolerated as other setrons, and slightly less than placebo.
References https://en.wikipedia.org/wiki/Palonosetron
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.
Chemical Properties White Solid
Originator Syntex (Roche Bioscience) (US)
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.[Cayman Chemical]
Uses 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.
Definition ChEBI: A hydrochloride obtained by combining palonosetron with one molar equivalent of hydrogen chloride; an antiemetic used in combination with netupitant (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy.
Brand name Aloxi (Helsinn).

 

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palonosetron hydrochloride  CAS:135729-62-3

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