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Palonosetron Hydrochloride

Palonosetron Hydrochloride 구조식 이미지
카스 번호:
135729-62-3
상품명:
Palonosetron Hydrochloride
동의어(영문):
Aloxi;Onicit;RS 25259;RS-25259-197;Palonosetron HCI;PALONOSETRON HCL;Palonosetron-d3 HCl;(S,S)-Palonosetron HCl;PALONOSETRON HYDROCHLORIDE;Palonosetron Hydrochloride API
CBNumber:
CB0210849
분자식:
C19H25ClN2O
포뮬러 무게:
332.87
MOL 파일:
135729-62-3.mol

Palonosetron Hydrochloride 속성

녹는점
>290°C
알파
D25 -94.1° (c = 0.4 in water)
저장 조건
Refrigerator
Merck
14,6997
CAS 데이터베이스
135729-62-3(CAS DataBase Reference)

안전

HS 번호 29339900

Palonosetron Hydrochloride C화학적 특성, 용도, 생산

개요

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.

화학적 성질

White Solid

Originator

Syntex (Roche Bioscience) (US)

용도

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]

용도

Serotonin 5-HT3 receptor antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). Antiemetic.

용도

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

용도

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

정의

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.

상표명

Aloxi (Helsinn).

Palonosetron Hydrochloride 준비 용품 및 원자재

원자재

준비 용품


Palonosetron Hydrochloride 공급 업체

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ATK CHEMICAL COMPANY LIMITED
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