Palonosetron Hydrochloride

한글명:Palonosetron Hydrochloride

카스 번호135729-62-3

상품명:Palonosetron Hydrochloride

CBNumberCB0210849

분자식C19H25ClN2O

포뮬러 무게332.87

MOL 파일135729-62-3.mol

화학적 성질

녹는점	>290°C
알파	D25 -94.1° (c = 0.4 in water)
저장 조건	Inert atmosphere,Store in freezer, under -20°C
용해도	Methanol (Slightly, Heated), Water (Slightly)
물리적 상태	고체
물리적 상태	단단한 모양
색상	흰색에서 황백색까지
optical activity	[α]/D -90 to -110°, c =0.4 in H2O
수용성	H2O: 20mg/mL, clear
Merck	14,6997
InChI	InChI=1/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-;/s3
InChIKey	OLDRWYVIKMSFFB-HYCRUXCXNA-N
SMILES	N1(C[C@@]2([H])CCCC3=CC=CC(=C32)C1=O)[C@H]1[C@]2([H])CCN(CC2)C1.Cl \|&1:2,15,16,r\|
CAS 데이터베이스	135729-62-3(CAS DataBase Reference)

위험 및 안전 성명

HS 번호

29339900

그림문자(GHS)

Palonosetron Hydrochloride 화학적 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
용도
(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.
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.

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