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阿扎司瓊

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阿扎司瓊
臨床資料
AHFS/Drugs.com國際藥品名稱
給藥途徑口服
ATC碼
  • 未分配
藥物動力學數據
生物利用度90%
排泄途徑60-70%
識別資訊
  • N-(1-azabicyclo[2.2.2]octan-8-yl)-6-chloro-4-methyl-3-oxo-1,4-benzoxazine-8-carboxamide
CAS號123040-69-7
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard英語CompTox Chemicals Dashboard (EPA)
化學資訊
化學式C17H20ClN3O3
摩爾質量349.82 g·mol−1
3D模型(JSmol英語JSmol
  • CN1C(=O)COc2c1cc(Cl)cc2C(=O)NC3CN4CCC3CC4
  • InChI=1S/C17H20ClN3O3/c1-20-14-7-11(18)6-12(16(14)24-9-15(20)22)17(23)19-13-8-21-4-2-10(13)3-5-21/h6-7,10,13H,2-5,8-9H2,1H3,(H,19,23) checkY
  • Key:WUKZPHOXUVCQOR-UHFFFAOYSA-N checkY

阿扎司瓊(英語:Azasetron)是一種止吐藥,作為5-HT3受體英語5-HT3 receptor拮抗劑英語5-HT3 antagonist,pKi=9.27,[1]用於治療癌症化療(如順鉑化療)引起的噁心和嘔吐。鹽酸阿扎司瓊的常用劑量為10毫克,每日一次,口服或靜脈注射。它在日本獲准上市,由鳥居製藥有限公司獨家銷售,商品名為「Serotone I.V. Injection 10 mg」和「Serotone Tablets 10 mg」。[2]該藥物的藥代動力學數據來自塚越茂(Tsukagoshi Shigeru)。[3]

苯磺酸R-阿扎司瓊(R-azasetron besylate,SENS-401)已被研究用於預防與突發感音神經性聽力損失[4]聲創傷英語Acoustic trauma[5]和順鉑引起的耳毒性英語Ototoxicity相關的聽力損失。[4][6]

參考資料

  1. ^ Azasetron. drugcentral.org/. UNM School of Medicine. 2016-07-31 [2016-11-11]. (原始內容存檔於2020-09-21). 
  2. ^ Torii Pharmaceutical to Solely Market Antiemetic Drugs. Torii Pharmaceutical Co Ltd. 2009-01-13 [2016-11-11]. (原始內容存檔於2014-06-13). 
  3. ^ Tsukagoshi S. [Pharmacokinetics of azasetron (Serotone), a selective 5-HT3 receptor antagonist]. Gan to Kagaku Ryoho. Cancer & Chemotherapy. June 1999, 26 (7): 10011008. PMID 10396331. 
  4. ^ 4.0 4.1 Drug and Device News. P & T. October 2017, 42 (10): 608651. PMC 5614410可免費查閱. PMID 29018295. SENS-401 for Platinum-Induced Ototoxicity Sensorion has received the FDAs orphan drug designation for SENS-401 for the prevention of platinum-induced ototoxicity in pediatric patients. As many as 60% of patients develop severe hearing loss due to platinum-based chemo therapies. There is no approved pharmaceutical treatment. SENS-401 (R-azasetron besylate) is designed to protect and preserve inner ear tissue when lesions may cause progressive hearing impairments. The drug (both oral and injectable) is also in development for the treatment of sudden sensorineural hearing loss. Sensorion expects to initiate a phase 2 clinical trial in this indication in the first half of 2018. 
  5. ^ Petremann M, Romanet C, Broussy A, Van Ba CT, Poli S, Dyhrfjeld-Johnsen J. SENS-401 Effectively Reduces Severe Acoustic Trauma-Induced Hearing Loss in Male Rats With Twice Daily Administration Delayed up to 96hours. Otology & Neurotology (Ovid Technologies (Wolters Kluwer Health)). February 2019, 40 (2): 254263. PMID 30570608. doi:10.1097/mao.0000000000002088. 
  6. ^ Petremann M, Tran Van Ba C, Broussy A, Romanet C, Dyhrfjeld-Johnsen J. Oral Administration of Clinical Stage Drug Candidate SENS-401 Effectively Reduces Cisplatin-induced Hearing Loss in Rats. Otology & Neurotology (Ovid Technologies (Wolters Kluwer Health)). October 2017, 38 (9): 13551361. PMID 28796092. doi:10.1097/mao.0000000000001546.