阿扎司瓊

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
	IUPAC命名法 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	2264;
IUPHAR/BPS	2285;
ChemSpider	2177 ;
UNII	77HC7URR9Z;
KEGG	D07481 ;
ChEMBL	ChEMBL1598608;
CompTox Dashboard（英語：CompTox Chemicals Dashboard） (EPA)	DTXSID7045651 ;
化學資訊
化學式	C17H20ClN3O3
摩爾質量	349.82 g·mol−1
3D模型（JSmol（英語：JSmol））	交互式圖像;
	SMILES CN1C(=O)COc2c1cc(Cl)cc2C(=O)NC3CN4CCC3CC4;
	InChI 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) ; Key:WUKZPHOXUVCQOR-UHFFFAOYSA-N ;

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），pK_i=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

^ Azasetron. drugcentral.org/. UNM School of Medicine. 2016-07-31 [2016-11-11]. （原始內容存檔於2020-09-21）.
^ 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）.
^ 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.
^ ^4.0 ^4.1 Drug and Device News. P & T. October 2017, 42 (10): 608651. PMC 5614410 . 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.
^ 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.
^ 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.

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[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.

[Pharmacy_and_Therapeutics_2022-4] 4.0 ^4.1 Drug and Device News. P & T. October 2017, 42 (10): 608651. PMC 5614410 . 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.

[Petremann_2019-5] 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.

[Petremann_2017-6] 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.

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