阿扎司琼

阿扎司琼（英语：Azasetron）是一种止吐药，作为5-HT3受体（英语：5-HT3 receptor）拮抗剂（英语：5-HT3 antagonist），pK_i=9.27，^[1]用于治疗癌症化疗（如顺铂化疗）引起的恶心和呕吐。盐酸阿扎司琼的常用剂量为10毫克，每日一次，口服或静脉注射。它在日本获准上市，由鸟居制药有限公司独家销售，商品名为“Serotone I.V. Injection 10 mg”和“Serotone Tablets 10 mg”。^[2]该药物的药代动力学数据来自冢越茂（Tsukagoshi Shigeru）。^[3]

阿扎司琼

临床资料
AHFS/Drugs.com	国际药品名称
给药途径	口服
ATC码	未分配
药物动力学数据
生物利用度	90%
排泄途径	60-70%
识别信息
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号	123040-69-7
PubChem CID	2264
IUPHAR/BPS	2285
ChemSpider	2177 Y
UNII	77HC7URR9Z
KEGG	D07481 Y
ChEMBL	ChEMBL1598608
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID7045651
化学信息
化学式	C17H20ClN3O3
摩尔质量	349.82 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像
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) Y Key:WUKZPHOXUVCQOR-UHFFFAOYSA-N Y

苯磺酸R-阿扎司琼（R-azasetron besylate，SENS-401）已被研究用于预防与突发感音神经性听力损失、^[4]声创伤（英语：Acoustic trauma）^[5]和顺铂引起的耳毒性（英语：Ototoxicity）相关的听力损失。^[4][6]

参考资料

1. Azasetron. drugcentral.org/. UNM School of Medicine. 2016-07-31 [2016-11-11]. （原始内容存档于2020-09-21）.
2. Torii Pharmaceutical to Solely Market Antiemetic Drugs. Torii Pharmaceutical Co Ltd. 2009-01-13 [2016-11-11]. （原始内容存档于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. 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.
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.