아자셋론

Azasetron
아자셋론
Azasetron Structure.svg
임상 데이터
AHFS/Drugs.com국제 의약품명
루트
행정부.
오랄
ATC 코드
  • 없음.
약동학 데이터
바이오 어베이러빌리티90%
배설물60-70%
식별자
  • N-(1-아자비시클로[2.2]옥탄-8-일)-6-클로로-4-메틸-3-옥소-1,4-벤조옥사진-8-카르복사미드
CAS 번호
PubChem CID
IUPHAR/BPS
켐스파이더
유니
케그
첸블
CompTox 대시보드 (EPA )
화학 및 물리 데이터
공식C17H20클론N3O3
몰 질량349.82 g/120−1
3D 모델(JSmol)
  • CN1C(=O)COC2c1cc(Cl)cc2C(=O)NC3CN4CC3CC4
  • InChI=1S/C17H20ClN3O3/c1-20-14-7-11(18)6-12(16)24-9-15(20)22)17(23)19-13-21-21-10(133-5-21/7-10,135-2
  • 키: WUKZPHOXUVCOR-UHFFFAOYSA-N checkY
(표준)

Azasetron5-HT3 수용체 길항제인 pKi = 9.27로 작용하는 구토제로, 암 화학요법(시스플라틴 화학요법 등)에 의해 유발되는 메스꺼움 및 구토 관리에 사용된다.염산아자세트론은 구강 또는 정맥주사로 매일 한 번 10mg의 일반 용량으로 투여된다.일본에서의 마케팅이 인정되어 도리이 제약 주식회사가 「세로톤 I.V.」라고 하는 상호로 독점 판매되고 있다.주사 10mg" 및 "세로톤 태블릿 10mg"[2]입니다.S의 약동학 데이터.츠카고시[3]

R-Azasetron besylate(SENS-401)는 갑작스러운 감각성 [4][6]난청(SSNHL),[4] 음향 [5]외상 및 시스플라틴 유도 이독성관련된 난청을 예방하기 위해 연구되었다.

레퍼런스

  1. ^ "Azasetron". drugcentral.org/. UNM School of Medicine. 2016-07-31. Retrieved 2016-11-11.
  2. ^ "Torii Pharmaceutical to Solely Market Antiemetic Drugs". Torii Pharmaceutical Co Ltd. 2009-01-13. Archived from the original on 2014-06-13. Retrieved 2016-11-11.
  3. ^ Tsukagoshi S (June 1999). "[Pharmacokinetics of azasetron (Serotone), a selective 5-HT3 receptor antagonist]". Gan to Kagaku Ryoho. Cancer & Chemotherapy. 26 (7): 10011008. PMID 10396331.
  4. ^ a b "Drug and Device News". P & T. 42 (10): 608651. October 2017. 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 (February 2019). "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). 40 (2): 254263. doi:10.1097/mao.0000000000002088. PMID 30570608.
  6. ^ Petremann M, Tran Van Ba C, Broussy A, Romanet C, Dyhrfjeld-Johnsen J (October 2017). "Oral Administration of Clinical Stage Drug Candidate SENS-401 Effectively Reduces Cisplatin-induced Hearing Loss in Rats". Otology & Neurotology. Ovid Technologies (Wolters Kluwer Health). 38 (9): 13551361. doi:10.1097/mao.0000000000001546. PMID 28796092.