替莫唑胺

替莫唑胺(英语:Temozolomide,简称:TMZ)是一种口服化疗药物(屬於烷基化剂),在商品名帝盟多(英语:Temodar)等下贩售,用于治疗某些脑癌,如成人恶性神经胶质瘤和恶性黑色素瘤。该药物由英國伯明翰阿斯顿大学的教授马尔寇姆史蒂文斯帶領的团队研發成功。[1][2][3]它自1999年8月在美国上市以来便可购得,2000年以後開始在其他国家上市。

替莫唑胺
臨床資料
商品名Temodar, Temodal, Temcad
AHFS/Drugs.comMonograph
MedlinePlusa601250
核准狀況
给药途径Oral, intravenous
ATC碼
法律規範狀態
法律規範
  • 处方药(-only)
  • 处方药(-only)
藥物動力學數據
血漿蛋白結合率15%
药物代谢spontaneously hydrolyzed at physiologic pH to the active species, 3-methyl-(triazen-1-yl)imidazole-4-carboxamide (MTIC) and to temozolomide acid metabolite
生物半衰期1.8 hours
识别
  • 4-methyl-5-oxo-2,3,4,6,8-pentazabicyclo[4.3.0]nona-2,7,9-triene-9-carboxamide
CAS号85622-93-1  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.158.652
化学
化学式C6H6N6O2
摩尔质量194.151 g/mol
3D模型(JSmol
熔点212 °C(414 °F) (分解)
  • O=C(c1ncn2C(=O)N(\N=N/c12)C)N
  • InChI=1S/C6H6N6O2/c1-11-6(14)12-2-8-3(4(7)13)5(12)9-10-11/h2H,1H3,(H2,7,13) checkY
  • Key:BPEGJWRSRHCHSN-UHFFFAOYSA-N checkY

藥物合成

参考文献

  1. Sansom C. (PDF). Chemistry World. July 2009: 48–51 [2018-04-25]. (原始内容存档 (PDF)于2020-10-22).
  2. . Cancer Research UK impact & achievements page. (原始内容存档于14 March 2012).
  3. Newlands ES, Stevens MF, Wedge SR, Wheelhouse RT, Brock C. . Cancer Treatment Reviews. January 1997, 23 (1): 35–61. PMID 9189180. doi:10.1016/S0305-7372(97)90019-0.
This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.