氨柔比星

化合物

氨柔比星INN:amrubicin;开发代号:SM-5887)是一种用于治疗肺癌蒽环类药物[1]它自2002年起由住友制药以商品名Calsed在日本销售。[2]

氨柔比星
臨床資料
AHFS/Drugs.com国际药品名称
给药途径IV
ATC碼
法律規範狀態
法律規範
  • 处方药(-only)
识别信息
  • (7S,9S)-9-Acetyl-9-amino-7-[(2S,4S,5R)-4,5-dihydroxyoxan-2-yl]oxy-6,11-dihydroxy-8,10-dihydro-7H-tetracene-5,12-dione
CAS号110267-81-7  checkY
PubChem CID
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
化学信息
化学式C25H25NO9
摩尔质量483.47 g·mol−1
3D模型(JSmol英语JSmol
  • O=C2c1c(O)c5c(c(O)c1C(=O)c3ccccc23)C[C@](C(=O)C)(N)C[C@@H]5O[C@@H]4OC[C@@H](O)[C@@H](O)C4
  • InChI=1S/C25H25NO9/c1-10(27)25(26)7-13-18(16(8-25)35-17-6-14(28)15(29)9-34-17)24(33)20-19(23(13)32)21(30)11-4-2-3-5-12(11)22(20)31/h2-5,14-17,28-29,32-33H,6-9,26H2,1H3/t14-,15+,16-,17-,25-/m0/s1 checkY
  • Key:VJZITPJGSQKZMX-XDPRQOKASA-N checkY

氨柔比星通过抑制拓扑异构酶II发挥作用,并在临床试验中与拓扑替康(拓扑异构酶I抑制剂)进行了比较。[3][4]

它还被研究用于治疗膀胱癌[5]胃癌[6]

氨柔比星是第一个通过从头合成的蒽环类衍生物,由住友化学家的科学家于1989年首次发表。[7]

参考资料

  1. ^ Ueoka H, Ohnoshi T, Kimura I. [New anthracycline analogues in the treatment of lung cancer]. Gan to Kagaku Ryoho. November 1992, 19 (13): 2146–9. PMID 1332624 (日语). 
  2. ^ Sumitomo Pharmaceuticals Co., Ltd. CALSED for Injection (English) (PDF). 2003 [2008-08-17].  [失效連結]
  3. ^ Celgene Corporation. Amrubicin(R) Receives FDA Orphan Drug Designation for the Treatment of Small Cell Lung Cancer. 2008 [2009-07-10]. (原始内容存档于2013-01-19). 
  4. ^ Medical News Today. Pharmion's Amrubicin Shows Encouraging Results Compared To Standard Of Care In Second Line Treatment Of Small Cell Lung Cancer. 2007 [2009-07-10]. (原始内容存档于2009-01-03). 
  5. ^ Ohmori H, Tsushima T, Kobashi K. [Experimental studies on intravesical instillation of SM-5887, a novel anthracycline derivative for treatment of bladder carcinoma]. Gan to Kagaku Ryoho. April 1996, 23 (5): 601–6. PMID 8678519 (日语). 
  6. ^ Tsushima K, Sakata Y, Munakata A, et al. [A phase II study of SM-5887 for advanced gastric cancer]. Gan to Kagaku Ryoho. June 1991, 18 (7): 1151–4. PMID 1647150 (日语). 
  7. ^ Hanada M. Amrubicin, Chapter 6 in Case Studies in Modern Drug Discovery and Development. Eds. Huang X and Aslanian RG. John Wiley & Sons, 2012 ISBN 9780470601815 P 106