非布司他(Febuxostat)是一种用于治疗痛风的药物,而藥品所針對的痛風基本因尿酸水平过高而引起[4]。該藥物通過抑制黄嘌呤氧化酶,从而减少体内尿酸的产生。該藥的給藥途徑口服。該藥常见的副作用包括肝脏出現问题、恶心、关节痛和皮疹[4]等症狀。妊娠或哺乳期婦女不建议服用該藥物[5][6]

非布司他
臨床資料
商品名英语Drug nomenclatureUloric, Adenuric[1]
AHFS/Drugs.comMonograph
MedlinePlusa609020
核准狀況
懷孕分級
给药途径口服
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度≥84% absorbed
血漿蛋白結合率99.2% to albumin
药物代谢通過CYP1A1英语CYP1A1, CYP1A2, CYP2C8英语CYP2C8, CYP2C9, UGT1A1英语UGT1A1, UGT1A8英语UGT1A8, UGT1A9英语UGT1A9[3]
生物半衰期~5–8 小時
排泄途徑Urine (~49%, mostly as metabolites, 3% as unchanged drug); feces (~45%, mostly as metabolites, 12% as unchanged drug)
识别信息
  • 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-
    1,3-thiazole-5-carboxylic acid
CAS号144060-53-7  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.207.329 編輯維基數據鏈接
化学信息
化学式C16H16N2O3S
摩尔质量316.38 g·mol−1
3D模型(JSmol英语JSmol
  • N#Cc1c(OCC(C)C)ccc(c1)c2nc(c(s2)C(=O)O)C
  • InChI=1S/C16H16N2O3S/c1-9(2)8-21-13-5-4-11(6-12(13)7-17)15-18-10(3)14(22-15)16(19)20/h4-6,9H,8H2,1-3H3,(H,19,20) checkY
  • Key:BQSJTQLCZDPROO-UHFFFAOYSA-N checkY

非布司他于2008年和2009年分别在欧盟和美国被批准用于医疗用途[7][4]。2019年,该藥的仿制藥被監管部門批准,2020年起正式上市[8] [9]

参考文献

编辑
  1. ^ Drugs.com Drugs.com international names for febuxostat页面存档备份,存于互联网档案馆) Page accessed June 25, 2015
  2. ^ 2.0 2.1 Febuxostat (Uloric) Use During Pregnancy. Drugs.com. 22 February 2019 [17 May 2020]. (原始内容存档于2021-02-09). 
  3. ^ Adenuric: EPAR – Product Information (PDF). European Medicines Agency. 2019-08-06 [2021-02-04]. (原始内容 (PDF)存档于2021-08-28). 
  4. ^ 4.0 4.1 4.2 Febuxostat Monograph for Professionals. Drugs.com. American Society of Health-System Pharmacists. [26 February 2019]. (原始内容存档于2021-02-08) (英语). 
  5. ^ British national formulary : BNF 76 76. Pharmaceutical Press. 2018: 1087. ISBN 9780857113382. 
  6. ^ Drug Safety and Availability - FDA adds Boxed Warning for increased risk of death with gout medicine Uloric (febuxostat). FDA. 21 February 2019 [26 February 2019]. (原始内容存档于2019-04-23) (英语). 
  7. ^ Adenuric. European Medicines Agency - Commission. 17 September 2018 [26 February 2019]. (原始内容存档于2020-12-30) (英语). 
  8. ^ Generic Uloric Availability. Drugs.com. [1 August 2019]. (原始内容存档于2020-11-11) (英语). 
  9. ^ Febuxostat Generic Uloric. [15 April 2020]. (原始内容存档于2016-10-16).