来曲唑

化合物

来曲唑(英语:Letrozole),商品名复乳纳(英语:Femara),是治疗乳癌的口服药物[4]。也用于治疗女性不孕症,促进排卵[4]。它只用于治疗更年期后的乳腺癌[5]

来曲唑
临床资料
商品名英语Drug nomenclature复乳纳/Femara
AHFS/Drugs.comMonograph
MedlinePlusa698004
核准状况
给药途径口服给药
药物类别英语Drug class芳香环转化酶抑制剂英语Aromatase inhibitor抗雌激素英语Antiestrogen
ATC码
法律规范状态
法律规范
药物动力学数据
生物利用度99.9%
血浆蛋白结合率60%,主要是白蛋白
药物代谢pharmacologically-inactive metabolites Bis(4-cyanophenyl)methanol and 4,4'-dicyanobenzophenone.[3]
生物半衰期2天[3]
排泄途径[3]
识别信息
  • 4,4'-((1H-1,2,4-triazol-1-yl)methylene)dibenzonitrile
CAS号112809-51-5  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.200.357 编辑维基数据链接
化学信息
化学式C17H11N5
摩尔质量285.31 g·mol−1
3D模型(JSmol英语JSmol
  • N#Cc1ccc(cc1)C(c2ccc(C#N)cc2)n3ncnc3
  • InChI=1S/C17H11N5/c18-9-13-1-5-15(6-2-13)17(22-12-20-11-21-22)16-7-3-14(10-19)4-8-16/h1-8,11-12,17H checkY
  • Key:HPJKCIUCZWXJDR-UHFFFAOYSA-N checkY

常见副作用包括高胆固醇血症潮热、关节痛和肿胀[4]。其他副作用包括可能不孕、疲劳和骨质疏松[4]。怀孕期使用可能会伤害婴儿[4]。它是一种芳香环转化酶抑制剂英语Aromatase inhibitor[4]

来曲唑于1986年获得专利,并于1996年取得医疗使用许可[6]。名列世界卫生组织基本药物标准清单[7]。已有学名药流通于市[8]

参考文献

  1. ^ Femara- letrozole tablet, film coated. DailyMed. 13 May 2022 [28 August 2022]. 
  2. ^ List of nationally authorised medicinal products : Active substance(s): letrozole : Procedure No. PSUSA/00001842/202110 (PDF). Ema.europa.eu. [30 June 2022]. 
  3. ^ 3.0 3.1 3.2 Letrozole. 24 January 2003 [30 June 2022]. (原始内容存档于24 January 2003). 
  4. ^ 4.0 4.1 4.2 4.3 4.4 4.5 Letrozole Monograph for Professionals. Drugs.com. [21 November 2021]. (原始内容存档于10 August 2020) (英语). "Letrozole Monograph for Professionals". Drugs.com. Archived from the original on 10 August 2020. Retrieved 21 November 2021.
  5. ^ BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021: 999. ISBN 978-0857114105. 
  6. ^ Fischer J, Ganellin CR. Analogue-based Drug Discovery. John Wiley & Sons. 2006: 516 [2020-09-19]. ISBN 9783527607495. (原始内容存档于2016-12-20) (英语). 
  7. ^ World Health Organization. The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023). Geneva: World Health Organization. 2023. WHO/MHP/HPS/EML/2023.02. 
  8. ^ Letrozole Prices, Coupons & Savings Tips - GoodRx. GoodRx. [21 November 2021]. (原始内容存档于14 November 2016).