丙酚替诺福韦


丙酚替诺福韦Tenofovir alafenamide,缩写TAF,商品名韦立德Vemlidy))是一种口服抗逆转录病毒药物,临床上应用其延胡索酸盐的形式(富马酸丙酚替诺福韦) 用于治疗乙型肝炎或与其他药物联用治疗艾滋病

丙酚替诺福韦
临床资料
读音/ˌtəˈnfəvɪər ˌæləˈfɛnəmd/
商品名英语Drug nomenclature韦立德(Vemlidy)
其他名称GS-7340
AHFS/Drugs.comMonograph
核准状况
怀孕分级
给药途径口服
ATC码
法律规范状态
法律规范
药物动力学数据
血浆蛋白结合率~80%[3]
生物半衰期33分钟
排泄途径肠道排泄(31.7%)和肾脏排泄(<1%)
识别信息
  • Isopropyl (2S)-2-[[[(1R)-2-(6-aminopurin-9-yl)-1-methyl-ethoxy]methyl-phenoxy-phosphoryl]amino]propanoate
CAS号379270-37-8  checkY
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
化学信息
化学式C21H29N6O5P
摩尔质量476.47 g·mol−1
3D模型(JSmol英语JSmol
  • C[C@H](CN1C=NC2=C(N=CN=C21)N)OC[P@@](=O)(N[C@@H](C)C(=O)OC(C)C)OC3=CC=CC=C3
  • InChI=1S/C21H29N6O5P/c1-14(2)31-21(28)16(4)26-33(29,32-17-8-6-5-7-9-17)13-30-15(3)10-27-12-25-18-19(22)23-11-24-20(18)27/h5-9,11-12,14-16H,10,13H2,1-4H3,(H,26,29)(H2,22,23,24)/t15-,16+,33+/m1/s1
  • Key:LDEKQSIMHVQZJK-CAQYMETFSA-N

该药为替诺福韦前药,由吉利德科学研发。与常用的逆转录酶抑制剂替诺福韦二吡呋酯(TDF)相比,丙酚替诺福韦具有更强的抗病毒活性和更好的淋巴组织分布。[5][6]该药于2016年11月获得FDA批准上市。[7]

相关复方药物

  • 恩曲他滨/丙酚替诺福韦 [8] — 2016 年 4 月在美国获得批准治疗HIV。2019年10月,该药在美国被批准用于HIV-1暴露前预防(PrEP)。 [9] [10]
  • 达芦那韦/考比司他/恩曲他滨/丙酚替诺福韦[11] — 欧盟于2017年9月、美国于2018年7月、澳大利亚于2019年11月相继批准该药上市。[12][13][14]
  • 多替拉韦/恩曲他滨/丙酚替诺福韦。[15]

参考文献

  1. ^ 1.0 1.1 Tenofovir alafenamide (Vemlidy) Use During Pregnancy. Drugs.com. 26 December 2018 [18 April 2020]. (原始内容存档于2021-07-09). 
  2. ^ Vemlidy 25 mg film coated tablets - Summary of Product Characteristics (SmPC). (emc). 8 September 2020 [12 November 2020]. (原始内容存档于2021-07-11). 
  3. ^ 3.0 3.1 Vemlidy- tenofovir alafenamide tablet. DailyMed. 11 February 2020 [18 April 2020]. (原始内容存档于2021-07-09). 
  4. ^ Vemlidy EPAR. European Medicines Agency (EMA). [2021-07-01]. (原始内容存档于2021-07-13). 
  5. ^ Metabolism of GS-7340, a novel phenyl monophosphoramidate intracellular prodrug of PMPA, in blood. Nucleosides Nucleotides Nucleic Acids. 2001, 20 (4–7): 1091–8. PMID 11562963. doi:10.1081/NCN-100002496. 
  6. ^ M Markowitz, A Zolopa, et al.
  7. ^ FDA Approves Vemlidy (tenofovir alafenamide) for Chronic Hepatitis B in Adults. United States Department of Health and Human Services. 21 November 2016 [11 October 2019]. (原始内容存档于11 October 2019). 
  8. ^ Descovy- emtricitabine and tenofovir alafenamide tablet. DailyMed. 13 January 2020 [18 April 2020]. (原始内容存档于2021-06-24). 
  9. ^ FDA approves second drug to prevent HIV infection as part of ongoing efforts to end the HIV epidemic. U.S. Food and Drug Administration (FDA). 3 October 2019 [11 October 2019]. (原始内容存档于11 October 2019). 
  10. ^ Mandavilli, Apoorva. F.D.A. Approves New H.I.V.-Prevention Drug, but Not for Everyone. The New York Times. 4 October 2019 [11 October 2019]. (原始内容存档于2021-07-09). 
  11. ^ Symtuza- darunavir, cobicistat, emtricitabine, and tenofovir alafenamide tablet, film coated. DailyMed. 6 March 2020 [18 April 2020]. (原始内容存档于2021-07-09). 
  12. ^ Drug Approval Package: Symtuza (darunavir, cobicistat, emtricitabine, and tenofovir alafenamide). U.S. Food and Drug Administration (FDA). 11 December 2018 [19 August 2020]. (原始内容存档于2021-07-09). 
  13. ^ Symtuza EPAR. European Medicines Agency. [19 August 2020]. (原始内容存档于2021-07-10). 
  14. ^ http://www.ebs.tga.gov.au/servlet/xmlmillr6?dbid=ebs/PublicHTML/pdfStore.nsf&docid=CCE11C6BC5177A30CA2585AE00423857&agid=(PrintDetailsPublic)&actionid=1[失效链接]
  15. ^ Drugs@FDA: FDA-Approved Drugs. U.S. Food and Drug Administration (FDA). [5 December 2020]. (原始内容存档于2021-07-09). 

外部链接