达可替尼

达可替尼
臨床資料
商品名（英语：Drug nomenclature）Vizimpro
其他名稱PF-00299804
AHFS/Drugs.comMonograph
MedlinePlusa618055
核准狀況
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80%
血漿蛋白結合率98%
药物代谢CYP2D6、CYP3A4
代謝產物O-去甲基达可替尼
生物半衰期70小时
排泄途徑79%分辨、3%尿液
识别信息
  • (2E)-N4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl4-(1-piperidinyl)-2-butenamide
CAS号1110813-31-4  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB配體ID
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)
化学信息
化学式C24H25ClFN5O2
摩尔质量469.95 g·mol−1
3D模型（JSmol（英语：JSmol））
  • COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)NC(=O)/C=C/CN4CCCCC4
  • InChI=1S/C24H25ClFN5O2/c1-33-22-14-20-17(24(28-15-27-20)29-16-7-8-19(26)18(25)12-16)13-21(22)30-23(32)6-5-11-31-9-3-2-4-10-31/h5-8,12-15H,2-4,9-11H2,1H3,(H,30,32)(H,27,28,29)/b6-5+
  • Key:LVXJQMNHJWSHET-AATRIKPKSA-N

达可替尼（INN：dacomtinib；商品名：Vizimpro）或译达克替尼，是一种治疗非小细胞肺癌（NSCLC）的药物。它是一种选择性且不可逆的表皮生长因子受体（EGFR）抑制剂。[3]

达可替尼已进入多项III期临床试验。2014年1月首次试验的结果令人失望，未能达到研究目标。[4][5][6]其他III期试验仍在进行中。[4]

2017年，一项比较达可替尼和吉非替尼治疗NSCLC（由突变EGFR驱动）的试验结果被公布了。[7]

达可替尼于2018年9月在美国、[8]2019年在日本、2019年在欧盟[9]被批准用于医疗用途，用于治疗EGFR基因突变的非小细胞肺癌。

参考资料

  1. ^ Vizimpro Product information. Health Canada. 25 April 2012 [29 May 2022]. （原始内容存档于2022-05-29）. 
  2. ^ Summary Basis of Decision (SBD) for Verzenio. Health Canada. 23 October 2014 [29 May 2022]. （原始内容存档于2022-05-31）. 
  3. ^ Dacomitinib. NCI Drug Dictionary. National Cancer Institute, U.S. Department of Health and Human Services. [2024-04-07]. （原始内容存档于2015-04-28）. 
  4. ^ 4.0 4.1 Chustecka Z. Dacomitinib Fails in Pretreated Non-small Cell Lung Cancer. Medscape. January 27, 2014 [2024-04-07]. （原始内容存档于2017-06-13）. 
  5. ^ Taylor P. Blow to Pfizer as dacomitinib fails in lung cancer trials. pmlive.com. 28 January 2014 [2024-04-07]. （原始内容存档于2019-03-05）. 
  6. ^ Pfizer Announces Top-Line Results From Two Phase 3 Trials Of Dacomitinib In Patients With Refractory Advanced Non-Small Cell Lung Cancer. Pfizer Press Release. January 27, 2014 [2024-04-07]. （原始内容存档于2019-06-11）. 
  7. ^ Smith M. Dacomitinib Sets PFS Record in Phase III NSCLC Trial. MedPage Today. 6 June 2017 [2024-04-07]. （原始内容存档于2021-05-31）. 
  8. ^ Shirley M. Dacomitinib: First Global Approval. Drugs. December 2018, 78 (18): 1947–1953. PMID 30506139. S2CID 54034570. doi:10.1007/s40265-018-1028-x 可免费查阅. 
  9. ^ Vizimpro EPAR. European Medicines Agency (EMA). 5 June 2019 [13 December 2019]. （原始内容存档于2019-12-13）. 

外部链接

  • Dacomitinib. Drug Information Portal. U.S. National Library of Medicine. [2024-04-07]. （原始内容存档于2022-07-04）. 

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