厄洛替尼
厄洛替尼(英語:,商品名:Tarceva,特罗凯)是用于治疗非小细胞肺癌(NSCLC)、胰腺癌等几种癌症的药物,作为一种酪氨酸激酶抑制剂作用于表皮生长因子受体,由罗氏公司生产。
系统(IUPAC)命名名称 | |
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N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy) quinazolin-4-amine | |
临床数据 | |
商品名 | Tarceva |
Drugs.com | Monograph |
MedlinePlus | a605008 |
医疗法规 | |
妊娠分级 |
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给药途径 | Oral tablets |
合法狀態 | |
合法状态 |
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药代动力学数据 | |
生物利用度 | 59% |
蛋白结合度 | 95% |
代谢 | Hepatic (mainly CYP3A4, less CYP1A2) |
生物半衰期 | 36.2 hrs (median) |
排泄 | >98% as metabolites, of which >90% via faeces, 9% via urine |
识别 | |
CAS注册号 | 183321-74-6 |
ATC代码 | L01XE03 |
PubChem | CID 176870 |
DrugBank | DB00530 |
ChemSpider | 154044 |
UNII | J4T82NDH7E |
KEGG | D07907 |
ChEBI | CHEBI:114785 |
ChEMBL | CHEMBL553 |
化学 | |
化学式 | C22H23N3O4 |
摩尔质量 | 393.436 g/mol |
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藥物合成
- 第一種合成路徑
- 第二種合成路徑
参考文献
外部链接
- Official Tarceva website
- Tarceva Discussion Group for Cancer Patients
- Sordella R, Bell DW, Haber DA, Settleman J. . Science. August 2004, 305 (5687): 1163–7. PMID 15284455. doi:10.1126/science.1101637..
- Genzyme "Genzyme Launches Exclusive Lung Cancer Test" Press Release September 27, 2005
- "Determinants of Tumor Response and Survival With Erlotinib in Patients With Non-Small-Cell Lung Cancer, Journal of Clinical Oncology, August 15, 2004.
- October 2003 issue of Lung Cancer Frontiers on rash/effectiveness correlation
- FAQ: I started an EGFR inhibitor two weeks ago but haven’t developed a rash. Does this mean it’s not working?, Dr. Howard L. (Jack) West, M.D., GRACE页面存档备份,存于, February 21, 2011 (directed toward the layperson).
- http://www.cancer.gov/clinicaltrials/results/lung-and-erlotinib0604l%5B%5D
- https://web.archive.org/web/20081012081613/http://www.roche.com/med-cor-2007-10-22
- https://web.archive.org/web/20110726060413/http://www.roche.com/med-cor-2009-05-30b
- https://web.archive.org/web/20120918193637/http://www.cipla.com/whatsnew/news.htm#27apr09
- https://web.archive.org/web/20120918193637/http://www.cipla.com/whatsnew/news.htm#20mar08
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