替尼达普

替尼达普
臨床資料
ATC碼
法律規範狀態
法律規範
  • 未上市
识别信息
  • 5-chloro-2-hydroxy-3-(2-thienylcarbonyl)-1H-indole-1-carboxamide
CAS号120210-48-2  checkY
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)
化学信息
化学式C14H9ClN2O3S
摩尔质量320.75 g·mol−1
3D模型（JSmol（英语：JSmol））
  • c1cc(sc1)C(=O)c2c3cc(ccc3n(c2O)C(=O)N)Cl
  • InChI=1S/C14H9ClN2O3S/c15-7-3-4-9-8(6-7)11(13(19)17(9)14(16)20)12(18)10-2-1-5-21-10/h1-6,19H,(H2,16,20) ☒N
  • Key:IZSFDUMVCVVWKW-UHFFFAOYSA-N ☒N

替尼达普（INN：tenidap）[1]是一种环氧合酶/5-脂氧合酶(COX/5-LOX)双效抑制剂和细胞因子调节消炎药候选药物[2]。由辉瑞公司开发的具有治疗类风湿性关节炎前景的潜在药物[3]。但因其肝肾毒性原因，1996年上市批准遭到美国FDA拒绝，辉瑞因此停止了对其开发[4]。造成其肝肾毒性的原因是药物结构中含有噻吩基团的部分在体内代谢过程中会造成氧化损伤[5]。

参考文献

  1. ^ 刘治军,韩红蕾 (编). 华法林+替尼达普(warfarin+tenidap). 药物相互作用基础与临床 第三版. 北京: 人民卫生出版社. 2019. 
  2. ^ Wylie G, Appelboom T, Bolten W, Breedveld FC, Feely J, Leeming MR, et al. A comparative study of tenidap, a cytokine-modulating anti-rheumatic drug, and diclofenac in rheumatoid arthritis: a 24-week analysis of a 1-year clinical trial. British Journal of Rheumatology. June 1995, 34 (6): 554–63. PMID 7543348. doi:10.1093/rheumatology/34.6.554. 
  3. ^ Staff, American Journal of Nursing. Drug Watch: Tenidap Offers Arthritis Therapy Minus Toxicity （页面存档备份，存于互联网档案馆） AJN 1996 96(1):58
  4. ^ Pfizer. Sept 27, 1996 Press release: Pfizer To Halt Plans For Commercialization Of Tenidap For Rheumatoid Arthritis 互联网档案馆的存檔，存档日期2016-03-05.
  5. ^ Hwang SH, Wecksler AT, Wagner K, Hammock BD. Rationally designed multitarget agents against inflammation and pain. Current Medicinal Chemistry. 2013, 20 (13): 1783–99. PMC 4113248 可免费查阅. PMID 23410172. doi:10.2174/0929867311320130013. 

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