期刊文献+

新型类风湿关节炎治疗药物托法替尼 被引量:10

Tofacitinib,a new drug for the treatment of rheumatoid arthritis
原文传递
导出
摘要 托法替尼是辉瑞公司开发的一种口服小分子Janus激酶(Janus kinase,JAK)抑制剂,于2012年11月获得美国FDA批准,用于治疗甲氨蝶呤反应不足或不耐受的中度至重度类风湿关节炎成年患者。本文对其药理作用、药动学、临床研究以及安全性等做一综述。 Tasocitinib is an oral small-molecule Janus kinase(JAK) inhibitor developed by Pfizer.In November 2012,Food and Drug Administration(FDA) has approved tasocitinib for the treatment of adults with moderately to severely active rheumatoid arthritis(RA) who have had an inadequate response or intolerance to methotrexate.The pharmacology,pharmacokinetics,clinical efficacy and safety of tofacitinib were reviewed in this paper.
机构地区 天津药物研究院
出处 《中国新药杂志》 CAS CSCD 北大核心 2013年第14期1607-1609,1680,共4页 Chinese Journal of New Drugs
关键词 类风湿关节炎 JANUS激酶 托法替尼 rheumatoid arthritis Janus kinase tofacitinib
  • 相关文献

参考文献18

  • 1ARNETT FC,EDWORTHY SM, BLOCH DA,et al. The American rheumatism association 1987 revised criteria for classification ofrheumatoid arthritis [ J ]. Arthritis Rheum, 1988,31 ( 3 ) : 315 - 324.
  • 2PERICOLINI E, ALUNNO A, GABRIELLI E, et al. The microbial capsular polysaceharide galactoxylomannan inhibits IL-17A production in circulating T cells from rheumatoid arthritis patients [J]. PLoS 0ne,2013,8(1): e53336.
  • 3ZERBINI CA, LOMONTE AB. Tofaeitinib for the treatment of rheumatoid arthritis [J]. Expert Rev Clin lmmunol, 2012,8 (4) : 319 -331.
  • 4CHAPARRO DEL MORAL R, RILLO OL,CASALLA L, et al. Work productivity in rheumatoid arthritis: relationship with clinical and radiological features[ J]. Arthritis, 2012 : 137635.
  • 5MCINNES IB, LIEW FY. Cytokine networks-towards new thera- pies for rheumatoid arthritis [ J ]. Nat Clin Pract Rheumatol, 2005,11(1) :31 -39.
  • 6FLANAGAN ME, BLUMENKOPF TA, BRISSETTE WH, et al. Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection [ J ]. J Med Chem, 2010,53 ( 24 ) : 8468 - 8484.
  • 7GHORESCHI K, JESSON MI, LI X, et al. Modulation of innate and adaptive immune responses by tofaeitinib (CP-690,550) [J]. J lmmunol,2011,186(7) : 4234 -4243.
  • 8TANAKA Y,MAESHIMA Y, YAMAOKA K. In vitro and in vivo analysis of a JAK inhibitor in rheumatoid arthritis [J]. Ann Rheum Dis ,2012,71 (2) :70 -74.
  • 9KARAMAN MW,HERRGARD S,TREIBER DK, et al. A quan- titative analysis of kinase inhibitor selectivity [ J ]. Nat Biotechnol,2008,26(1) : 127 - 132.
  • 10CHANGELIAN PS,FLANAGAN ME,BALL DJ,et al. Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor[J]. Science.2003.302(5646): 875 -878.

同被引文献69

  • 1王文娟,刘艳芳,赵性泉.脑出血治疗指南[J].中国卒中杂志,2006,1(12):888-899. 被引量:75
  • 2李瑞,孟庆刚.类风湿性关节炎的临床治疗研究[J].中华中医药学刊,2007,25(7):1348-1352. 被引量:35
  • 3FDA. FDA approves Xeljanz for rheumatoid arthritis[EB/OL] . 2012[2015 -03 -12]. http://www.fda.gov/newsevents/news?room/pressannouncements/ucm327152. html.
  • 4BHIRUD SB, MISHRA S, NARAYANAN SB, et at. Process for the preparation of tofacitinib and intermediates thereof: WO, 2014102826 Al[PJ. 2013 -12 - 27.
  • 5LARSEN SD, GRIECO PA. Aza Diels-Alder reactions in aque?ous solution: cyclocondensation of dienes with simple iminium salts generated under Mannich conditions[J].J Am Chem Soc, 1985, 107(6): 1768 -1769.
  • 6CAl WL, COLONYJL, FROST H, et at. Investigation of practi- cal routes for the kilogram-scale production of cis-3-methylamino- 4-methylpiperidines[J]. Org Process Res Dev, 2005, 9 ( 1 ) : 51 - 56.
  • 7WILCOX GE, KOECHER C, VRIES T, et al. Optical resolution of ( I-benzyI4-methylpiperidi-3 -yl ) -rnethylamine and thereof for the preparation of pyrrolo-2, 3 -pyrimidine derivatives as protein kinases inhibitors: W 0, 02096909 Al[P]. 2002 - 12 - 05 .
  • 8JIANGJK, GHORESCHI K, DEFLORIAN F, et al, Examining the chirality, conformation and selective kinase inhibition of 3- ( (3R ,4R) 4-methyl-3-( methyl ( 7 H-pyrrolo[2 ,3-dJ pyrimidin4- yl) amino) piperidin-l=yl ) -3-oxopropanenitrile ( CP-690, 550)[J].J Med Chern, 2008, 51(24) :8012 -8018.
  • 9HAO BY, LIUJQ, ZHANG WH, et al, A novel asymmetric syn?thesis of cis-f 3R, 4R ) -N-( tert-butoxycarbonyl ) 4-methyl-3- (methylamino) piperidine[J]. Synthesis, 2011, 2011 (8): 1208 -1212.
  • 10HAO BY, LIUJQ, ZHANG WH, et al, Chiral pool synthesis of Nvcba-cis-f 3R, 4R) -3-methylamino4-methylpiperidine from L?malic acid[J]. Bull Korean Chem Soc, 2013, 34 (5) : 1371 - 1377.

引证文献10

二级引证文献48

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部