You Position: Home > Paper
Innovation of anti-inflammatory drugs - strategy of moderate inhibition of cyclooxygenases
( views:184, downloads:24 )
- Author:
- No author available
- Journal Title:
- ACTA PHARMACEUTICA SINICA
- Issue:
- 11
- DOI:
- 10.3321/j.issn:0513-4870.2005.11.002
- Key Word:
- 抗炎药物;环氧合酶;适度抑制
Abstract： @@ 由来罗非昔布(rofecoxib)为选择性环氧合酶-2(COX-2)抑制剂,由默克公司研发,以商品名万络于1999年上市,临床上治疗骨关节炎和风湿性关节炎.数年来与辉瑞公司的新药塞来昔布(celecoxib,商品名西乐葆)并驾称雄于抗炎药物市场,年销售额各达30亿美元.然而好景不长,罗非昔布因引起心血管事件于2004年9月被迫撤出市场,尽管美国FDA的专家以微弱多数肯定了抗炎效果,但元气大伤,已无回天之力.
- [1]C, Bombardier,L, Laine,A, Reicin,etc.Comparison of upper gastrointestinal toxicity of rofecoxib and naproxen in patients with rheumatoid arthritis. VIGOR Study Group.[J].2000,343(21).
- [2]W L, Xie,J G, Chipman,D L, Robertson,etc.Expression of a mitogen-responsive gene encoding prostaglandin synthase is regulated by mRNA splicing.[J].1991,88(7).
- [3]Jane A. Mitchell,Timothy D. Warner.Cyclooxygenase-3 (COX-3): Filling in the gaps toward a COX continuum?[J].2002,99(21).
- [4]Warner TD,Giuliano F,Vojnovic I,etc.Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis.[J].1999,96(13).
- [5]J A, Mitchell,P, Akarasereenont,C, Thiemermann,etc.Selectivity of nonsteroidal antiinflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase.[J].1993,90(24).
- [6]Tacconelli S,Patrignani P,Capone ML.Clinical Pharmacology of Novel Selective COX-2 Inhibitors.[J].2004,10(6).
- [7]Garret A, FitzGerald.Cardiovascular pharmacology of nonselective nonsteroidal anti-inflammatory drugs and coxibs: clinical considerations.[J].2002,89(6A).
- [8]Burr AM,Faich G,Stenson WF,etc.Gastrointestinal toxicity with celecoxib vs nonsteroidal anti-inflammatory drugs for osteoarthritis and rheumatoid arthritis: the CLASS study: A randomized controlled trial. Celecoxib Long-term Arthritis Safety Study (see comments)[J].2000,284(10).
- [9]VANE J. R..Inhibition of Prostaglandin Synthesis as a Mechanism of Action for Aspirin-like Drugs[J].1971.
- [10]de Leval-X,Delarge J,Somers F,etc.Recent advances in inducible cyclooxygenase (COX-2) inhibition.[J].2000,7(10).
- [11]Khan KN,Verburg KM,Lefkowith JB,etc.Pharmacology of cyclooxygenase-2 inhibition in the kidney.[J].2002,61(4).
- [12]Vane, John R..Back to an Aspirin a Day?[J].2002,296(5567).