The coxibs, selective inhibitors of cyclooxygenase-2

New England Journal of Medicine

Volumn 345, Issue 6, 2001, Pages 433-442

  FitzGerald, Garret A ^a   Patrono, Carlo ^b  

^a UNIVERSITY OF PENNSYLVANIA   (United States)

^b UNIVERSITY OF CHIETI   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

6 METHOXY 2 NAPHTHYLACETIC ACID; ACETYLSALICYLIC ACID; ANTIHYPERTENSIVE AGENT; CELECOXIB; CYCLOOXYGENASE 1; CYCLOOXYGENASE 2; CYCLOOXYGENASE 2 INHIBITOR; CYTOCHROME P450 INHIBITOR; DICLOFENAC; DIGOXIN; ETORICOXIB; IBUPROFEN; INDOMETACIN; MELOXICAM; NAPROXEN; NIMESULIDE; NONSTEROID ANTIINFLAMMATORY AGENT; PARACETAMOL; PROSTAGLANDIN G; PROSTAGLANDIN H; PROSTAGLANDIN SYNTHASE; ROFECOXIB; UNCLASSIFIED DRUG; VALDECOXIB; WARFARIN;

ANTIINFLAMMATORY ACTIVITY; CARDIOVASCULAR DISEASE; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG MECHANISM; DRUG METABOLISM; DRUG POTENTIATION; DRUG SELECTIVITY; DRUG TOLERABILITY; GASTROINTESTINAL SYMPTOM; HUMAN; IC 50; INFLAMMATION; KIDNEY FUNCTION; OSTEOARTHRITIS; PAIN; PRIORITY JOURNAL; REVIEW; THROMBOSIS;

ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; ARTHRITIS; CARDIOVASCULAR DISEASES; CYCLOOXYGENASE 2; CYCLOOXYGENASE 2 INHIBITORS; CYCLOOXYGENASE INHIBITORS; DRUG INTERACTIONS; FEMALE; GASTROINTESTINAL DISEASES; HUMANS; ISOENZYMES; KIDNEY; LACTONES; MALE; MEMBRANE PROTEINS; PROSTAGLANDIN-ENDOPEROXIDE SYNTHASES; PYRAZOLES; SULFONAMIDES; SULFONES; TREATMENT OUTCOME;

EID: 0035833502     PISSN: 00284793     EISSN: None     Source Type: Journal    
DOI: 10.1056/NEJM200108093450607     Document Type: Review

References (96)

1. Arachidonic acid oxygenation by COX-1 and COX-2: Mechanisms of catalysis and inhibition
2. 2 synthase
3. Inhibition by corticosteroids of epidermal growth factor-induced recovery of cyclooxygenase after aspirin inactivation
4. Inhibition of eicosanoid biosynthesis by glucocorticoids in humans
5. Selective regulation of cellular cyclooxygenase by dexamethasone and endotoxin in mice
6. Expression of a mitogen-responsive gene encoding prostaglandin synthase is regulated by mRNA splicing
7. Dexamethasone inhibits mitogen induction of the T1S10 prostaglandin synthase/cyclooxygenase gene
8. cDNA cloning and functional activity of a glucocorticoid-regulated inflammatory cyclooxygenase
9. Selective expression of mitogen-inducible cyclooxygenase in macrophages stimulated with lipopolysaccharide
10. Transforming growth factor-β1 enhances Ha-ras-induced expression of cyclooxygenase-2 in intestinal epithelial cells via stabilization of mRNA
11. Induction of prostaglandin endoperoxide synthase-1 (COX-1) in a human promonocytic cell line by treatment with the differentiating agent TPA
12. Distinct roles of prostaglandin H synthases 1 and 2 in T-cell development
13. Cyclooxygenase-1 and -2 expression in rheumatoid synovial tissues: Effects of interleukin-1β, phorbol ester, and corticosteroids
14. Augmented expression of cyclooxygenase-2 in human atherosclerotic lesions
15. Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents
16. The productive conformation of arachidonic acid bound to prostaglandin synthase
17. 4-[5-Methyl-3-phenylisoxazol-4-yl]-benzenesulfonamide, valdecoxib: A potent and selective inhibitor of COX-2
18. Etoricoxib (MK-0663): Preclinical profile and comparison with other agents that selectively inhibit cyclooxygenase-2
19. 2 production in healthy subjects
20. Biochemical and pharmacological characterization of the cyclooxygenase activity of human blood prostaglandin endoperoxide synthases
21. Gastrointestinal toxicity with celecoxib vs nonsteroidal anti-inflammatory drugs for osteoarthritis and rheumatoid arthritis: The CLASS study: A randomized controlled trial
22. Comparison of upper gastrointestinal toxicity of rofecoxib and naproxen in patients with rheumatoid arthritis
23. Differential inhibition of human prostaglandin endoperoxide synthase-1 and -2 by nonsteroidal anti-inflammatory drugs
24. Rofecoxib [Vioxx, MK-0966;4-(4′-methylsulfonylphenyl)-3-phenyl-2-(5H)-furanone]: A potent and orally active cyclooxygenase-2 inhibitor: Pharmacological and biochemical profiles
25. Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: A full in vitro analysis
26. Cyclooxygenase-1 and cyclooxygenase-2 selectivity of widely used nonsteroidal anti-inflammatory drugs
27. Biochemical selectivity of rofecoxib in rheumatoid arthritis
28. Dose-dependent inhibition of platelet cyclooxygenase-1 and monocyte cyclooxygenase-2 by meloxicam in healthy subjects
29. Risk of hospitalization for upper gastrointestinal tract bleeding associated with ketorolac, other nonsteroidal anti-inflammatory drugs, calcium antagonists, and other antihypertensive drugs
30. The risk of upper gastrointestinal complications associated with nonsteroidal anti-inflammatory drugs, glucocorticoids, acetaminophen, and combination of these agents
31. Major role of human liver microsomal cytochrome P450 2C9 (CYP2C9) in the oxidative metabolism of celecoxib, a novel cyclooxygenase-II inhibitor
32. Clinical pharmacokinetics and pharmacodynamics of celecoxib: A selective cyclo-oxygenase-2 inhibitor
33. 14C]celecoxib in healthy male volunteers
34. Celecoxib, a specific COX-2 inhibitor, has no significant effect on methotrexate pharmacokinetics in patients with rheumatoid arthritis
35. Single and multiple dose pharmacokinetics (PK) of rofecoxib (R) in healthy subjects
36. Pharmacokinetics, COX-2 specificity, and tolerability of supratherapeutic doses of rofecoxib in humans
37. Pharmacokinetics of rofecoxib in mild to moderate hepatic insufficiency (H1)
38. Effect of rofecoxib (R) on the pharmacodynamics and pharmacokinetics (PK) of warfarin (W)
39. Synthesis, characterization, and activity of metabolites derived from the cyclooxygenase-2 inhibitor rofecoxib (MK-0966, Vioxx)
40. Comparison of the effect of rofecoxib (a cyclooxygenase 2 inhibitor), ibuprofen, and placebo on the gastroduodenal mucosa of patients with osteoarthritis: A randomized, double-blind, placebo-controlled trial
41. Preliminary study of the safety and efficacy of SC-58635, a novel cyclooxygenase 2 inhibitor: Efficacy and safety in two placebo-controlled trials in osteoarthritis and rheumatoid arthritis, and studies of gastrointestinal and platelet effects
42. Treatment of osteoarthritis with celecoxib, a cyclooxygenase-2 inhibitor: A randomized controlled trial
43. Celecoxib: A review of its use in osteoarthritis, rheumatoid arthritis and acute pain
44. Rofecoxib, a specific inhibitor of cyclooxygenase 2, with clinical efficacy comparable with that of diclofenac sodium: Results of a one-year, randomized, clinical trial in patients with osteoarthritis of the knee and hip
45. A randomized trial of the efficacy and tolerability of the COX-2 inhibitor rofecoxib vs ibuprofen in patients with osteoarthritis
46. Anti-inflammatory and upper gastrointestinal effects of celecoxib in rheumatoid arthritis: A randomized controlled trial
47. Effect of regulated expression of human cyclooxygenase isoforms on eicosanoid and isoeicosanoid production in inflammation
48. Pharmacological and biochemical demonstration of the role of cyclooxygenase 2 in inflammation and pain
49. Inducible cyclooxygenase may have anti-inflammatory properties
50. Adverse upper gastrointestinal effects of rofecoxib compared with NSAIDs
51. Misoprostol reduced serious gastrointestinal complications in patients with rheumatoid arthritis receiving nonsteroidal anti-inflammatory drugs: A randomized, double-blind, placebo-controlled trial
52. Constitutive cyclooxygenase-2 expression in healthy human and rabbit gastric mucosa
53. Helicobacter pylori infection induces cyclooxygenase-2 expression in human gastric mucosa
54. Cyclooxygenase-2 expression in gastric antral mucosa before and after eradication of Helicobacter pylori infection
55. Induction of cyclooxygenase-2 in gastric mucosal lesions and its inhibition by the specific antagonist delays healing in mice
56. Is cyclooxygenase-2 the alpha and the omega in cancer?
57. Cyclooxygenase-2-dependent arachidonic acid metabolites are essential modulators of the intestinal immune response to dietary antigen
58. Impaired mucosal defense to acute colonic injury in mice lacking cyclooxygenase-1 or cyclooxygenase-2
59. Exacerbation of inflammation-associated colonic injury in rat through inhibition of cyclooxygenase-2
60. Increased prostacyclin biosynthesis in patients with severe atherosclerosis and platelet activation
61. Systemic biosynthesis of prostacyclin by cyclooxygenase (COX)-2: The human pharmacology of a selective inhibitor of COX-2
62. Selective cyclooxygenase-2 inhibition by nimesulide in man
63. Effects of specific inhibition of cyclooxygenase-2 on sodium balance, hemodynamics, and vasoactive eicosanoids
64. Estimated rate of prostacyclin secretion into the circulation of normal man
65. Suppression of eicosanoid biosynthesis during coronary angioplasty by fish oil and aspirin
66. 2 metabolites during leg exercise in humans
67. Identification of vascular endothelial genes differentially responsive to fluid mechanical stimuli: Cyclooxygenase-2, manganese superoxide dismutase, and endothelial cell nitric oxide synthase are selectively up-regulated by steady laminar shear stress
68. Altered pain perception and inflammatory response in mice lacking prostacyclin receptor
69. Thrombosis in patients with connective tissue diseases treated with specific cyclooxygenase 2 inhibitors: A report of four cases
70. Cardiovascular morbidity and mortality in patients with seropositive rheumatoid arthritis in northern Sweden
71. Hemostatic factors and cardiovascular disease in active rheumatoid arthritis: An 8 year followup study
72. Comparative inhibitory activity of rofecoxib, meloxicam, diclofenac, ibuprofen, and naproxen on COX-2 versus COX-1 in healthy volunteers
73. Effects of nabumetone compared with naproxen on platelet aggregation in patients with rheumatoid arthritis
74. Differential effects of aspirin and nonaspirin nonsteroidal antiinflammatory drugs in the primary prevention of myocardial infarction in postmenopausal women
75. Prevention of death, myocardial infarction and stroke by antiplatelet therapy: Collaborative meta-analysis of 266 trials involving 200,000 patients at high risk of occlusive vascular events
76. Platelet-active drugs: The relationships among dose, effectiveness, and side effects
77. Acceleration of atherogenesis by COX-1-dependent prostanoid formation in low density lipoprotein receptor knockout mice
78. Oxidative damage of cardiomyocytes is limited by extracellular regulated kinases 1/2-mediated induction of cyclooxygenase-2
79. Cyclooxygenase-2 mediates the cardioprotective effects of the late phase of ischemic preconditioning in conscious rabbits
80. Renal abnormalities and an altered inflammatory response in mice lacking cyclooxygenase II
81. Cyclooxygenase-2-selective inhibitors impair glomerulogenesis and renal cortical development
82. Immunolocalization of cyclooxygenase 2 in the macula densa of human elderly
83. The clinical significance of inhibition of renal prostaglandin synthesis
84. Randomized evaluations of the effects of cyclooxygenase-2 inhibition on renal function in elderly persons receiving a low-salt diet: A randomized, controlled trial
85. Renal safety and tolerability of celecoxib, a novel cyclooxygenase-2 inhibitor
86. Renal aspects of treatment with conventional nonsteroidal anti-inflammatory drugs versus cyclooxygenase-2 specific inhibitors
87. Effects of nimesulicle on constitutive and inducible prostanoid biosynthesis in human beings
88. Comparison of inhibitory effects of meloxicam and diclofenac on human thromboxane biosynthesis after single doses and at steady state
89. Do cyclooxygenase-2 inhibitors provide benefits similar to those of traditional nonsteroidal anti-inflammatory drugs, with less gastrointestinal toxicity?
90. Nimesulide: Some pharmaceutical and pharmacological aspects - An update
91. Selective inhibition of COX-2 in humans is associated with less gastrointestinal injury: A comparison of nimesulide and naproxen
92. Double-blind study evaluating by endoscopy the tolerability of nimesulide and diclofenac on the gastric mucosa in osteoarthritic patients
93. Multi-centre double-blind study to define the most favourable dose of nimesulide in terms of efficacy/safety ratio in the treatment of osteoarthritis
94. Gastrointestinal tolerability of meloxicam compared to diclofenac in osteoarthritis patients
95. Improvement in gastrointestinal tolerability of the selective cyclooxygenase (COX)-2 inhibitor, meloxicam, compared with piroxicam: Results of the Safety and Efficacy Large-scale Evaluation of COX-inhibiting Therapies (SELECT) trial in osteoarthritis
96. Gastrointestinal safety profile of meloxicam: A meta-analysis and systematic review of randomized controlled trials