Target General Infomation
Target ID
T03403
Former ID
TTDS00039
Target Name
Cyclooxygenase
Synonyms
Cyclooxygenase (COX1 and COX2); PHS; Prostaglandin H2 synthase; Prostaglandin synthase
Target Type
Successful
Disease Ankylosing spondylitis [ICD9: 720; ICD10: M08.1, M45]
Asthma [ICD10: J45]
Atopic dermatitis [ICD9: 691.8, 692.9; ICD10: L00-L99]
Arthritis [ICD9: 710-719; ICD10: M00-M25]
Back pain [ICD9: 724.5,338,780; ICD10: M54, G89, R52]
Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63]
Cardiovascular disorder [ICD10: I00-I99]
Chemotherapy or radiotherapy-induced mucositis [ICD9: 338, 528.0,780; ICD10: K12.3, R52, G89]
Dysmenorrhea [ICD9: 625.3; ICD10: N94.4-N94.6]
Hyperglyceridemic [ICD9: 790.29; ICD10: R73.9]
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Immuno-modulator [ICD9: 135, 691.8, 692.9, 710-719, 714; ICD10: D86, L20, L20-L30, M00-M25, M05-M06]
Inflammation [ICD10: E08-E13, E10.2, E11, E11.2, E13.2, I73.9, I80-I82, N00-N29, G89]
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51]
Joint and muscular pain; Ankylosing spondylitis [ICD9:719.4, 729.1, 338, 780, 720; ICD10: M25.5, M79.1, G89, R52, M08.1, M45]
Migraine [ICD9: 346; ICD10: G43]
Myocardial infarction; Cerebrovascular ischaemia [ICD9: 410, 434.91; ICD10: I21, I22, I61-I63]
Osteoarthritis of knee [ICD10: M15-M19, M47]
Osteoarthritis [ICD9: 715; ICD10: M15-M19, M47]
Otitis media [ICD10: H65-H67]
Parkinson's disease [ICD9: 332; ICD10: G20]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Postoperative inflammation undergone cataract extraction [ICD code not available]
Platelet aggregatory [ICD10: D69.1]
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06]
Type 2 diabetes; Early nephropathy; Claudication [ICD9: 250, 250.00, 250.02, 250.4, 338, 437.6, 443.9, 453, 580-599, 671.5, 671.9,780; ICD10: E08-E13, E10.2, E11, E11.2, E13.2, I73.9, I80-I82, N00-N29, G89]
Unspecified [ICD code not available]
BioChemical Class
Oxidoreductases acting on paired donors
Target Validation
T03403
Drugs and Mode of Action
Drug(s) Aceclofenac Drug Info Approved Inflammatory disease [524388], [551871]
Acetaminophen Drug Info Approved Pain [538502], [540707]
Ampiroxicam Drug Info Approved Inflammatory disease [551871]
Amtolmetin guacil Drug Info Approved Inflammatory disease [551871]
Asasantin Drug Info Approved Cerebrovascular ischaemia [536186]
Aspirin Drug Info Approved Pain [467484], [536186]
Dexibuprofen Drug Info Approved Ankylosing spondylitis [551871]
Diclofenac Drug Info Approved Osteoarthritis of knee [551871]
Felbinac Drug Info Approved Arthritis [551871]
Fenoprofen Drug Info Approved Rheumatoid arthritis [468052], [538244]
Fosfosal Drug Info Approved Pain [551871]
Icosapent Drug Info Approved Hyperglyceridemic [542465], [550112]
Ketorolac Drug Info Approved Postoperative inflammation undergone cataract extraction [551871]
Lornoxicam Drug Info Approved Migraine [522825], [551871]
Loxoprofen gel Drug Info Approved Inflammatory disease [522818], [551871]
Meclofenamic acid Drug Info Approved Joint and muscular pain; Ankylosing spondylitis [536575], [542233], [551871]
Morniflumate Drug Info Approved Otitis media [551871]
Nepafenac Drug Info Approved Osteoarthritis [542564], [551186], [551871]
Oxaprozin Drug Info Approved Rheumatoid arthritis [551871]
Pelubiprofen Drug Info Approved Back pain [551871]
Pravigard Drug Info Approved Myocardial infarction; Cerebrovascular ischaemia [536186]
Aspirin Drug Info Phase 3 Cardiovascular disorder [467484], [526874], [533508]
K-103-IP Drug Info Phase 3 Pain [524680]
Naproxcinod Drug Info Phase 3 Inflammatory disease [522137]
BN82451 Drug Info Phase 2 Parkinson's disease [524900]
NCX 1022 Drug Info Phase 2 Atopic dermatitis [551443]
NCX-4016 Drug Info Phase 2 Inflammation [527729]
TZI-41078 Drug Info Phase 2 Arthritis [534101]
4-aminosalicylate sodium (oral controlled release, ulcerative colitis), AGI Therapeutics Drug Info Phase 1 Inflammatory bowel disease [548169]
SKF-105809 Drug Info Phase 1 Pain [529852]
Felbinac prodrug Drug Info Preclinical Inflammatory disease [546514]
Droxicam Drug Info Withdrawn from market Inflammatory disease [545401]
Zomepirac Drug Info Withdrawn from market Pain [551871]
Bermoprofen Drug Info Discontinued in Preregistration Inflammatory disease [544769]
Pirazolac Drug Info Discontinued in Preregistration Inflammatory disease [544777]
KC-764 Drug Info Discontinued in Phase 3 Platelet aggregatory [544800]
Benzydamine Drug Info Discontinued in Phase 2 Chemotherapy or radiotherapy-induced mucositis [536838]
D-7193 Drug Info Discontinued in Phase 2 Immuno-modulator [546273]
FS-205-397 Drug Info Discontinued in Phase 2 Pain [545598]
NCX-4016 Drug Info Discontinued in Phase 2 Type 2 diabetes; Early nephropathy; Claudication [536186]
NCX-701 Drug Info Discontinued in Phase 2 Pain [547214]
PSD-508 Drug Info Discontinued in Phase 2 Dysmenorrhea [548659]
D-1367 Drug Info Discontinued in Phase 1 Arthritis [546016]
Eltenac Drug Info Discontinued in Phase 1 Arthritis [545584]
F-11105 Drug Info Discontinued in Phase 1 Asthma [546838]
E-5110 Drug Info Terminated Inflammatory disease [544773]
Florifenine Drug Info Terminated Inflammatory disease [545593]
NMI-1182 Drug Info Terminated Inflammatory disease [547873]
RP-66364 Drug Info Terminated Inflammatory disease [545586]
S-14080 Drug Info Terminated Inflammatory disease [533782]
WY-28342 Drug Info Terminated Rheumatoid arthritis [545972]
Diclofenac Drug Info Investigative Unspecified [525985], [551871]
Modulator 4-aminosalicylate sodium (oral controlled release, ulcerative colitis), AGI Therapeutics Drug Info [531873]
Aceclofenac Drug Info [526718], [551871]
Ampiroxicam Drug Info [528085], [551871]
Amtolmetin guacil Drug Info [527959], [551871]
Bermoprofen Drug Info [529154]
D-1367 Drug Info [550835]
D-7193 Drug Info [550919]
Dexibuprofen Drug Info [526606], [551871]
Diclofenac Drug Info [525985], [551871]
Droxicam Drug Info [526788]
E-5110 Drug Info [533847]
Eltenac Drug Info [525975]
Felbinac Drug Info [533532], [551871]
Felbinac prodrug Drug Info [550035], [551871]
Florifenine Drug Info [533656]
Fosfosal Drug Info [533530], [536361]
FS-205-397 Drug Info [533438], [551871]
K-103-IP Drug Info [524680]
KC-764 Drug Info [527720], [551871]
Lornoxicam Drug Info [525560], [551871]
Morniflumate Drug Info [528117], [551871]
Naproxcinod Drug Info [537263]
NCX 1022 Drug Info [527171]
NCX-701 Drug Info [529064], [544102]
Pelubiprofen Drug Info [531590], [551871]
Pirazolac Drug Info [533491]
RP-66364 Drug Info [550934]
S-14080 Drug Info [550923]
SKF-105809 Drug Info [529852]
TZI-41078 Drug Info [534101], [551871]
WY-28342 Drug Info [533715]
Zomepirac Drug Info [533421], [551871]
Inhibitor Acetaminophen Drug Info [535569], [535717], [536038]
Asasantin Drug Info [536186]
Aspirin Drug Info [536976]
Benzydamine Drug Info [536838]
BN82451 Drug Info [537349]
F-11105 Drug Info [550919]
Fenoprofen Drug Info [536364], [536391]
Ketorolac Drug Info [536379]
Loxoprofen gel Drug Info [532557], [551871]
Meclofenamic acid Drug Info [537872], [537903]
NCX-4016 Drug Info [536186]
Nepafenac Drug Info [526496], [551871]
NMI-1182 Drug Info [527835]
Oxaprozin Drug Info [536391]
Pravigard Drug Info [536186]
PSD-508 Drug Info [550869]
Binder Icosapent Drug Info [535691]
References
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Ref 468052(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4820).
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Ref 524900ClinicalTrials.gov (NCT02231580) Study Exploring Safety, Pharmacokinetic and Pharmacodynamic of BN82451 in Male Huntington's Disease Patients. U.S. National Institutes of Health.
Ref 525985Diclofenac and NS-398, a selective cyclooxygenase-2 inhibitor, decrease agonist-induced contractions of the pig isolated ureter. Urol Res. 2000 Dec;28(6):376-82.
Ref 526874The mechanism of action of aspirin. Thromb Res. 2003 Jun 15;110(5-6):255-8.
Ref 527729Direct and irreversible inhibition of cyclooxygenase-1 by nitroaspirin (NCX 4016). J Pharmacol Exp Ther. 2005 Dec;315(3):1331-7. Epub 2005 Sep 6.
Ref 529852Analgetic activity of SK&F 105809, a dual inhibitor of arachidonic acid metabolism. Agents Actions Suppl. 1991;32:113-7.
Ref 533508Inhibition of prostaglandin synthesis as a mechanism of action for aspirin-like drugs. Nat New Biol. 1971 Jun 23;231(25):232-5.
Ref 533782S14080, a peripheral analgesic acting by release of an endogenous circulating opioid-like substance. Br J Pharmacol. 1995 Jan;114(2):303-8.
Ref 534101Hydroxylamine analogs of 2,6-di-t-butylphenols: dual inhibitors of cyclooxygenase and 5-lipoxygenase or selective 5-lipoxygenase inhibitors. Bioorg Med Chem. 1995 Apr;3(4):403-10.
Ref 536186Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90.
Ref 536575Pharmacology, pharmacokinetics, and therapeutic use of meclofenamate sodium. Clin J Pain. 1991;7 Suppl 1:S44-8.
Ref 536838Emerging drugs for chemotherapy-induced mucositis. Expert Opin Emerg Drugs. 2008 Sep;13(3):511-22.
Ref 538244FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 072267.
Ref 538502FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018337.
Ref 540707(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5239).
Ref 542233(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7219).
Ref 542465(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7441).
Ref 542564(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7564).
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Ref 525560The analgesic NSAID lornoxicam inhibits cyclooxygenase (COX)-1/-2, inducible nitric oxide synthase (iNOS), and the formation of interleukin (IL)-6 in vitro. Inflamm Res. 1999 Jul;48(7):369-79.
Ref 525975Effect of eltenac in horses with induced endotoxaemia. Equine Vet J Suppl. 2000 Jun;(32):26-31.
Ref 525985Diclofenac and NS-398, a selective cyclooxygenase-2 inhibitor, decrease agonist-induced contractions of the pig isolated ureter. Urol Res. 2000 Dec;28(6):376-82.
Ref 526496Topical nepafenac inhibits ocular neovascularization. Invest Ophthalmol Vis Sci. 2003 Jan;44(1):409-15.
Ref 526606Comparison of the efficacy and tolerability of dexibuprofen and celecoxib in the treatment of osteoarthritis of the hip. Int J Clin Pharmacol Ther. 2003 Apr;41(4):153-64.
Ref 526718Aceclofenac spares cyclooxygenase 1 as a result of limited but sustained biotransformation to diclofenac. Clin Pharmacol Ther. 2003 Sep;74(3):222-35.
Ref 526788Pharmacokinetic profile of droxicam. Eur J Rheumatol Inflamm. 1991;11(4):10-4.
Ref 527171Anti-inflammatory effects of nitric oxide-releasing hydrocortisone NCX 1022, in a murine model of contact dermatitis. Br J Pharmacol. 2004 Nov;143(5):618-25. Epub 2004 Aug 16.
Ref 527720Clinical and preclinical pharmacology of KC-764, a novel antiplatelet agent. Nihon Rinsho. 1992 Feb;50(2):379-84.
Ref 527835NMI-1182, a gastro-protective cyclo-oxygenase-inhibiting nitric oxide donor. Inflammopharmacology. 2005;12(5-6):521-34.
Ref 527959Gastrointestinal safety of amtolmetin guacyl in comparison with celecoxib in patients with rheumatoid arthritis. Clin Exp Rheumatol. 2005 Nov-Dec;23(6):809-18.
Ref 528085Premedication with cyclooxygenase-2 inhibitor meloxicam reduced postoperative pain in patients after oral surgery. Int J Oral Maxillofac Surg. 2006 Jul;35(7):613-7. Epub 2006 Mar 15.
Ref 528117Modulation of arachidonic acid metabolism by orally administered morniflumate in man. Agents Actions. 1991 Jul;33(3-4):233-9.
Ref 529064Nitroparacetamol (NCX-701) and pain: first in a series of novel analgesics. CNS Drug Rev. 2007 Fall;13(3):279-95.
Ref 529154Prolongation of antipyretic action and reduction of gastric ulcerogenicity in the rat by controlled-release granules of bermoprofen, a new nonsteroidal anti-inflammatory drug. J Pharm Sci. 1991 Sep;80(9):876-80.
Ref 529852Analgetic activity of SK&F 105809, a dual inhibitor of arachidonic acid metabolism. Agents Actions Suppl. 1991;32:113-7.
Ref 531590Anti-inflammatory effect of pelubiprofen, 2-[4-(oxocyclohexylidenemethyl)-phenyl]propionic acid, mediated by dual suppression of COX activity and LPS-induced inflammatory gene expression via NF-?B inactivation. J Cell Biochem. 2011 Dec;112(12):3594-603.
Ref 5318735-aminosalicylic acid mediates expression of cyclooxygenase-2 and 15-hydroxyprostaglandin dehydrogenase to suppress colorectal tumorigenesis. Anticancer Res. 2012 Apr;32(4):1193-202.
Ref 532557Comparative study of the clinical efficacy of the selective cyclooxygenase-2 inhibitor celecoxib compared with loxoprofen in patients with frozen shoulder. Mod Rheumatol. 2014 Jan;24(1):144-9.
Ref 533421Effect of preischemia cyclooxygenase inhibition by zomepirac sodium on reflow, cerebral autoregulation, and EEG recovery in the cat after global ischemia. J Cereb Blood Flow Metab. 1986 Dec;6(6):691-702.
Ref 533438FS 205-397: a new antipyretic analgesic with a paracetamol-like profile of activity but lack of acute hepatotoxicity in mice. Life Sci. 1988;43(11):905-12.
Ref 533491Differential dosing study of pirazolac, a new non-steroidal anti-inflammatory agent, in patients with rheumatoid arthritis. Curr Med Res Opin. 1985;9(8):542-7.
Ref 533530Pharmacological study of 2-phosphonoxybenzoic acid (fosfosal), a new analgesic drug. Arzneimittelforschung. 1980;30(7):1091-8.
Ref 533532A review of the effects of fenbufen and a metabolite, biphenylacetic acid, on platelet biochemistry and function. Arzneimittelforschung. 1980;30(4A):702-7.
Ref 533656A study of the novel anti-inflammatory agent florifenine topical anti-inflammatory activity and influence on arachidonic acid metabolism and neutrophil functions. Naunyn Schmiedebergs Arch Pharmacol.1995 Mar;351(3):298-304.
Ref 533715Synthesis and antiinflammatory activity of certain 5,6,7,8-tetrahydroquinolines and related compounds. J Med Chem. 1995 Apr 28;38(9):1473-81.
Ref 533847Effect of E-5110, a novel non-steroidal anti-inflammatory drug, on trimethadione metabolism as an indicator of hepatic drug-oxidizing capacity in beagle dog. Xenobiotica. 1994 Mar;24(3):215-20.
Ref 534101Hydroxylamine analogs of 2,6-di-t-butylphenols: dual inhibitors of cyclooxygenase and 5-lipoxygenase or selective 5-lipoxygenase inhibitors. Bioorg Med Chem. 1995 Apr;3(4):403-10.
Ref 535569COX-3, a cyclooxygenase-1 variant inhibited by acetaminophen and other analgesic/antipyretic drugs: cloning, structure, and expression. Proc Natl Acad Sci U S A. 2002 Oct 15;99(21):13926-31. Epub 2002 Sep 19.
Ref 535691Differential modulation of Toll-like receptors by fatty acids: preferential inhibition by n-3 polyunsaturated fatty acids. J Lipid Res. 2003 Mar;44(3):479-86. Epub 2002 Dec 1.
Ref 535717COX-3: just another COX or the solitary elusive target of paracetamol? Lancet. 2003 Mar 22;361(9362):981-2.
Ref 536038Mechanism of action of paracetamol. Am J Ther. 2005 Jan-Feb;12(1):46-55.
Ref 536186Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 536364Immunomodulatory effect of nonsteroidal anti-inflammatory drugs (NSAIDs) at the clinically available doses. Arch Pharm Res. 2007 Jan;30(1):64-74.
Ref 536379Cyclooxygenase and nitric oxide synthase dependence of cutaneous reactive hyperemia in humans. Am J Physiol Heart Circ Physiol. 2007 Jul;293(1):H425-32. Epub 2007 Mar 16.
Ref 536391The aryl propionic acid R-flurbiprofen selectively induces p75NTR-dependent decreased survival of prostate tumor cells. Cancer Res. 2007 Apr 1;67(7):3254-62.
Ref 536838Emerging drugs for chemotherapy-induced mucositis. Expert Opin Emerg Drugs. 2008 Sep;13(3):511-22.
Ref 536976Cyclooxygenase inhibitors: instrumental drugs to understand cardiovascular homeostasis and arterial thrombosis. Cardiovasc Hematol Disord Drug Targets. 2008 Dec;8(4):268-77.
Ref 537263Naproxcinod, a new cyclooxygenase-inhibiting nitric oxide donator (CINOD). Expert Opin Biol Ther. 2009 May;9(5):649-57.
Ref 537349Emerging drug therapies in Huntington's disease. Expert Opin Emerg Drugs. 2009 Jun;14(2):273-97.
Ref 537872Interactions of PGH synthase isozymes-1 and -2 with NSAIDs. Ann N Y Acad Sci. 1994 Nov 15;744:50-7.
Ref 537903Pharmacology of prostaglandin endoperoxide synthase isozymes-1 and -2. Ann N Y Acad Sci. 1994 Apr 18;714:136-42.
Ref 544102Antinociceptive effects of NCX-701 (nitro-paracetamol) in neuropathic rats: enhancement of antinociception by co-administration with gabapentin. Br J Pharmacol. 2009 September; 158(2): 601-609.
Ref 550035Predicting Cyclooxygenase Inhibition by Three??imensional Pharmacophoric Profiling. Part I: Model Generation, Validation and Applicability in Ethnopharmacology. Molecular Informatics 01/2010; 29(1??):75 - 86.
Ref 550835US patent application no. 2007,0072,861, Method of using cyclooxygenase-2 inhibitors in the prevention of cardiovascular disorders.
Ref 550869CN patent application no. 104797935, A method for prognosis and treatment of cancer metastasis.
Ref 550919US patent application no. 6,673,908, Tumor necrosis factor receptor 2.
Ref 550923US patent application no. 7,022,689, 5-amidino-n-(2-aminophenethyl)-n-hydroxy-benzenesulffonamide derivative, medical composition containing the same, pharmaceutical use thereof and intermediate therefor.
Ref 550934WO patent application no. 1997,0297,75, Compositions comprising a cyclooxygenase-2 inhibitor and a leukotriene b4 receptor antagonist.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

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