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Chemical Compound Review

Celebrex     4-[5-(4-methylphenyl)-3...

Synonyms: Celecoxi, Celebra, Celecox, Celocoxib, Eurocox, ...
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Disease relevance of Celebra


Psychiatry related information on Celebra


High impact information on Celebra


Chemical compound and disease context of Celebra


Biological context of Celebra


Anatomical context of Celebra

  • Celecoxib, but not SC-560, significantly increased leukocyte adherence, whereas SC-560, but not celecoxib, reduced gastric blood flow [24].
  • Celecoxib treatment caused exfoliation of the mucosal surface epithelium, but neither caused deep erosions or altered survivin expression [25].
  • These findings suggests that (i) aspirin and NCX-4016 trigger ATL formation in humans, (ii) celecoxib inhibits ATL formation and exacerbates the mucosal injury caused by low doses of aspirin, and (iii) the NO-donating moiety of NCX-4016 protects the gastric mucosa even in the presence of suppression of COX-1 and COX-2 [26].
  • Increased levels of PGs were found in the cerebrospinal fluid after carrageenan injection and were markedly reduced by celecoxib, but were not affected by SC-560 [27].
  • Here we show that DMC (and celecoxib) inhibits the proliferation of various multiple myeloma cell lines, including several (multi) drug-resistant variants [28].

Associations of Celebra with other chemical compounds

  • Western blotting was used to monitor the effects of the compounds on phosphorylation of the serine/threonine kinase Akt and extracellular signal-regulated kinase 2 (ERK2), two components of celecoxib-induced apoptosis signaling [21].
  • We compared small intestinal function and morphology in untreated wild-type, COX-1- and COX-2-deficient mice and the effect of indomethacin, selective COX-1 (SC-560), and COX-2 (celecoxib) inhibition [29].
  • METHODS: The effects of SC-560, celecoxib (selective COX-2 inhibitor), or a combination of both inhibitors on gastric damage and prostaglandin synthesis were determined [24].
  • METHODS: We conducted a randomized, controlled trial of selenomethionine 200 microg daily and/or celecoxib 200 mg twice daily (2 x 2 factorial design) among residents of Linxian, People's Republic of China. Subjects had histologically confirmed mild or moderate esophageal squamous dysplasia at baseline [30].
  • By contrast, both ibuprofen and celecoxib suppressed a biochemical index of COX-2 activity (endotoxin induced PGE2 in whole blood ex vivo) to a comparable degree (-93.3 +/- 2% vs. -83 +/- 6.1%) [31].
  • An alternative mechanism is proposed for the cancer-preventive role of celecoxib other than the classic mechanism of inhibiting prostaglandin synthesis, stressing mainly the role of cyclin D1 [32].
  • The pharmacokinetics of celecoxib is not significantly affected by the concomitant administration of phenytoin [33].
  • In contrast to nonresponders, those patients with complete and partial responses had a significant decrease in the level of urinary 11alpha-hydroxy-9,15-dioxo-2,3,4,5-tetranor-prostane-1,20-dioic acid (PGE-M), the major metabolite of prostaglandin E(2), after 1 week of celecoxib administration [34].

Gene context of Celebra

  • We examined the variability in degree and selectivity of COX-2 inhibition in humans in response to celecoxib and rofecoxib [35].
  • Furthermore, long-term celecoxib administration in wild-type animals was associated with similar damage as in the COX-2(-/-) mice [29].
  • However, celecoxib, having caused no damage in COX-1(+/+) animals, caused small bowel ulcers in COX-1(-/-) animals [29].
  • Treatment of various pancreatic cancer cells with celecoxib suppressed VEGF expression at both the mRNA and protein level in a dose-dependent manner [36].
  • Cyclooxygenase-2 expression and effect of celecoxib in gastric adenomas of trefoil factor 1-deficient mice [37].
  • A genetically null mutant of Drosophila Shab (Kv2) channels reproduced the cardiac effect of celecoxib, and the drug was unable to further enhance the effect of the mutation [38].

Analytical, diagnostic and therapeutic context of Celebra


  1. The effect of celecoxib, a cyclooxygenase-2 inhibitor, in familial adenomatous polyposis. Steinbach, G., Lynch, P.M., Phillips, R.K., Wallace, M.H., Hawk, E., Gordon, G.B., Wakabayashi, N., Saunders, B., Shen, Y., Fujimura, T., Su, L.K., Levin, B. N. Engl. J. Med. (2000) [Pubmed]
  2. Efficacy of rofecoxib, celecoxib, and acetaminophen in osteoarthritis of the knee: a randomized trial. Geba, G.P., Weaver, A.L., Polis, A.B., Dixon, M.E., Schnitzer, T.J. JAMA (2002) [Pubmed]
  3. 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. Silverstein, F.E., Faich, G., Goldstein, J.L., Simon, L.S., Pincus, T., Whelton, A., Makuch, R., Eisen, G., Agrawal, N.M., Stenson, W.F., Burr, A.M., Zhao, W.W., Kent, J.D., Lefkowith, J.B., Verburg, K.M., Geis, G.S. JAMA (2000) [Pubmed]
  4. Risk of cardiovascular events associated with selective COX-2 inhibitors. Mukherjee, D., Nissen, S.E., Topol, E.J. JAMA (2001) [Pubmed]
  5. Atorvastatin and celecoxib inhibit prostate PC-3 tumors in immunodeficient mice. Zheng, X., Cui, X.X., Avila, G.E., Huang, M.T., Liu, Y., Patel, J., Kong, A.N., Paulino, R., Shih, W.J., Lin, Y., Rabson, A.B., Reddy, B.S., Conney, A.H. Clin. Cancer Res. (2007) [Pubmed]
  6. Efficacy and safety of epicutaneous ketoprofen in Transfersome (IDEA-033) versus oral celecoxib and placebo in osteoarthritis of the knee: multicentre randomised controlled trial. Rother, M., Lavins, B.J., Kneer, W., Lehnhardt, K., Seidel, E.J., Mazgareanu, S. Ann. Rheum. Dis. (2007) [Pubmed]
  7. Celecoxib prevents neuroblastoma tumor development and potentiates the effect of chemotherapeutic drugs in vitro and in vivo. Ponthan, F., Wickström, M., Gleissman, H., Fuskevåg, O.M., Segerström, L., Sveinbjörnsson, B., Redfern, C.P., Eksborg, S., Kogner, P., Johnsen, J.I. Clin. Cancer Res. (2007) [Pubmed]
  8. Acute onset of auditory hallucinations after initiation of celecoxib therapy. Lantz, M.S., Giambanco, V. The American journal of psychiatry. (2000) [Pubmed]
  9. Celecoxib augmentation of continuously ill patients with schizophrenia. Rapaport, M.H., Delrahim, K.K., Bresee, C.J., Maddux, R.E., Ahmadpour, O., Dolnak, D. Biol. Psychiatry (2005) [Pubmed]
  10. Surveillance colonoscopy or chemoprevention with COX-2 inhibitors in average-risk post-polypectomy patients: a decision analysis. Arguedas, M.R., Heudebert, G.R., Wilcox, C.M. Aliment. Pharmacol. Ther. (2001) [Pubmed]
  11. Long-term efficacy and safety of celecoxib in Alzheimer's disease. Soininen, H., West, C., Robbins, J., Niculescu, L. Dementia and geriatric cognitive disorders (2007) [Pubmed]
  12. Celecoxib, a cyclooxygenase 2 inhibitor as a potential chemopreventive to UV-induced skin cancer: a study in the hairless mouse model. Orengo, I.F., Gerguis, J., Phillips, R., Guevara, A., Lewis, A.T., Black, H.S. Archives of dermatology. (2002) [Pubmed]
  13. Rofecoxib vs celecoxib vs acetaminophen for treatment of osteoarthritis. Henderson, P. JAMA (2002) [Pubmed]
  14. Anti-inflammatory and upper gastrointestinal effects of celecoxib in rheumatoid arthritis: a randomized controlled trial. Simon, L.S., Weaver, A.L., Graham, D.Y., Kivitz, A.J., Lipsky, P.E., Hubbard, R.C., Isakson, P.C., Verburg, K.M., Yu, S.S., Zhao, W.W., Geis, G.S. JAMA (1999) [Pubmed]
  15. Rofecoxib vs celecoxib vs acetaminophen for treatment of osteoarthritis. Bierma-Zeinstra, S.M., Bohnen, A.M., Berger, M.Y., Thomas, S. JAMA (2002) [Pubmed]
  16. Nonsteroidal anti-inflammatory drugs as anticancer agents: mechanistic, pharmacologic, and clinical issues. Thun, M.J., Henley, S.J., Patrono, C. J. Natl. Cancer Inst. (2002) [Pubmed]
  17. Celecoxib versus diclofenac in long-term management of rheumatoid arthritis: randomised double-blind comparison. Emery, P., Zeidler, H., Kvien, T.K., Guslandi, M., Naudin, R., Stead, H., Verburg, K.M., Isakson, P.C., Hubbard, R.C., Geis, G.S. Lancet (1999) [Pubmed]
  18. Effects of celecoxib and naproxen on renal function in nonazotemic patients with cirrhosis and ascites. Clària, J., Kent, J.D., López-Parra, M., Escolar, G., Ruiz-Del-Arbol, L., Ginès, P., Jiménez, W., Vucelic, B., Arroyo, V. Hepatology (2005) [Pubmed]
  19. Direct evidence for a role of cyclooxygenase 2-derived prostaglandin E2 in human head and neck xenograft tumors. Zweifel, B.S., Davis, T.W., Ornberg, R.L., Masferrer, J.L. Cancer Res. (2002) [Pubmed]
  20. Cyclooxygenase-2, player or spectator in cyclooxygenase-2 inhibitor-induced apoptosis in prostate cancer cells. Song, X., Lin, H.P., Johnson, A.J., Tseng, P.H., Yang, Y.T., Kulp, S.K., Chen, C.S. J. Natl. Cancer Inst. (2002) [Pubmed]
  21. Using cyclooxygenase-2 inhibitors as molecular platforms to develop a new class of apoptosis-inducing agents. Zhu, J., Song, X., Lin, H.P., Young, D.C., Yan, S., Marquez, V.E., Chen, C.S. J. Natl. Cancer Inst. (2002) [Pubmed]
  22. Targeting cyclooxygenase 2 and HER-2/neu pathways inhibits colorectal carcinoma growth. Mann, M., Sheng, H., Shao, J., Williams, C.S., Pisacane, P.I., Sliwkowski, M.X., DuBois, R.N. Gastroenterology (2001) [Pubmed]
  23. CD24 is a new oncogene, early at the multistep process of colorectal cancer carcinogenesis. Sagiv, E., Memeo, L., Karin, A., Kazanov, D., Jacob-Hirsch, J., Mansukhani, M., Rechavi, G., Hibshoosh, H., Arber, N. Gastroenterology (2006) [Pubmed]
  24. NSAID-induced gastric damage in rats: requirement for inhibition of both cyclooxygenase 1 and 2. Wallace, J.L., McKnight, W., Reuter, B.K., Vergnolle, N. Gastroenterology (2000) [Pubmed]
  25. Survivin: a novel target for indomethacin-induced gastric injury. Chiou, S.K., Tanigawa, T., Akahoshi, T., Abdelkarim, B., Jones, M.K., Tarnawski, A.S. Gastroenterology (2005) [Pubmed]
  26. Interaction of a selective cyclooxygenase-2 inhibitor with aspirin and NO-releasing aspirin in the human gastric mucosa. Fiorucci, S., Santucci, L., Wallace, J.L., Sardina, M., Romano, M., del Soldato, P., Morelli, A. Proc. Natl. Acad. Sci. U.S.A. (2003) [Pubmed]
  27. Pharmacological analysis of cyclooxygenase-1 in inflammation. Smith, C.J., Zhang, Y., Koboldt, C.M., Muhammad, J., Zweifel, B.S., Shaffer, A., Talley, J.J., Masferrer, J.L., Seibert, K., Isakson, P.C. Proc. Natl. Acad. Sci. U.S.A. (1998) [Pubmed]
  28. Multitarget inhibition of drug-resistant multiple myeloma cell lines by dimethyl-celecoxib (DMC), a non-COX-2 inhibitory analog of celecoxib. Kardosh, A., Soriano, N., Liu, Y.T., Uddin, J., Petasis, N.A., Hofman, F.M., Chen, T.C., Schönthal, A.H. Blood (2005) [Pubmed]
  29. COX-1 and 2, intestinal integrity, and pathogenesis of nonsteroidal anti-inflammatory drug enteropathy in mice. Sigthorsson, G., Simpson, R.J., Walley, M., Anthony, A., Foster, R., Hotz-Behoftsitz, C., Palizban, A., Pombo, J., Watts, J., Morham, S.G., Bjarnason, I. Gastroenterology (2002) [Pubmed]
  30. Randomized, placebo-controlled, esophageal squamous cell cancer chemoprevention trial of selenomethionine and celecoxib. Limburg, P.J., Wei, W., Ahnen, D.J., Qiao, Y., Hawk, E.T., Wang, G., Giffen, C.A., Wang, G., Roth, M.J., Lu, N., Korn, E.L., Ma, Y., Caldwell, K.L., Dong, Z., Taylor, P.R., Dawsey, S.M. Gastroenterology (2005) [Pubmed]
  31. Systemic biosynthesis of prostacyclin by cyclooxygenase (COX)-2: the human pharmacology of a selective inhibitor of COX-2. McAdam, B.F., Catella-Lawson, F., Mardini, I.A., Kapoor, S., Lawson, J.A., FitzGerald, G.A. Proc. Natl. Acad. Sci. U.S.A. (1999) [Pubmed]
  32. Gene expression analysis proposes alternative pathways for the mechanism by which celecoxib selectively inhibits the growth of transformed but not normal enterocytes. Sagiv, E., Rozovski, U., Kazanov, D., Liberman, E., Arber, N. Clin. Cancer Res. (2007) [Pubmed]
  33. Effect of phenytoin on celecoxib pharmacokinetics in patients with glioblastoma. Grossman, S.A., Olson, J., Batchelor, T., Peereboom, D., Lesser, G., Desideri, S., Ye, X., Hammour, T., Supko, J.G. Neuro-oncology (2008) [Pubmed]
  34. A phase II study of celecoxib in combination with paclitaxel, carboplatin, and radiotherapy for patients with inoperable stage IIIA/B non-small cell lung cancer. Mutter, R., Lu, B., Carbone, D.P., Csiki, I., Moretti, L., Johnson, D.H., Morrow, J.D., Sandler, A.B., Shyr, Y., Ye, F., Choy, H. Clin. Cancer Res. (2009) [Pubmed]
  35. Marked interindividual variability in the response to selective inhibitors of cyclooxygenase-2. Fries, S., Grosser, T., Price, T.S., Lawson, J.A., Kapoor, S., DeMarco, S., Pletcher, M.T., Wiltshire, T., FitzGerald, G.A. Gastroenterology (2006) [Pubmed]
  36. Celecoxib inhibits vascular endothelial growth factor expression in and reduces angiogenesis and metastasis of human pancreatic cancer via suppression of Sp1 transcription factor activity. Wei, D., Wang, L., He, Y., Xiong, H.Q., Abbruzzese, J.L., Xie, K. Cancer Res. (2004) [Pubmed]
  37. Cyclooxygenase-2 expression and effect of celecoxib in gastric adenomas of trefoil factor 1-deficient mice. Saukkonen, K., Tomasetto, C., Narko, K., Rio, M.C., Ristimäki, A. Cancer Res. (2003) [Pubmed]
  38. Inhibition of delayed rectifier potassium channels and induction of arrhythmia: a novel effect of celecoxib and the mechanism underlying it. Frolov, R.V., Berim, I.G., Singh, S. J. Biol. Chem. (2008) [Pubmed]
  39. Up-regulation of the enzymes involved in prostacyclin synthesis via Ras induces vascular endothelial growth factor. Buchanan, F.G., Chang, W., Sheng, H., Shao, J., Morrow, J.D., DuBois, R.N. Gastroenterology (2004) [Pubmed]
  40. Suppression of Peutz-Jeghers polyposis by inhibition of cyclooxygenase-2. Udd, L., Katajisto, P., Rossi, D.J., Lepistö, A., Lahesmaa, A.M., Ylikorkala, A., Järvinen, H.J., Ristimäki, A.P., Mäkelä, T.P. Gastroenterology (2004) [Pubmed]
  41. Prevention of colon cancer by low doses of celecoxib, a cyclooxygenase inhibitor, administered in diet rich in omega-3 polyunsaturated fatty acids. Reddy, B.S., Patlolla, J.M., Simi, B., Wang, S.H., Rao, C.V. Cancer Res. (2005) [Pubmed]
  42. Chemoprevention of breast cancer in rats by celecoxib, a cyclooxygenase 2 inhibitor. Harris, R.E., Alshafie, G.A., Abou-Issa, H., Seibert, K. Cancer Res. (2000) [Pubmed]
  43. Suppression of prostate carcinogenesis by dietary supplementation of celecoxib in transgenic adenocarcinoma of the mouse prostate model. Gupta, S., Adhami, V.M., Subbarayan, M., MacLennan, G.T., Lewin, J.S., Hafeli, U.O., Fu, P., Mukhtar, H. Cancer Res. (2004) [Pubmed]
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