COX-2 inhibitor
COX-2 selektivni inhibitor je forma steroidnog antiinflamatornog leka (NSAID) koji direktno deluju na COX-2, enzim koji je odgovoran za inflamaciju i bol. Selektivan inhibicija COX-2 enzima redukuje rizik pojave peptične ulceracije. To je glavna karakteristika celekoksiba, rofekoksiba i drugih članova ove klase lekova. COX-2 selektivnost ne umanjuje druge nepoželjne efekte NSAID lekova (pogotovu povišeni rizik od bubrežne insuficijencije), a rezultati nekih istraživanja ukazuju i na povišeni rizik od srčanog udara, tromboze i moždanog udara kao posledica relativnog povišenja nivoa tromboksana. Rofekoksib (poznatiji kao Vioxx) je povučen sa tržišta 2004 zbog ovih problema.
Istorija istraživanja uredi
COX-2 gen miša je klonirao UCLA naučnik dr. Harvi Herčman.[1] Enzim je otkrio 1988. Danijel Simons.[2] On je odmah uvideo značaj svog otkrića, te je istog dana odredio sekvencu enzima. Naknadno je kompanija Pfizer, sa kojom je Simons imao ugovor, navodno raskinula ugovor i odbila ispoštuje njegova autorska prava, iz kog razloga je usledio dugotrajni sudski spor.[3][4]
Reference uredi
- ↑ Kujubu DA, Fletcher BS, Varnum BC, Lim RW, Herschman HR (July 1991). „TIS10, a phorbol ester tumor promoter-inducible mRNA from Swiss 3T3 cells, encodes a novel prostaglandin synthase/cyclooxygenase homologue”. J. Biol. Chem. 266 (20): 12866–72. PMID 1712772.
- ↑ Xie WL, Chipman JG, Robertson DL, Erikson RL, Simmons DL (April 1991). „Expression of a mitogen-responsive gene encoding prostaglandin synthase is regulated by mRNA splicing”. Proceedings of the National Academy of Sciences of the United States of America 88 (7): 2692–6. DOI:10.1073/pnas.88.7.2692. PMC 51304. PMID 1849272.
- ↑ Yajnik J (2006-10-27). „University sues Pfizer over COX-2 research”. The Scientist. Arhivirano iz originala na datum 2009-02-03. Pristupljeno 11. 11. 2010.
- ↑ Tom Harvey (21. 09. 2010.). „BYU spices up Celebrex lawsuit against Pfizer”. The Salt Lake Tribune. Pristupljeno 28. 02. 2011.
Literatura uredi
- Green GA (2001). „Understanding NSAIDs: from aspirin to COX-2”. Clin Cornerstone 3 (5): 50–60. DOI:10.1016/S1098-3597(01)90069-9. PMID 11464731.
- Malhotra S, Shafiq N, Pandhi P (2004). „COX-2 Inhibitors: A CLASS Act or Just VIGORously Promoted”. MedGenMed 6 (1): 6. PMC 1140734. PMID 15208519.
- Montero Fernández MJ, Rodríguez Alcalá FJ, Valles Fernández N, López de Castro F, Esteban Tudela M, Cordero García B (October 2002). „[At what care level are cyclo-oxygenase-2 inhibitors prescribed?”] (Spanish; Castilian). Aten Primaria 30 (6): 363–7. PMID 12396942. Arhivirano iz originala na datum 2007-07-08. Pristupljeno 2014-01-25.
- "You and A: Arthritis drugs. Pain and confusion"; Francesca Lunzer Kritz; Washington Post; Sept. 4, 2001; HE01.
- "Vioxx (rofecoxib) reduces night-time osteoarthritis pain better than celecoxib or acetaminophen"; European League Against Rheumatism (EULAR) conference proceedings.
- "Will the promise of the COX-II selective NSAIDs come to fruition?"; Drug Ther Perspect 17(11); 6-10, 2001.
- Chancellor JV, Hunsche E, de Cruz E, Sarasin FP (2001). „Economic evaluation of celecoxib, a new cyclo-oxygenase 2 specific inhibitor, in Switzerland”. Pharmacoeconomics 19 Suppl 1: 59–75. DOI:10.2165/00019053-200119001-00005. PMID 11280106.
- Kamath CC, Kremers HM, Vanness DJ, O'Fallon WM, Cabanela RL, Gabriel SE (2003). „The cost-effectiveness of acetaminophen, NSAIDs, and selective COX-2 inhibitors in the treatment of symptomatic knee osteoarthritis”. Value Health 6 (2): 144–57. DOI:10.1046/j.1524-4733.2003.00215.x. PMID 12641865. Arhivirano iz originala na datum 2013-01-18. Pristupljeno 2014-01-25.
- "Osteoarthritis drug Celebrex (celecoxib) less likely to cause increased blood pressure than Vioxx (rofecoxib)"; European League Against Rheumatism (EULAR) conference proceedings.
- Johnsen JI, Lindskog M, Ponthan F, et al. (October 2004). „Cyclooxygenase-2 is expressed in neuroblastoma, and nonsteroidal anti-inflammatory drugs induce apoptosis and inhibit tumor growth in vivo”. Cancer Res. 64 (20): 7210–5. DOI:10.1158/0008-5472.CAN-04-1795. PMID 15492235.
- Dai C, Stafford RS, Alexander GC. National Trends in Cox-2 inhibitor use since market release: non-selective diffusion of a selectively cost-effective innovation Archives of Internal Medicine. 2005; 165: 171-177.
- Editorial: Solomon DH, Avorn J. Coxibs, science, and the public trust Archives of Internal Medicine. 2005;165:158-160