View source for Etoricoxib

{{drugbox |
| IUPAC_name = 5-chloro-6'-methyl-3-[4-(methylsulfonyl)phenyl]-<br>2,3'-bipyridine
| image = Etoricoxib.svg
| CAS_number = 202409-33-4
| ATC_prefix = M01
| ATC_suffix = AH05
| PubChem = 123619
| DrugBank = 
| C = 18 | H = 15 | Cl = 1 | N = 2 | O = 2 | S = 1
| molecular_weight = 358.842 g/mol
| bioavailability = 100%
| protein_bound = 92%
| metabolism = [[Liver|Hepatic]], [[Cytochrome P450 oxidase|CYP]] extensively involved (mainly [[CYP3A4]])
| elimination_half-life = 22 hours
| excretion = [[Kidney|Renal]] (70%) and fecal (20%)
| pregnancy_category = Not recommended
| legal_UK = POM
| routes_of_administration = Oral
}}

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==Overview==
'''Etoricoxib''' (brand name '''Arcoxia''' worldwide; also '''Algix''' and '''Tauxib''' in Italy) is a new [[COX-2 selective inhibitor]] (approx. 106.0 times more selective for COX-2 inhibition over COX-1) from [[Merck & Co.]] Doses are 60, 90&nbsp;mg/day for chronic pain and 120&nbsp;mg/day for acute pain. Currently it is approved in more than 60 countries worldwide but not in the US, where the [[Food and Drug Administration]] (FDA) require additional safety and efficacy data for etoricoxib before it will issue approval. Current therapeutic indications are: treatment of [[rheumatoid arthritis]], [[osteoarthritis]], [[ankylosing spondylitis]], chronic [[low back pain]], acute pain and [[gout]]. Note that approved indications differ by country.

Like any other [[COX-2 selective inhibitor]], '''Etoricoxib''' selectively inhibits isoform 2 of cyclo-oxigenase enzyme (COX-2). This reduces the generation of [[prostaglandins]] (PGs) from arachidonic acid. Among the different functions exerted by PGs, their role in the inflammation cascade should be highlighted. 
[[COX-2 selective inhibitor]] (aka "COXIB") showed less marked activity on type 1 cycloxigenase compared to traditional [[non-steroidal anti-inflammatory drug|non-steroidal anti-inflammatory drugs]] (NSAID). This reduced activity is the cause of reduced gastrointestinal toxicity, as demonstrated in several large clinical trials performed with different COXIB (see below links on NEJM and The Lancet).

Some clinical trials and meta-analysis showed that treatment with ''COXIB'' led to increased incidence of adverse cardiovascular events compared to placebo. Because of these results, some molecules were withdrawn from the market ([[Rofecoxib]], September 2004 and [[Valdecoxib]], April 2005). In addition, the FDA and EMEA (USA and European Community Health Authorities respectively) started a revision process of the entire class of both NSAID and COX-2 inhibitors.

FDA concluded its revision on April 6, 2005: the final document can be found at: http://www.fda.gov/cder/drug/infopage/COX2/NSAIDdecisionMemo.pdf

EMEA concluded its revision on June 27, 2005: the final document can be found at: http://www.emea.europa.eu/pdfs/human/press/pr/20776605en.pdf

On April 27, 2007, the Food and Drug Administration issued Merck a "non-approvable letter" for Arcoxia. The letter said Merck needs to provide more test results showing that Arcoxia's benefits outweigh its risks before it has another chance of getting approved.


==External links==
* [http://www.emea.europa.eu/ European Medicines Agency (EMEA) - Homepage] - [http://www.emea.europa.eu/Cox2inhibitors.htm]
* [http://www.fda.gov/ US Food and Drug Administration (FDA) - Homepage] - [http://www.fda.gov/cder/drug/infopage/COX2/default.htm]
* [http://content.nejm.org/cgi/content/abstract/343/21/1520 (VIGOR study on The New England Journal of Medicine - NEJM)]
* [http://www.thelancet.com/journals/lancet/article/PIIS0140673606696669/abstract (MEDAL study on The Lancet)]



{{NSAIDs}}
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[[Category:Non-steroidal anti-inflammatory drugs]]
[[Category:Drugs]]

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