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Description of Celecoxib: Celecoxib was developed by G. D. Searle & Company and
co-promoted by Monsanto Company (parent company of Searle) and Pfizer
under the brand name Celebrex. Monsanto merged with Pharmacia, from
which the Medical Research Division was acquired by Pfizer, giving
Pfizer ownership of Celebrex. The drug was at the core of a major patent
dispute that was resolved in Searle's favor (later Pfizer) in 2004. In
University of Rochester v. G.D. Searle & Co., 358 F.3d 916 (Fed. Cir.
2004), the University of Rochester claimed that United States Pat. No.
6,048,850 (which claimed a method of inhibiting COX-2 in humans using a
compound, without actually disclosing what that compound might be)
covered drugs such as celecoxib. The court ruled in favor of Searle,
holding in essence that the University had claimed a method requiring,
yet provided no written description of, a compound that could inhibit
COX-2 and therefore the patent was invalid.
MedKoo Code#: 200700
Chemical Formula: C17H14F3N3O2S
Exact Mass: 381.07588
Molecular Weight: 381.37
Elemental Analysis: C, 53.54; H, 3.70; F,
14.94; N, 11.02; O, 8.39; S, 8.41
Availability and price:
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Information about this agent
Celecoxib is a sulfa non-steroidal anti-inflammatory
drug (NSAID) used in the treatment of osteoarthritis, rheumatoid
arthritis, acute pain, painful menstruation and menstrual symptoms, and
to reduce numbers of colon and rectum polyps in patients with familial
adenomatous polyposis. It is marketed by Pfizer. It is known under the
brand name Celebrex or Celebra for arthritis and Onsenal for polyps.
Celecoxib is available by prescription in capsule form.
Pfizer sells celecoxib under the brand name Celebrex.
Celecoxib is not currently available as a generic in the United States,
because the intellectual property is still controlled by Pfizer.
However, in other countries, including India and the Philippines, it is
legally available as a generic under the brand names Cobix and Celcoxx.
XL Laboratories sells celecoxib under the brand name Selecap in Vietnam
and the Philippines. See
After the withdrawal of rofecoxib (Vioxx) from the
market in September 2004, Celebrex enjoyed a robust increase in sales.
However, the results of the APC trial in December of that year raised
concerns that Celebrex might carry risks similar to those of Vioxx, and
Pfizer announced a moratorium on direct-to-consumer advertising of
Celebrex soon afterwards. After a significant drop, sales of Celebrex
have recovered, and reached $2 billion in 2006. Pfizer resumed
advertising Celebrex in magazines in 2006, and resumed television
advertising in April 2007 with an unorthodox, 2˝ minute advertisement
which extensively discussed the adverse effects of Celebrex in
comparison with other anti-inflammatory drugs. The ad drew criticism
from the consumer advocacy group Public Citizen, which called the ad's
comparisons misleading. Pfizer has responded to Public Citizen's
concerns with assurances that they are truthfully advertising the risk
and benefits of Celebrex as set forth by the FDA.
In late 2007, Pfizer released another U.S. television ad for Celebrex,
which also discussed celecoxib's adverse effects in comparison with
those of other anti-inflammatory drugs. Dr. Simmons of Brigham Young
University, who discovered the COX-2 enzyme, is suing Pfizer to be
credited with discovery of the technique in 1989 that eventually led to
the drug, and for $1 billion USD, (The company has made about $30
billion from the drug as of 2006).
Research into cancer prevention
The role that celecoxib might have in reducing the
rates of certain cancers has been the subject of many studies. However,
given the side effects of anti-COX-2 on rates of heart disease, there is
no current medical recommendation to use this drug for cancer reduction.
Colorectal cancer risk is clearly reduced in people regularly taking a
NSAID like aspirin or celecoxib. In addition, some epidemiological
studies, and most preclinical studies pointed out that specific COX-2
inhibitors like celecoxib are more potent and less toxic than "older"
NSAIDs. Twelve carcinogenesis studies support that celecoxib is
strikingly potent to prevent intestinal cancer in rats or mice (data
available on the Chemoprevention Database). Small-scale clinical trials
in very high risk people (belonging to FAP families) also indicate that
celecoxib can prevent polyp growth. Hence large-scale randomized
clinical trials were undertaken and results published by N. Arber and M.
Bertagnolli in the New England Journal of Medicine, August 2006. Results
show a 33 to 45% polyp recurrence reduction in people taking 400–800 mg
celecoxib each day. However, serious cardiovascular events were
significantly more frequent in the celecoxib-treated groups (see above,
cardiovascular toxicity). Aspirin shows a similar (and possibly larger)
protective effect, has demonstrated cardioprotective effects and is
significantly cheaper, but there have been no head-to-head clinical
trials comparing the two drugs.
Research into cancer treatment
Different from cancer prevention, cancer treatment is
focused on the therapy of tumors that have already formed and have
established themselves inside the patient. Many studies are ongoing to
determine whether celecoxib might be useful for this latter condition.
However, during molecular studies in the laboratory, it became apparent
that celecoxib could interact with other intracellular components
besides its most famous target, cyclooxygenase 2 (COX-2). The discovery
of these additional targets has generated much controversy, and the
initial assumption that celecoxib reduces tumor growth primarily via the
inhibition of COX-2 became contentious.
Certainly, the inhibition of COX-2 is paramount for the
anti-inflammatory and analgesic function of celecoxib. However, whether
inhibition of COX-2 also plays a dominant role in this drug’s anticancer
effects is unclear. For example, a recent study with malignant tumor
cells showed that celecoxib could inhibit the growth of these cells in
vitro, but COX-2 played no role in this outcome; even more strikingly,
the anticancer effects of celecoxib were also obtained with the use of
cancer cell types that don’t even contain COX-2. Additional support for
the idea that other targets besides COX-2 are important for celecoxib's
anticancer effects has come from studies with chemically modified
versions of celecoxib. Several dozen analogs of celecoxib were generated
with small alterations in their chemical structures. Some of these
analogs retained COX-2 inhibitory activity, whereas many others didn't.
However, when the ability of all these compounds to kill tumor cells in
cell culture was investigated, it turned out that the antitumor potency
did not at all depend on whether or not the respective compound could
inhibit COX-2, showing that inhibition of COX-2 was not required for the
anticancer effects. One of these compounds,
2,5-dimethyl-celecoxib, which entirely lacks the ability to inhibit
COX-2, actually turned out to display stronger anticancer activity than
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