Metagenics Inc. (San Clemente, CA), a leading developer and
manufacturer of science-based medical foods and nutraceuticals,
announced in October that it has been awarded 3 new patents for 2 of
its ingredients derived from hops (Humulus lupulus) with anti-inflammatory properties.1 Metagenics uses the hops-derived ingredient TetraseTM in its supplements Kaprex® and Kaprex® AI, and the hops-derived ingredient LuduxinTM is included in the medical food UltraMeal® Plus 360 and the nutraceutical InsinaseTM.
One of the new patents protects the composition of Luduxin and its
use in preserving joint health, while the other 2 patents protect the
composition of Tetrase and its use in supporting the management of
inflammation. Metagenics describes the ingredients as selective kinase
response modulators (SKRMs), meaning that they modulate the enzymes
that chemically modify other proteins and regulate cellular pathways,
particularly those involved in the transmission of signals within
cells. According to a press release distributed by Metagenics, many
prevalent health issues can be attributed to inflammation and/or have
underlying kinase signaling components.
“The significance of these three patents is that the formalization
of the discoveries that Metagenics has made on the anti-inflammatory
properties of specific lipophilic extracts of hops represents the first
time that these properties have been understood mechanistically and in
terms of human clinical pharmacology,” explained Metagenics’ Chief
Science Officer Jeff Bland, PhD (e-mail, November 7, 2007). “These
patents also frame a fundamental discovery that the Metagenics research
team has made related to how phytochemicals can influence gene
expression and proteomic/metabolomic activity, which in turn alters the
phenotype of the cell, tissue, organ or organ system. In essence we
feel that we have discovered a fundamental mechanism by which
phytochemicals alter physiological function that is beyond that of the
hops discoveries themselves.”
Dr. Bland added that the method by which Metagenics researched and
developed Luduxin and Tetrase can be used to discover and produce other
natural product-derived therapeutics with enhanced safety and efficacy,
which the company should then be able to enter onto the market over the
next several years. “The Metagenics product pipeline is very rich due
to our ability to leverage the SKRM discovery process that we have
pioneered,” said Dr. Bland.
According to Dr. Bland, multiple studies concerning Luduxin and
Tetrase have been published in journals or presented at key scientific
meetings. Several studies have investigated the safety and efficacy of
Luduxin and/or Tetrase as principal ingredients of a
phytochemical-based anti-inflammatory formula also consisting of
rosemary (Rosmarinus officinalis) leaf extract and oleanolic acid from olive (Olea europa).2,3,4 The most recent report, published in the Canadian Journal of Physiology and Pharmacology
in October, examined multiple previous studies of the formula,
documenting its efficacy in trials for alleviating pain from
osteoarthritis and joint discomfort, as well as its safety as shown
through animal and human data.2 Metagenics is also looking for additional applications for the SKRM technology.1
A hops extract called PerluxanTM was introduced to the market several years ago for the purpose of treating pain caused by inflammation.5
According to Dr. Bland, Perluxan, which was ultimately licensed to
Lipoprotein Technologies, was created through earlier work from the
developers of Luduxin and Tetrase.
“Our continued work as leaders in this field since 1999 led us to
discover and develop both Luduxin and Tetrase that have superior safety
and efficacy profiles to that of Perluxan,” said Dr. Bland. “We have
data comparing the anti-inflammatory activity of Luduxin to that of the
most common herbal anti-inflammatory extracts showing superiority in
both anti-inflammatory activity and safety. These differences we
believe are a result of the fact that both Luduxin and Tetrase work by
a different mechanism than the traditional herbal anti-inflammatory
agents that inhibit cyclooxygenase 1 and/or 2 enzymes.”
Dr. Bland explained that Luduxin and Tetrase have been found to have
a previously unknown mechanism of action. This novel mode of action
causes the ingredients to only impact the sites in the body where
inflammation is present and not adversely influence the normal
“housekeeping function” of the COX-1 and COX-2 genes that are necessary
for proper immune function and protection of the integrity of the
gastrointestinal, vascular endothelial and kidney functions.
Metagenics products are currently sold solely through licensed
healthcare providers. More information about Metagenics and its
products is available at the website http://www.metagenics.com/.
—Courtney Cavaliere
References
1Metagenics Inc. awarded three patents for the discovery of LuduxinTM and TetraseTM, all-natural anti-inflammatory agents derived from hops [press release]. San Clemente, CA: Metagenics Inc.; October 22, 2007.
2Minich
DM, Bland JS, Katke J, et al. Clinical safety and efficacy of NG440: a
novel combination of rho iso-alpha acids from hops, rosemary, and
oleanolic acid for inflammatory conditions. Can J Physiol Pharmacol. 2007;85:872-883.
3Lukaczer
D, Darland G, Tripp M, et al. A pilot trial evaluating Meta050, a
proprietary combination of reduced iso-alph acids, rosemary extract and
oleanolic acid in patients with arthritis and fibromyalgia. Phytother Res. 2005;19:864-869.
4Tripp
M, Darland G, Lerman R, Lukaczer D, Bland J. Hop and modified hop
extracts have potent in vitro anti-inflammatory properties. Acta Hort. 2005;668:217-228.
5Metagenics gets patents for hops joint formulas. NutraIngredients.com. October 22, 2007. Available at: http://www.nutraingredients-usa.com/news/ng.asp?id=80784-metagenics-luduxin-tetrase. Accessed November 5, 2007. |